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GAL2 receptor

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Target id: 244

Nomenclature: GAL2 receptor

Family: Galanin receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 387 17q25.1 GALR2 galanin receptor 2
Mouse 7 371 11 81.1 cM Galr2 galanin receptor 2
Rat 7 372 10q32.1 Galr2 galanin receptor 2
Previous and Unofficial Names Click here for help
GALNR2
Database Links Click here for help
Specialist databases
GPCRdb galr2_human (Hs), galr2_mouse (Mm), galr2_rat (Rn)
Other databases
Alphafold O43603 (Hs), O88854 (Mm), O08726 (Rn)
ChEMBL Target CHEMBL3176 (Hs), CHEMBL5577 (Rn)
Ensembl Gene ENSG00000182687 (Hs), ENSMUSG00000020793 (Mm), ENSRNOG00000061733 (Rn)
Entrez Gene 8811 (Hs), 14428 (Mm), 29234 (Rn)
Human Protein Atlas ENSG00000182687 (Hs)
KEGG Gene hsa:8811 (Hs), mmu:14428 (Mm), rno:29234 (Rn)
OMIM 603691 (Hs)
Pharos O43603 (Hs)
RefSeq Nucleotide NM_003857 (Hs), NM_010254 (Mm), NM_019172 (Rn)
RefSeq Protein NP_003848 (Hs), NP_034384 (Mm), NP_062045 (Rn)
UniProtKB O43603 (Hs), O88854 (Mm), O08726 (Rn)
Wikipedia GALR2 (Hs)
Natural/Endogenous Ligands Click here for help
galanin {Sp: Human} , galanin {Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat}
spexin-1 {Sp: Human}
Potency order of endogenous ligands (Human)
galanin-like peptide (GALP, Q9UBC7) ≥ galanin (GAL, P22466)  [41]

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I][Tyr26]galanin (pig) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.5 – 9.9 pKd 6,17
⤷ pKd 9.9 (Kd 1.2x10-10 M) [17]
pKd 9.5 (Kd 3.1x10-10 M) [6]
[125I][Tyr26]galanin (human) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.5 – 9.6 pKd 5,26
⤷ pKd 9.5 – 9.6 (Kd 3.1x10-10 – 2.4x10-10 M) [5,26]
[125I][Tyr26]galanin (human) Peptide Ligand is labelled Ligand is radioactive Mm Agonist 9.3 pKd 42
⤷ pKd 9.3 (Kd 4.7x10-10 M) [42]
[125I][Tyr26]galanin (human) Peptide Ligand is labelled Ligand is radioactive Rn Agonist 9.2 pKd 61
⤷ pKd 9.2 (Kd 5.9x10-10 M) [61]
[125I][Tyr26]galanin (pig) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Agonist 8.4 – 9.9 pKd 12,18,54,61
⤷ pKd 8.4 – 9.9 (Kd 4x10-9 – 1.3x10-10 M) [12,18,54,61]
galmic Small molecule or natural product Rn Agonist <5.0 pKd 3,33
⤷ pKd <5.0 (Kd >1x10-5 M) [3,33]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 9.1 pKi 53
⤷ pKi 9.1 (Ki 7x10-10 M) [53]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 9.0 – 9.3 pKi 53-54
⤷ pKi 9.0 – 9.3 (Ki 1.05x10-9 – 5x10-10 M) [53-54]
galanin(1-20) (human) Peptide Hs Agonist 9.1 pKi 5
⤷ pKi 9.1 (Ki 7.8x10-10 M) [5]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Hs Full agonist 9.0 pKi 5
⤷ pKi 9.0 (Ki 9.1x10-10 M) [5]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.0 pKi 6
⤷ pKi 9.0 (Ki 9.5x10-10 M) [6]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.6 – 9.1 pKi 5-6,48
⤷ pKi 8.6 – 9.1 (Ki 2.34x10-9 – 8.6x10-10 M) [5-6,48]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.3 – 9.3 pKi 33,42,54,60-62
⤷ pKi 8.3 – 9.3 (Ki 5.6x10-9 – 5.6x10-10 M) [33,42,54,60-62]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 8.5 – 8.8 pKi 5-6,36,44,47,55
⤷ pKi 8.5 – 8.8 (Ki 2.98x10-9 – 1.54x10-9 M) [5-6,36,44,47,55]
galanin {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 8.6 pKi 54
⤷ pKi 8.6 (Ki 2.51x10-9 M) [54]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Rn Agonist 8.6 pKi 5
⤷ pKi 8.6 (Ki 2.51x10-9 M) [5]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 8.5 pKi 6
⤷ pKi 8.5 (Ki 2.88x10-9 M) [6]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 8.5 pKi 5
⤷ pKi 8.5 (Ki 3.5x10-9 M) [5]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 8.4 pKi 42
⤷ pKi 8.4 (Ki 3.9x10-9 M) [42]
galanin(2-30) (human) Peptide Click here for species-specific activity table Hs Full agonist 8.0 – 8.7 pKi 5,11
⤷ pKi 8.0 – 8.7 (Ki 1x10-8 – 1.8x10-9 M) [5,11]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 7.9 – 8.8 pKi 5-6,8
⤷ pKi 7.9 – 8.8 (Ki 1.3x10-8 – 1.6x10-9 M) [5-6,8]
galanin(1-19) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist 8.3 pKi 62
⤷ pKi 8.3 (Ki 4.7x10-9 M) [62]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 7.9 – 8.7 pKi 42,53-54,60-62
⤷ pKi 7.9 – 8.7 (Ki 1.3x10-8 – 1.8x10-9 M) [42,53-54,60-62]
J20 (galanin analogue) Peptide Click here for species-specific activity table Hs Agonist 8.3 pKi 45
⤷ pKi 8.3 (Ki 4.9x10-9 M) [45]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 8.3 pKi 6
⤷ pKi 8.3 (Ki 4.9x10-9 M) [6]
M1153 Peptide Click here for species-specific activity table Hs Agonist 8.3 pKi 47
⤷ pKi 8.3 (Ki 4.98x10-9 M) [47]
M617 Peptide Click here for species-specific activity table Hs Agonist 8.2 pKi 36
⤷ pKi 8.2 (Ki 5.71x10-9 M) [36]
M242 Peptide Click here for species-specific activity table Hs Agonist 8.2 pKi 48
⤷ pKi 8.2 (Ki 5.84x10-9 M) [48]
galanin(1-12) Peptide Hs Agonist 8.2 pKi 5
⤷ pKi 8.2 (Ki 6.4x10-9 M) [5]
M1145 Peptide Click here for species-specific activity table Hs Full agonist 8.2 pKi 44
⤷ pKi 8.2 (Ki 6.55x10-9 M) [44]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Full agonist 8.2 pKi 42
⤷ pKi 8.2 (Ki 6.8x10-9 M) [42]
[D-Trp2]galanin-(1-29) Peptide Rn Full agonist 8.1 pKi 53
⤷ pKi 8.1 (Ki 7x10-9 M) [53]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Full agonist 7.3 – 8.7 pKi 42,60-62
⤷ pKi 7.3 – 8.7 (Ki 5.6x10-8 – 1.9x10-9 M) [42,60-62]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Mm Agonist 7.9 pKi 42
⤷ pKi 7.9 (Ki 1.18x10-8 M) [42]
Gal-B2-dPEG24 Peptide Click here for species-specific activity table Hs Agonist 7.9 pKi 69
⤷ pKi 7.9 (Ki 1.35x10-8 M) [69]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Rn Agonist 7.6 – 8.1 pKi 53-54
⤷ pKi 7.6 – 8.1 (Ki 2.754x10-8 – 7x10-9 M) [53-54]
Gal-B2-C10 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.44x10-8 M) [70]
Gal-B2-C8 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.49x10-8 M) [70]
Gal-B2-C18 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.5x10-8 M) [70]
Gal-B2-C12 Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 70
⤷ pKi 7.8 (Ki 1.61x10-8 M) [70]
galanin(2-11) Peptide Click here for species-specific activity table Hs Agonist 7.8 pKi 44
⤷ pKi 7.8 (Ki 1.66x10-8 M) [44]
Gal-B2-C14 Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 70
⤷ pKi 7.7 (Ki 1.82x10-8 M) [70]
J18 (galanin analogue) Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 45
⤷ pKi 7.7 (Ki 2x10-8 M) [45]
[N-Me,des-Sar]Gal-B2 Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 43
⤷ pKi 7.7 (Ki 2.02x10-8 M) [43]
Gal-B2-MPEG4 Peptide Click here for species-specific activity table Hs Agonist 7.7 pKi 70
⤷ pKi 7.7 (Ki 2.05x10-8 M) [70]
Gal-(K)4 Peptide Click here for species-specific activity table Hs Agonist 7.6 pKi 70
⤷ pKi 7.6 (Ki 2.4x10-8 M) [70]
M1151 Peptide Click here for species-specific activity table Hs Agonist 7.5 pKi 47
⤷ pKi 7.5 (Ki 2.89x10-8 M) [47]
M1160 Peptide Click here for species-specific activity table Hs Agonist 7.5 pKi 46
⤷ pKi 7.5 (Ki 3.33x10-8 M) [46]
M1152 Peptide Click here for species-specific activity table Hs Agonist 7.4 pKi 47
⤷ pKi 7.4 (Ki 3.64x10-8 M) [47]
Gal-B5 Peptide Click here for species-specific activity table Hs Agonist 7.3 pKi 8
⤷ pKi 7.3 (Ki 4.8x10-8 M) [8]
Gal-B2 Peptide Click here for species-specific activity table Hs Agonist 7.3 pKi 8
⤷ pKi 7.3 (Ki 5.15x10-8 M) [8]
Gal-R2-dPEG24 Peptide Hs Agonist 7.2 pKi 69
⤷ pKi 7.2 (Ki 6.04x10-8 M) [69]
galanin(2-11) Peptide Click here for species-specific activity table Rn Agonist 7.1 pKi 32
⤷ pKi 7.1 (Ki 8.8x10-8 M) [32]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Hs Agonist 6.7 pKi 6
⤷ pKi 6.7 (Ki 1.995x10-7 M) [6]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(10-29) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(5-29) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(9-29) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(9-25) (rat/mouse) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(3-30) (human) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
galanin(1-10) Peptide Hs Agonist <6.2 pKi 5
⤷ pKi <6.2 (Ki >7x10-7 M) [5]
GMAP(1-41) {Sp: Pig} Peptide Rn Agonist <6.1 pKi 61
⤷ pKi <6.1 (Ki >8.4x10-7 M) [61]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pKi 6
⤷ pKi <6.0 (Ki >1x10-6 M) [6]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Rn Agonist <6.0 pKi 53-54
⤷ pKi <6.0 (Ki >1x10-6 M) [53-54]
GMAP(44-59) {Sp: Pig} Peptide Rn Agonist <6.0 pKi 62
⤷ pKi <6.0 (Ki >1x10-6 M) [62]
(D-Thr6, D-Trp8,9)galanin(1-15)ol Peptide Click here for species-specific activity table Rn Agonist <5.9 pKi 61
⤷ pKi <5.9 (Ki >1.25x10-6 M) [61]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist 5.5 – 6.0 pKi 42,60,62
⤷ pKi 5.5 – 6.0 (Ki 3.125x10-6 – 1x10-6 M) [42,60,62]
galanin(10-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Agonist <5.7 pKi 42
⤷ pKi <5.7 (Ki >1.86x10-6 M) [42]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Mm Agonist <5.7 pKi 42
⤷ pKi <5.7 (Ki >2.2x10-6 M) [42]
galnon Small molecule or natural product Rn Agonist 4.5 pKi 3,33
⤷ pKi 4.5 (Ki 3.41x10-5 M) [3,33]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 9.1 pEC50 17
⤷ pEC50 9.1 (EC50 7.2x10-10 M) [17]
galanin-like peptide {Sp: Pig} Peptide Click here for species-specific activity table Rn Agonist 8.6 pEC50 41
⤷ pEC50 8.6 (EC50 2.4x10-9 M) [41]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 7.9 – 9.1 pEC50 6,17
⤷ pEC50 7.9 – 9.1 (EC50 1.23x10-8 – 7.1x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 7.3 – 9.4 pEC50 6,17
⤷ pEC50 7.3 – 9.4 (EC50 5.495x10-8 – 4.2x10-10 M) [6,17]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.3 pEC50 41
⤷ pEC50 8.3 (EC50 5.2x10-9 M) [41]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 7.6 – 8.9 pEC50 6,17
⤷ pEC50 7.6 – 8.9 (EC50 2.399x10-8 – 1.17x10-9 M) [6,17]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 8.1 pEC50 6
⤷ pEC50 8.1 (EC50 8.12x10-9 M) [6]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 7.7 pEC50 53
⤷ pEC50 7.7 (EC50 1.8x10-8 M) [53]
galanin(7-29) (pig) Peptide Click here for species-specific activity table Hs Agonist 7.5 pEC50 6
⤷ pEC50 7.5 (EC50 3.467x10-8 M) [6]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 7.2 pEC50 53
⤷ pEC50 7.2 (EC50 6.5x10-8 M) [53]
Qu-SPX Peptide Hs Agonist 7.1 pEC50 30
⤷ pEC50 7.1 (EC50 8.71x10-8 M) [30]
Description: SRE-luc reporter activation in HEK293 Gqi cells expressing hGAL3 receptor.
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 7.0 pEC50 53
⤷ pEC50 7.0 (EC50 9.4x10-8 M) [53]
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Rn Agonist 6.8 pEC50 53
⤷ pEC50 6.8 (EC50 1.5x10-7 M) [53]
spexin-1 {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Agonist 6.8 pEC50 25
⤷ pEC50 6.8 (EC50 1.61x10-7 M) [25]
Description: Determined by measuring SRE-luc activity in HEK293-Gqi cells expressing hGALR2.
galanin(D-Trp2) (pig) Peptide Click here for species-specific activity table Hs Agonist 6.5 pEC50 6
⤷ pEC50 6.5 (EC50 3.388x10-7 M) [6]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pEC50 6
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [6]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Rn Agonist <6.0 pEC50 53
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [53]
galanin(10-29) (pig) Peptide Hs Agonist <6.0 pEC50 17
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [17]
galanin-like peptide {Sp: Pig} Peptide Click here for species-specific activity table Rn Agonist 9.6 pIC50 41
⤷ pIC50 9.6 (IC50 2.4x10-10 M) [41]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 9.5 pIC50 17
⤷ pIC50 9.5 (IC50 3.5x10-10 M) [17]
galanin {Sp: Pig} Peptide Click here for species-specific activity table Rn Full agonist 9.3 – 9.4 pIC50 18,22
⤷ pIC50 9.3 – 9.4 (IC50 4.6x10-10 – 3.7x10-10 M) [18,22]
galanin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 9.3 pIC50 17
⤷ pIC50 9.3 (IC50 5.1x10-10 M) [17]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Rn Full agonist 8.7 – 9.3 pIC50 7,18,41
⤷ pIC50 8.7 – 9.3 (IC50 1.9x10-9 – 4.8x10-10 M) [7,18,41]
galanin {Sp: Human} Peptide Click here for species-specific activity table Rn Full agonist 8.6 – 9.0 pIC50 18,22,31
⤷ pIC50 8.6 – 9.0 (IC50 2.5x10-9 – 1x10-9 M) [18,22,31]
galanin(1-11) Peptide Rn Agonist 8.8 pIC50 31
⤷ pIC50 8.8 (IC50 1.65x10-9 M) [31]
[Sar1, D-Ala12]galanin(1-16) Peptide Rn Agonist 8.8 pIC50 31
⤷ pIC50 8.8 (IC50 1.74x10-9 M) [31]
galanin(2-11) Peptide Click here for species-specific activity table Rn Agonist 8.8 pIC50 31
⤷ pIC50 8.8 (IC50 1.76x10-9 M) [31]
galanin(2-29) (pig) Peptide Click here for species-specific activity table Hs Full agonist 8.7 – 8.7 pIC50 17-18
⤷ pIC50 8.7 – 8.7 (IC50 1.87x10-9 – 1.8x10-9 M) [17-18]
galanin {Sp: Mouse, Rat} Peptide Click here for species-specific activity table Hs Full agonist 7.9 – 9.5 pIC50 6,17
⤷ pIC50 9.5 (IC50 3.4x10-10 M) [17]
pIC50 7.9 – 9.1 (IC50 1.175x10-8 – 7.6x10-10 M) [6,17]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Hs Agonist 8.7 pIC50 17
⤷ pIC50 8.7 (IC50 2.17x10-9 M) [17]
galanin(1-15) Peptide Click here for species-specific activity table Hs Agonist 8.6 pIC50 17
⤷ pIC50 8.6 (IC50 2.47x10-9 M) [17]
galanin(2-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Full agonist 8.5 pIC50 22
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [22]
galanin(1-16) (rat/mouse/pig) Peptide Click here for species-specific activity table Rn Agonist 7.9 – 8.5 pIC50 18,22
⤷ pIC50 7.9 – 8.5 (IC50 1.32x10-8 – 3x10-9 M) [18,22]
galanin(1-15) Peptide Click here for species-specific activity table Rn Agonist 8.1 pIC50 18
⤷ pIC50 8.1 (IC50 7.4x10-9 M) [18]
GALP(3-32) (human) Peptide Click here for species-specific activity table Hs Agonist 7.8 pIC50 27
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [27]
galanin-like peptide {Sp: Human} Peptide Click here for species-specific activity table Hs Agonist 7.6 – 7.7 pIC50 7,27
⤷ pIC50 7.6 – 7.7 (IC50 2.8x10-8 – 1.87x10-8 M) [7,27]
GALP(1-32) (human) Peptide Click here for species-specific activity table Hs Agonist 7.2 pIC50 27
⤷ pIC50 7.2 (IC50 6.9x10-8 M) [27]
galanin(5-29) (pig) Peptide Rn Agonist 6.7 pIC50 65
⤷ pIC50 6.7 (IC50 2x10-7 M) [65]
galanin(3-29) (pig) Peptide Click here for species-specific activity table Hs Agonist <6.0 pIC50 17-18
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [17-18]
galanin(3-29) (rat/mouse) Peptide Click here for species-specific activity table Rn Agonist <6.0 pIC50 22
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [22]
galanin(10-29) (pig) Peptide Click here for species-specific activity table Rn Agonist 6.0 pIC50 18
⤷ pIC50 6.0 (IC50 1x10-6 M) [18]
alarin {Sp: Rat} Peptide Click here for species-specific activity table Rn Agonist <6.0 pIC50 7
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [7]
[125I]spexin-1 Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist - - 25
⤷ [25]
View species-specific agonist tables
Agonist Comments
Binding affinity is lost with removal of amino acids 1 and 2 of galanin [6]. Galanin(D-Trp2) has a higher binding affinity for GAL2 receptor than GAL1 receptor.
In [60], affinities are given for both membrane binding assays and whole cell binding assays. Two populations of binding sites (larger population of low affinity/ smaller population of higher affinity) are identified in [18].

In [8] and [43] many different galanin analogues were trialled. The most active compounds are reported here. The Ki values of other analogues are listed in these publications. In [49] a series of 2,4,6-triaminopyridimines analogs were tested and found to have IC50 values in the range 300-100nM.

NOTE that compounds with -ve log10 affinities <6 have no appreciable agonist function.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
M15 Peptide Am Antagonist 9.0 pKi 6
⤷ pKi 9.0 (Ki 1.07x10-9 M) [6]
C7 Peptide Click here for species-specific activity table Hs Antagonist 8.7 – 9.2 pKi 5-6
⤷ pKi 8.7 – 9.2 (Ki 2x10-9 – 6.3x10-10 M) [5-6]
M15 Peptide Click here for species-specific activity table Mm Antagonist 8.9 pKi 42
⤷ pKi 8.9 (Ki 1.4x10-9 M) [42]
M32 Peptide Click here for species-specific activity table Hs Antagonist 8.7 – 8.8 pKi 6,48
⤷ pKi 8.7 – 8.8 (Ki 2.18x10-9 – 1.45x10-9 M) [6,48]
M35 Peptide Click here for species-specific activity table Hs Antagonist 8.7 – 8.7 pKi 5-6
⤷ pKi 8.7 – 8.7 (Ki 1.95x10-9 – 1.8x10-9 M) [5-6]
M35 Peptide Click here for species-specific activity table Rn Antagonist 8.1 – 9.2 pKi 33,42,53-54,61
⤷ pKi 8.1 – 9.2 (Ki 8.2x10-9 – 6x10-10 M) [33,42,53-54,61]
M40 Peptide Click here for species-specific activity table Hs Antagonist 8.4 – 8.8 pKi 5-6
⤷ pKi 8.4 – 8.8 (Ki 4.07x10-9 – 1.5x10-9 M) [5-6]
M32 Peptide Click here for species-specific activity table Rn Antagonist 7.9 – 9.2 pKi 53-54
⤷ pKi 9.1 – 9.2 (Ki 7.9x10-10 – 6x10-10 M) [53-54]
pKi 7.9 (Ki 1.3x10-8 M) [53]
M40 Peptide Click here for species-specific activity table Mm Antagonist 8.6 pKi 42
⤷ pKi 8.6 (Ki 2.8x10-9 M) [42]
C7 Peptide Click here for species-specific activity table Rn Antagonist 7.7 – 9.3 pKi 42,53-54,61
⤷ pKi 7.7 – 9.3 (Ki 1.9x10-8 – 5.6x10-10 M) [42,53-54,61]
M40 Peptide Click here for species-specific activity table Rn Antagonist 7.7 – 9.1 pKi 33,42,53-54,61-62
⤷ pKi 7.7 – 9.1 (Ki 1.8x10-8 – 7x10-10 M) [33,42,53-54,61-62]
M15 Peptide Click here for species-specific activity table Rn Antagonist 7.8 – 9.0 pKi 33,42,53-54,61-62
⤷ pKi 7.8 – 9.0 (Ki 1.57x10-8 – 1x10-9 M) [33,42,53-54,61-62]
M35 Peptide Mm Antagonist 8.3 pKi 42
⤷ pKi 8.3 (Ki 4.9x10-9 M) [42]
M871 Peptide Click here for species-specific activity table Hs Antagonist 7.9 pKi 55
⤷ pKi 7.9 (Ki 1.31x10-8 M) [55]
C7 Peptide Click here for species-specific activity table Mm Antagonist 7.8 pKi 42
⤷ pKi 7.8 (Ki 1.4x10-8 M) [42]
SNAP 398299 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 58
⤷ pKi <6.0 (Ki >1x10-6 M) [58]
SNAP 37889 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 58
⤷ pKi <5.0 (Ki >1x10-5 M) [58]
GalR3ant Small molecule or natural product Click here for species-specific activity table Rn Antagonist <5.0 pKi 33
⤷ pKi <5.0 (Ki >1x10-5 M) [33]
M15 Peptide Click here for species-specific activity table Hs Antagonist 8.0 – 9.2 pEC50 5-6,17
⤷ pEC50 8.0 – 9.2 (EC50 9.12x10-9 – 6.5x10-10 M) [5-6,17]
C7 Peptide Click here for species-specific activity table Rn Antagonist 8.5 pEC50 53
⤷ pEC50 8.5 (EC50 3x10-9 M) [53]
M35 Peptide Click here for species-specific activity table Hs Antagonist 7.9 – 9.1 pEC50 6,17
⤷ pEC50 7.9 – 9.1 (EC50 1.38x10-8 – 7.2x10-10 M) [6,17]
M32 Peptide Click here for species-specific activity table Hs Antagonist 7.8 – 8.4 pEC50 6,17
⤷ pEC50 7.8 – 8.4 (EC50 1.413x10-8 – 4.23x10-9 M) [6,17]
C7 Peptide Click here for species-specific activity table Hs Antagonist 8.0 pEC50 6
⤷ pEC50 8.0 (EC50 9.33x10-9 M) [6]
M40 Peptide Click here for species-specific activity table Hs Antagonist 7.8 pEC50 6
⤷ pEC50 7.8 (EC50 1.621x10-8 M) [6]
M40 Peptide Click here for species-specific activity table Rn Antagonist 7.6 pEC50 53
⤷ pEC50 7.6 (EC50 2.8x10-8 M) [53]
M35 Peptide Click here for species-specific activity table Rn Antagonist 7.5 pEC50 53
⤷ pEC50 7.5 (EC50 2.9x10-8 M) [53]
M15 Peptide Click here for species-specific activity table Rn Antagonist 6.5 pEC50 53
⤷ pEC50 6.5 (EC50 3x10-7 M) [53]
M35 Peptide Click here for species-specific activity table Rn Antagonist 8.6 – 9.4 pIC50 18,22
⤷ pIC50 8.6 – 9.4 (IC50 2.8x10-9 – 4.3x10-10 M) [18,22]
M40 Peptide Click here for species-specific activity table Rn Antagonist 8.6 – 8.7 pIC50 18,22
⤷ pIC50 8.6 – 8.7 (IC50 2.7x10-9 – 1.9x10-9 M) [18,22]
M15 Peptide Click here for species-specific activity table Hs Antagonist 8.4 pIC50 17
⤷ pIC50 8.4 (IC50 4.02x10-9 M) [17]
C7 Peptide Click here for species-specific activity table Hs Antagonist 8.1 pIC50 17
⤷ pIC50 8.1 (IC50 8.39x10-9 M) [17]
C7 Peptide Click here for species-specific activity table Rn Antagonist 7.6 – 8.4 pIC50 18,22
⤷ pIC50 7.6 – 8.4 (IC50 2.3x10-8 – 3.6x10-9 M) [18,22]
M15 Peptide Click here for species-specific activity table Rn Antagonist 7.6 – 8.3 pIC50 18,22
⤷ pIC50 7.6 – 8.3 (IC50 2.8x10-8 – 4.8x10-9 M) [18,22]
dithiipin-1,1,4,4-tetroxide analogue 7 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <4.5 pIC50 51
⤷ pIC50 <4.5 (IC50 >3x10-5 M) [51]
View species-specific antagonist tables
Antagonist Comments
GalR3ant displays receptor selectivity for GAL3 receptor, with low affinity for GAL1 and GAL2 receptors [33].
In [51], a series of compounds was tested, and the IC50 value for human GAL2 receptor is reported above. Analogue 7 is reported as the first non-peptide sub-micromolar antagonist to human GAL1 receptor.
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CYM2503 Small molecule or natural product Primary target of this compound Rn Positive 9.2 pEC50 34
⤷ pEC50 9.2 (EC50 6.9x10-10 M) [34]
Description: Potentiation of galanin-induced IP1 accumulation in vitro.
Allosteric Modulator Comments
CYM2503, a putative GalR2-positive allosteric modulator, does not by itself stimulate IP1 production in HEK293 stably expressing the rat GAL2 receptor in the absence of galanin. CYM2503 does however potentiate the effect of 100nM galanin (i.e. galanin alone EC50 = 300nM; galanin+CYM2503 EC50 = 690nM) and shifts the galanin concentration-response curve to the left (EC50 shifted by 50.4 fold with 100μM CYM2503; 12.5 fold with 10μM CYM2503 and 0.7 fold with 1μM CYM2503) [34]. The results with CYM2503 suggest that the GAL2 receptor is a plausible target for the development of novel anticonvulsant drug therapy.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Comments:  The most commonly reported pathway involves phospholipase C activation, which increases insoitol phosphate hydrolysis, mediating the release of Ca2+ into the cytoplasm from intracellular stores and opening Ca2+-dependent chloride channels [6,12,17-18,42,53,63]. These GAL2 receptor-mediated intracellular effects are not affected by pertussis toxin, suggesting that GAL2 receptor acts via Gq/G11-type G-proteins (reviewed in [28]).
References:  6,12,17-18,42,53,63
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family
G12/G13 family 		Adenylyl cyclase inhibition
Other - See Comments
Comments:  The ability of GAL2 receptor to signal via other G proteins is somewhat controversial (reviewed in [28]). Several studies demonstrate no alterations in forskolin-stimulated cAMP accumulation following galanin exposure [16,42,53]; whereas several other studies demonstrate at least some inhibition of forskolin-stimulated cAMP accumulation, although less than reported for GAL1 receptor, which is inhibited by pertussis toxin [12,17,61,63]. In addition, GAL2 receptor activation inhibits cyclic-AMP-responsive element-binding protein [1]. There is also evidence that GAL2 receptor is coupled to a Go-type G-protein, which activates mitogen-activated protein kinase (MAPK) in a pertussis toxin-sensitive, PKC (protein kinase C)-dependent fashion [12,20-21]; although it may also proceed via PKC-independent pathways [63]. Another proposed signalling pathway for GAL2 receptor is via functional coupling to a G12/G13 G-protein and activation of RhoA in small cell lung cancer cells [63].

In non-tumour cells, galanin enhances neuronal survival, mediated via the Akt-signalling pathway, leading to suppression of caspase-3 and capase-9 activity, likely via GAL2 receptor stimulation [13,68]; whereas in the tumour cell line (PC12), galanin mediates apoptotic cell death via GAL2 receptor, by inhibition of the PI3K/Akt pathway [59].

GAL2 receptor has been demonstrated to be internalised following incubation with galanin in a GAL2-EGFP (enhanced green fluorescent protein)-transfected PC12 cell line (derived from phaeochromocytoma of rat adrenal medulla) [66-67] (reviewed in [28]).
References:  12,17,61
Tissue Distribution Click here for help
Small intestine and colon. Not detected in whole brain, amygdala, caudate nucleus, corpus callosum, hippocampus, substantia nigra, subthalamic nucleus, thalamus, cerebellum, cerebral cortex, medulla, spinal cord, occipital lobe, frontal lobe, temporal lobe, putamen, heart, placenta, lung, liver, skeletal muscle, kidney, pancreas, spleen, thymus, prostate, testes, ovary, peripheral blood leukocytes.
Species:  Human
Technique:  Northern blot.
References:  5
Brain, lung, heart, spleen, kidney > skeletal muscle, liver, testis.
Species:  Rat
Technique:  Northern blot.
References:  53
High levels in GH3 pituitary cell line, anterior pituitary, whole brain, hypothalamus, gut tissues; lower levels in spleen, lung, skeletal muscle, heart, kidney, liver, testis.
Species:  Rat
Technique:  Ribonuclease protection analysis.
References:  18
About 25% normal dorsal root ganglia in lumbar spine were GAL2 receptor mRNA positive. Strong increase in GAL2 receptor mRNA neuron profiles after peripheral tissue inflammation and long-lasting decrease after axotomy.
Species:  Rat
Technique:  In situ hybridisation.
References:  56
Granule cell layer of dentate gyrus.
Species:  Rat
Technique:  In situ hybridisation.
References:  42
Following facial nerve injury, GAL2 receptor mRNA expression is increased in the ipsilateral facial nucleus (at 3 & 7 days post facial nerve injury).
Species:  Rat
Technique:  In situ hybridisation.
References:  9
Highest levels – hippocampus (including dentate gyus) and hypothalamic nuclei (supraoptic, retrochiasmic, arcuate, lateral mammillary nuclei) > paraventricular nuclei>>anterior hypothalamic area, lateral hypothalamic area, preoptic area). Lower levels – amygdala and piriform cortex. Detected in brain stem, anterodorsal thalamic nucleus, Purkinje cells of cerebellum, anterior pituitary (not posterior pituitary).
Species:  Rat
Technique:  In situ hybridisation.
References:  18
Kidney, testis, skeletal muscle, liver > brain, heart, spleen, lung.
Species:  Rat
Technique:  Northern blot.
References:  61
Uterus, RIN m5F cells (rat insulinoma cell line) > large intestine, stomach > lung, prostate, vas deferens, ovary. Minimal to none in heart, kidney, liver, skeletal muscle, testes, pancreas.
Species:  Rat
Technique:  Northern blot.
References:  22
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of intracellular Ca2+ in rat GAL2 receptor-transfected CHO cells.
Species:  Rat
Tissue:  CHO cells transfected with rat GAL2 receptor.
Response measured:  Increase in intracellular free Ca2+.
References:  53
Rat galanin causes concentration dependent inhibition of forskolin-stimulated cAMP production.
Species:  Rat
Tissue:  COS-1 cells.
Response measured:  Measurement of forskolin-stimulated cAMP production in rat GAL2 receptor transfected COS-1 cells.
References:  61
Measurement of inositol phosphate accumulation in rat GAL2-transfected CHO cells following application of porcine galanin.
Species:  Rat
Tissue:  CHO cells transfected with rat GAL2 receptor.
Response measured:  Inositol phosphate accumulation.
References:  12,53
Measurement of inward currents in Xenopus oocytes injected with rat GAL2 receptor mRNA following application of porcine galanin (100-1000nM).
Species:  Rat
Tissue:  Xenopus oocytes.
Response measured:  Activation of rapid inward currents (most likely mediated by endogenous calcium-activated Cl- currents from the resulting increase in intracellular free Ca2+)
References:  53
Measurement of inositol phosphate levels in rat GAL2 receptor-transfected HEK 293 cells.
Species:  Rat
Tissue:  HEK293 cell line transfected with rat GAL2 receptor.
Response measured:  Stimulation of inositol phosphate accumulation, which isinsensitive to pertussis toxin.
References:  18
Inhibition of forskolin-stimulated cAMP production by 30% (compared to 70% in GAL1 receptor-transfected CHO cells)
Species:  Rat
Tissue:  CHO cells.
Response measured:  Measurement of forskolin-stimulated cAMP production in rat GAL2 receptor-transfected CHO cells.
References:  12
Galanin stimulates MAPK activity, which is inhibited by pretreatment with pertussis toxin and also with the protein kinase C (PKC) inhibitor, bis[indolylmaleimide I] and PKC depletion. Galanin-stimulated MAPK activity is not affected by β-ARKct expression, suggesting that the pathway was not mediated via the βγ subunit of Gi.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Measurement of MAPK (mitogen-activated protein kinase) activity in GAL2 receptor-transfected CHO cells.
References:  12
Human galanin causes a concentration-dependent decrease in forskolin-stimulated intracellular cAMP levels in human GAL2 receptor-transfected HEK293 cells.
Species:  Human
Tissue:  HEK293 cells.
Response measured:  Measurement of forskolin-stimulated intracellular cAMP levels.
References:  17,63
Human galanin caused a concentration-dependent increase in transient intracellular Ca2+ levels in human GAL2 receptor-transfected HEK293 cells.
Species:  Human
Tissue:  HEK293 cells.
Response measured:  Measurement of intracellular Ca2+ levels
References:  17
Galanin stimulates inositol phosphate accumulation in rat GAL2 receptor-transfected COS-7 cells. This response is not affected by pertussis toxin.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Measurement of inositol phosphate levels.
References:  42
Galanin stimulates inositol phosphate accumulation in mouse GAL2 receptor transfected COS-7. This response is not affected by pertussis toxin.
Species:  Mouse
Tissue:  COS-7 cells.
Response measured:  Measurement of inositol phosphate levels.
References:  42
Human galanin (10-1000nM) activates rapid inward currents in Xenopus oocytes injected with human GAL2 receptor mRNA
Species:  Human
Tissue:  Xenopus oocytes.
Response measured:  Measurement of inward currents in Xenopus oocytes.
References:  6
Galanin led to the formation of actin stress fibres in Swiss 3T3 fibroblast cells expressing the human GAL2 receptor, which is likely mediated via G12/G13 protein family.
Species:  Human
Tissue:  Swiss 3T3 fibroblast cell line.
Response measured:  Measurement of Rho-dependent stress fibre formation.
References:  63
Human galanin caused a concentration-dependent increase in intracellular inositol phosphate levels in human GAL2 receptor-transfected HEK293 cells.
Species:  Human
Tissue:  HEK293 cells.
Response measured:  Measurement of inositol phosphate levels.
References:  17
Glutamate increases phosphorylation of Akt in wild-type hippocampal cultures, which is significantly attenuated in GAL2 receptor knockout cultures, suggesting that it is mediated via GAL2 receptor.
Species:  Mouse
Tissue:  Hippocampal tissue.
Response measured:  Measurement of Akt phosphorylation.
References:  15
Galanin down-regulates phosphorylation of Akt and Bad in GAL2 receptor-transfected PC12 cells, suggesting that GAL2 receptor-mediated signalling leads to inhibition of the PI3K/Akt pathway, which in turn leads to caspase-dependent apoptotic cell death.
Species:  Rat
Tissue:  PC12 cell line (derived from phaeochromocytoma of rat adrenal medulla).
Response measured:  Measurement of phosphorylation of Akt and Bad.
References:  59
Galanin (100nM) stimulates increased intracellular Ca2+ in human GAL2 receptor-transfected CHO cells. Galanin also increases Ca2+ release In GAL2 receptor-expressing H69 cells, which is not blocked by pretreatment with pertussis toxin, suggesting it is mediated via a Gq/G11 pathway. Galanin stimulates ERK activity in GAL2 receptor-expressing H69 cells. This ERK stimulation is nearly abolished by pretreatment with staurosporine, indicating participation of serine/threonine kinases e.g. PKC isozymes, although the activation is not altered by pretreatment with the PKC inhibitor, bisindolylmaleimide I (GF10903X), suggesting that galanin-dependent ERK activation can proceed through alternative pathways independent of PKC.
Species:  Human
Tissue:  CHO cells, H69 cells (small cell lung cancer cell line).
Response measured:  Measurement of intracellular Ca2+ and measurement of ERK activation.
References:  6,63
Galanin stimulates inositol phosphate accumulation in human GAL2 receptor-transfected CHO and COS-7 cells. Pertussis toxin does not alter the galanin-induced inositol phosphate accumulation in COS-7 cells.
Species:  Human
Tissue:  CHO cells, COS-7 cells.
Response measured:  Measurement of inositol phosphate levels.
References:  6,63
Galanin(1-29), which is a high affinity agonist for both GAL1 receptor and GAL2 receptor, and galanin (2-11), a GAL2 receptor agonist, significantly reduce CREB phosphorylation induced by high-frequency trans stimulation, suggesting GAL2 receptor may be involved.
Species:  Mouse
Tissue:  Hippocampal tissue.
Response measured:  Measurement of LTP-induced CREB phosphorylation in the dentate gyrus of mice.
References:  1
Galanin demonstrates neuroprotective effects against A-beta (β-amyloid) on basal forebrain neurons, which is replicated by the GAL2 receptor agonist, galanin(2-11) (AR-M1896), suggesting that the effect is mediated via GAL2 receptor. Further studies demonstrate that galanin reverses A-beta-induced inhibition of Akt phosphorylation (a pro-survival pathway), blocks the cleavage of capase-3, and attenuates cleavage of capase-9. It is likely this effect is also mediated via GAL2 receptor.
Species:  Rat
Tissue:  Rat basal forebrain
Response measured:  Measurement of phosphorylation of Akt (serine/threonine kinase), and cleavage of caspase-3 and capase-9 levels in rat basal forebrain neurons.
References:  13
GAL2 receptor is internalised in a dose dependent manner after incubation with galanin in GAL2 receptor-EGFP (enhanced green fluorescent protein)-transfected PC12 cells. In addition, galanin and GALP (which preferentially binds to 2 receptor) increase ERK phosphorylation in PC12 cells, which is inhibited by the protein kinase C (PKC)- specific inhibitor, GF, and pertussis toxin, suggesting that galanin-induced ERK phosphorylation involves activation of Go proteins.
Species:  Rat
Tissue:  PC12 cell line (derived from phaeochromocytoma of rat adrenal medulla).
Response measured:  Measurement of receptor internalisation and ERK phosphorylation.
References:  20,66-67
Galanin rapidly activates ERK1 in wild-type but not GAL2 receptor knockout mice.
Species:  Mouse
Tissue:  Dorsal root ganglion from wildtype and GAL2 receptor knockout mice.
Response measured:  Measurement of ERK phosphorylation.
References:  21
Physiological Functions Click here for help
Galanin analogue J18 (which is selective for Galr2) has antidepressant-like effects in mouse models of depression (forced swin and tail suspension tests) at low dose (<0.5mg/kg). This antidepressant-like effect is abbrogated by galanin antagonist M35.
Species:  Mouse
Tissue:  In vivo.
References:  45
Galanin, acting via GAL2 receptor, induces myometrial contraction.
Species:  Rat
Tissue:  Myometrium.
References:  40
In the Morris water maze, galanin significantly retards spatial acquisition without affecting swim speed or performance in the visible platform test, which appears to be mediated via GAL2 receptor (in areas where most of the galanin is present in noradrenergic terminals).
Species:  Rat
Tissue:  Hippocampal formation.
References:  50
Low dose galanin has a nociceptive role at the spinal cord level mediated by GAL2 receptors†.
Species:  Rat
Tissue:  Spinal cord.
References:  31
Galanin mediates neurite extension in adult sensory neurons (dorsal root ganglion) via GAL2 receptor in a PKC-dependent manner.
Species:  Mouse
Tissue:  Dorsal root ganglion.
References:  37
GAL2 receptor appears to control the excitability and Ca2+ entry in a large population of nociceptive neurons, which would increase excitability and enhance intracellular Ca2+ signalling, which would enhance sensory transmission.
Species:  Rat
Tissue:  Dorsal root ganglion neurons.
References:  24
In the dentate gyrus, galanin acting via GAL2 receptor inhibits seizures, promotes viability of hilar interneurons and stimulates seizure-induced neurogenesis (from studies with a 50% reduction of GAL2 receptor binding, achieved by continuous infusion of complemenatry peptide nucleic acid antisense oligonucleotide into dentate gyrus.
Species:  Rat
Tissue:  In vivo.
References:  39
Peripheral galanin appears to have an excitatory role in inflammatory pain (induced by capsaicin) likely mediated by peripheral GAL2 receptor.
Species:  Rat
Tissue:  In vivo/intraplantar injections of capsaicin.
References:  23
GAL2 receptor agonist blocked induction of LTP in the dentate gyrus, and caused a transient reduction in the maintenance phase of LTP. GAL2 receptor may also be involved in reducing the level of LTP-mediated phosphorylation of CREB in the dentate gyrus granule cells.
Species:  Mouse
Tissue:  In vivo/brain.
References:  1
GAL2 receptor inhibits cell proliferation and mediates apoptosis in SH-SY5Y neuroblastoma cells.
Species:  Human
Tissue:  SH-SY5Y neuroblastoma cells.
References:  4
Physiological Functions Comments
† Note that in this study [31], the effects were investigated using the GAL2 receptor agonist, AR-M1896, which has subsequently been demonstrated to bind with high affinity to GAL3 receptor. This suggests that the effects may also be mediated via GAL3 receptor.
Physiological Consequences of Altering Gene Expression Click here for help
Mice with GAL2 receptor knockout (C57BL/6 background) were tested in a variety of anxiety- and depressive-like tests. Mice with GAL2 receptor knockout exhibited a more persistent depressive-like phenotype in the learned helplessness paradigm and increased immobility in the tail suspension test; but showed similar levels of anxiety-like behaviour compared to wildtype in the elevated plus maze, open field and light-dark transfer test.
Species:  Mouse
Tissue:  In vivo/brain.
Technique:  Gene knock-outs.
References:  35
GAL2 receptor knockout mice do not exhibit antidepressant-like effects of GAL2 receptor analogue J18 observed in receptor intact mice.
Species:  Mouse
Tissue:  In vivo
Technique:  Gene knockouts.
References:  45
GAL2 receptor knockout mice were tested for basic motor and sensory function, feeding behaviour, reproduction, mood, learning and memory, and seizure susceptibility. GAL2 receptor knockout mice were indistinguishable from wildtype mice in these tests.
Species:  Mouse
Tissue:  Brain.
Technique:  Gene knock-outs.
References:  19
GAL2 receptor knockout mice demonstrated a 15% decrease in CGRP expressing neuronal profiles in the adult dorsal root ganglia, associated with marked deficits in neuropathic and inflammatory pain behaviours. They also demonstrated one third reduction in neurite outgrowth from cultured dorsal root ganglion neurons.
Species:  Mouse
Tissue:  Dorsal root ganglion.
Technique:  Gene knock-outs.
References:  21
Mice with GAL2 receptor knockout (129AS1/SvlmJ line) were tested in tests of general health, cognitive behaviour and anxiety-like behaviour. Mice with GAL2 receptor knockout demonstrated an anxiogenic-like phenotype on the elevated plus maze, but not in several other measures of anxeity-like behaviour. In addition, there was no siginificant differences from wildtype in terms of gnereal health or cognitive behaviour (Morris water maze, trace cued and contextual fear conditioning).
Species:  Mouse
Tissue:  In vivo.
Technique:  Gene knock-outs.
References:  2
GAL2 receptor knockout mice were tested for hippocampal neuronal survival following glutamate-induced hippocampal damage. The protective role played by galanin for glutamate-induced hippocampal damage is abolished in GAL2 receptor knockout mice.
Species:  Mouse
Tissue:  Hippocampal culture.
Technique:  Gene knock-outs.
References:  15
The role of GAL2 receptor in status epilepticus was investigated by intrahippocampal infusion of anti-GAL2 receptor peptide-nucleic acid antisense. Focal downregulation of GAL2 receptor in the hippocampus significantly increased the severity of perforant path stimulation-induced status epilepticus and led to milder injury to hilar interneurons and potentiated seizure-induced hippocampal damage.
Species:  Rat
Tissue:  Hippocampus.
Technique:  Peptide nucleic acid antisense methodology.
References:  38
Mice with GAL2 receptor knockout were tested for pain thresholds, and development and trophic effects of galanin. After 1 week post sciatic nerve transection, there were 16-20% fewer neurons in intact contralateral dorsal root ganglia of GAL2 receptor knockout mice. Compared to wildtype mice, GAL2 receptor knockout mice showed similar onset and duration of hyperalgia in the injured paw, and similar recovery from spinal nerve ligation-cause allodynia.
Species:  Mouse
Tissue:  In vivo/sciatic nerve/dorsal root ganglion.
Technique:  Gene knock-outs.
References:  52
Mice with GAL2 receptor knockout were tested for disease severity in the experimental autoimmune encephalitis (EAE) model of multiple sclerosis. GAL2 receptor knockout increases disease severity in this mouse model.
Species:  Mouse
Tissue:  In vivo.
Technique:  Gene knock-outs.
References:  64
Mice with GAL2 receptor knockout were tested for amyloid induced cell death. Mice with GAL2 receptor knockout demonstrated significantly greater cell death following amyloid than wildtype controls.
Species:  None
Tissue:  In vivo.
Technique:  Gene knock-outs.
References:  14
GAL2 receptor-overexpressing mice were assessed in various tests of anxiety- and depressive-like behaviour, including the Porsolt forced swim test, the open field, elevated plus maze, passive avoidance test. GAL2 receptor-overexpressing mice demonstrated decreased immobility in the forced swim test (indicative of antidepressive-like behaviour and/or increased stress resistance), but no difference in anxiety-like behaviour, motor activity levels, emotional learning or memory behaviours.
Species:  Mouse
Tissue:  In vivo.
Technique:  Gene over-expression.
References:  29
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Galr2tm1Dgen Galr2tm1Dgen/Galr2tm1Dgen
B6.129-Galr2		 MGI:1337018  MP:0001022 abnormal L5 dorsal root ganglion morphology PMID: 16487144 
Galr2Gt(OST105469)Lex Galr2Gt(OST105469)Lex/Galr2Gt(OST105469)Lex
involves: 129S5/SvEvBrd * C57BL/6J		 MGI:1337018  MP:0005017 decreased B cell number
Galr2Gt(OST105469)Lex Galr2Gt(OST105469)Lex/Galr2Gt(OST105469)Lex
involves: 129S5/SvEvBrd * C57BL/6J		 MGI:1337018  MP:0002757 decreased vertical activity
Galr2Gt(OST105469)Lex Galr2Gt(OST105469)Lex/Galr2Gt(OST105469)Lex
involves: 129S5/SvEvBrd * C57BL/6J		 MGI:1337018  MP:0005015 increased T cell number
Galr2tm1Dgen Galr2tm1Dgen/Galr2tm1Dgen
B6.129-Galr2		 MGI:1337018  MP:0001973 increased thermal nociceptive threshold PMID: 16487144 
Gene Expression and Pathophysiology Comments
GAL2 receptor is a candidate biomarker for colon cancer, with GAL2 receptor hypermethylation showing a sensitvity of 85% and specificity of 95% [10].
Biologically Significant Variant Comments
Linkage and mapping studies suggest that the 17q chromosomal region contains a gene (or genes) that contributes to the genetic aetiology of obesity (particularly visceral adiposity). One candidate gene in this region is the GAL2 receptor, although there is little evidence of an association between polymorphisms of GAL2 receptor and obesity [57].

References

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