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B1 receptor

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Target id: 41

Nomenclature: B1 receptor

Family: Bradykinin 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 7 353 14q32.2 BDKRB1 bradykinin receptor B1 16
Mouse 7 334 12 E Bdkrb1 bradykinin receptor, beta 1 69
Rat 7 337 6q32 Bdkrb1 bradykinin receptor B1 62
Previous and Unofficial Names Click here for help
B1BKR | BKR1 | B1R | kinin B1 receptor | bradykinin receptor | bradykinin receptor, B1
Database Links Click here for help
Specialist databases
GPCRdb bkrb1_human (Hs), bkrb1_mouse (Mm), bkrb1_rat (Rn)
Other databases
Alphafold P46663 (Hs), Q61125 (Mm), P97583 (Rn)
ChEMBL Target CHEMBL4308 (Hs), CHEMBL1250407 (Mm), CHEMBL4613 (Rn)
Ensembl Gene ENSG00000100739 (Hs), ENSMUSG00000041347 (Mm), ENSRNOG00000004488 (Rn)
Entrez Gene 623 (Hs), 12061 (Mm), 81509 (Rn)
Human Protein Atlas ENSG00000100739 (Hs)
KEGG Gene hsa:623 (Hs), mmu:12061 (Mm), rno:81509 (Rn)
OMIM 600337 (Hs)
Pharos P46663 (Hs)
RefSeq Nucleotide NM_000710 (Hs), NM_007539 (Mm), NM_030851 (Rn)
RefSeq Protein NP_000701 (Hs), NP_031565 (Mm), NP_110478 (Rn)
UniProtKB P46663 (Hs), Q61125 (Mm), P97583 (Rn)
Wikipedia BDKRB1 (Hs)
Natural/Endogenous Ligands Click here for help
bradykinin {Sp: Human, Mouse, Rat}
[des-Arg9]bradykinin {Sp: Human, Mouse, Rat}
[des-Arg10]kallidin {Sp: Human}
[Hyp3]bradykinin {Sp: Human}
kallidin {Sp: Human}
Lys-[Hyp3]-bradykinin {Sp: Human}
T-kinin {Sp: Human, Rat}
Comments: [Des-Arg10]kallidin is the most potent endogenous ligand in human
Potency order of endogenous ligands (Human)
[des-Arg10]kallidin (KNG1, P01042) > [des-Arg9]bradykinin (KNG1, P01042) = kallidin (KNG1, P01042) > bradykinin (KNG1, P01042)

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[des-Arg10]kallidin {Sp: Human} Peptide Ligand is endogenous in the given species Hs Full agonist 9.6 – 10.0 pKi 6,9,37,48
⤷ pKi 9.6 – 10.0 [6,9,37,48]
D-Lys0-[des-Arg10]kallidin Peptide Hs Full agonist 9.5 pKi 6
⤷ pKi 9.5 [6]
[des-Arg9]bradykinin {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 9.2 pKi 45
⤷ pKi 9.2 [45]
[des-Arg10]kallidin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 8.8 pKi 45
⤷ pKi 8.8 [45]
[des-Arg10]kallidin {Sp: Human} Peptide Ligand is endogenous in the given species Rn Full agonist 8.7 – 8.9 pKi 48
⤷ pKi 8.7 – 8.9 [48]
kallidin {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 7.0 – 8.9 pKi 6,9,48
⤷ pKi 7.0 – 8.9 [6,9,48]
[D-Lys1,des-Arg10]kallidin Peptide Hs Full agonist 7.4 – 7.6 pKi 6
⤷ pKi 7.4 – 7.6 [6]
[des-Arg11]T-kinin Peptide Rn Full agonist 7.2 – 7.5 pKi 48
⤷ pKi 7.2 – 7.5 [48]
[Sar,D-Phe8,des-Arg9]bradykinin Peptide Rn Full agonist 7.1 – 7.4 pKi 48
⤷ pKi 7.1 – 7.4 [48]
Lys-kallidin Peptide Hs Full agonist 6.7 – 6.9 pKi 6
⤷ pKi 6.7 – 6.9 [6]
bradykinin {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 6.7 pKi 45
⤷ pKi 6.7 [45]
kallidin {Sp: Human} Peptide Rn Full agonist 6.5 – 6.6 pKi 48
⤷ pKi 6.5 – 6.6 [48]
kallidin {Sp: Human} Peptide Click here for species-specific activity table Mm Full agonist 6.3 pKi 44-45
⤷ pKi 6.3 [44-45]
[des-Phe9,des-Arg10]kallidin Peptide Hs Full agonist 6.1 – 6.2 pKi 6
⤷ pKi 6.1 – 6.2 [6]
[des-Pro8,des-Phe9,des-Arg10]kallidin Peptide Hs Full agonist 5.8 – 5.9 pKi 6
⤷ pKi 5.8 – 5.9 [6]
[des-Arg11]T-kinin Peptide Hs Full agonist 5.7 – 5.9 pKi 48
⤷ pKi 5.7 – 5.9 [48]
[des-Arg9]bradykinin {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 5.7 – 5.8 pKi 9,48
⤷ pKi 5.7 – 5.8 [9,48]
[Sar,D-Phe8,des-Arg9]bradykinin Peptide Hs Full agonist 5.7 pKi 5,48
⤷ pKi 5.7 (Ki 1.99x10-6 M) [5,48]
T-kinin {Sp: Human, Rat} Peptide Ligand is endogenous in the given species Hs Full agonist 5.2 pKi 48
⤷ pKi 5.2 [48]
bradykinin {Sp: Human, Mouse, Rat} Peptide Ligand is endogenous in the given species Rn Full agonist 5.1 – 5.3 pKi 48
⤷ pKi 5.1 – 5.3 [48]
T-kinin {Sp: Human, Rat} Peptide Ligand is endogenous in the given species Rn Full agonist 5.0 – 5.2 pKi 48
⤷ pKi 5.0 – 5.2 [48]
bradykinin {Sp: Human, Mouse, Rat} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 4.0 pKi 6
⤷ pKi 4.0 [6]
[Leu8,des-Arg9]bradykinin Peptide Mm Partial agonist 7.3 pEC50 55
⤷ pEC50 7.3 [55]
NG29 Peptide Hs Full agonist 9.5 pIC50 75
⤷ pIC50 9.5 (IC50 3.16x10-10 M) [75]
Met-Lys-bradykinin Peptide Click here for species-specific activity table Hs Full agonist 7.1 pIC50 58
⤷ pIC50 7.1 [58]
View species-specific agonist tables
Agonist Comments
The presence of arginine carboxypeptidases in functional systems frequently distorts the potency estimates for BK or Lys-BK on the B1 receptor, as these ligands are transformed into their respectice des-Arg9 metabolites [56].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
B-9858 Peptide Hs Antagonist 9.2 pA2 72
⤷ pA2 9.2 [72]
R-954 Peptide Hs Antagonist 8.6 pA2 38
⤷ pA2 8.6 [38]
R-715 Peptide Hs Antagonist 8.5 pA2 36
⤷ pA2 8.5 [36]
B-9430 Peptide Click here for species-specific activity table Hs Antagonist 7.7 pA2 72
⤷ pA2 7.7 [72]
[des-Arg10]icatibant Peptide Mm Antagonist 7.2 pA2 72
⤷ pA2 7.2 [72]
[Leu9,des-Arg10]kallidin Peptide Mm Antagonist 7.0 pA2 1
⤷ pA2 7.0 [1]
R-715 Peptide Mm Antagonist 7.0 pA2 1
⤷ pA2 7.0 [1]
[Leu8,des-Arg9]bradykinin Peptide Mm Antagonist 6.9 pA2 1
⤷ pA2 6.9 [1]
B-9430 Peptide Click here for species-specific activity table Mm Antagonist 6.1 pA2 72
⤷ pA2 6.1 [72]
compound 11 [PMID: 12812482] Small molecule or natural product Hs Antagonist 10.5 pKi 78
⤷ pKi 10.5 [78]
NPC 18565 Peptide Click here for species-specific activity table Hs Antagonist 10.2 pKi 53
⤷ pKi 10.2 [53]
B-9958 Peptide Hs Antagonist 9.2 – 10.3 pKi 35,72
⤷ pKi 9.2 – 10.3 (Ki 6.3x10-10 – 5.1x10-11 M) [35,72]
B-9858 Peptide Hs Antagonist 8.7 – 10.4 pKi 48,53,55
⤷ pKi 8.7 – 10.4 [48,53,55]
B-10356 Peptide Hs Antagonist 8.8 – 10.2 pKi 35
⤷ pKi 8.8 – 10.2 [35]
[Leu9,des-Arg10]kallidin Peptide Hs Antagonist 9.1 – 9.3 pKi 6,9
⤷ pKi 9.1 – 9.3 [6,9]
R-715 Peptide Hs Antagonist 9.2 pKi 55
⤷ pKi 9.2 (Ki 6.3x10-10 M) [55]
compound 12 [PMID: 12723943] Small molecule or natural product Hs Antagonist 9.2 pKi 84
⤷ pKi 9.2 [84]
SSR240612 Small molecule or natural product Hs Antagonist 9.1 – 9.2 pKi 39
⤷ pKi 9.1 – 9.2 [39]
compound 12 [PMID: 12723943] Small molecule or natural product Rn Antagonist 9.0 pKi 84
⤷ pKi 9.0 [84]
B-9858 Peptide Rn Antagonist 8.4 – 8.7 pKi 48
⤷ pKi 8.4 – 8.7 [48]
[Leu8,des-Arg9]bradykinin Peptide Mm Antagonist 8.4 pKi 45
⤷ pKi 8.4 [45]
B-9858 Peptide Mm Antagonist 8.3 pKi 55
⤷ pKi 8.3 [55]
PS020990 Small molecule or natural product Hs Antagonist 8.2 pKi 47
⤷ pKi 8.2 [47]
[Leu9,des-Arg10]kallidin Peptide Mm Antagonist 8.1 pKi 45
⤷ pKi 8.1 [45]
NVP-SAA164 Small molecule or natural product Hs Antagonist 7.9 – 8.1 pKi 30,74
⤷ pKi 7.9 – 8.1 [30,74]
B-9430 Peptide Click here for species-specific activity table Hs Antagonist 7.9 pKi 55,77
⤷ pKi 7.9 [55,77]
[des-Arg10]icatibant Peptide Mm Antagonist 7.6 pKi 45
⤷ pKi 7.6 [45]
[Leu8,des-Arg9]bradykinin Peptide Rn Antagonist 7.4 – 7.7 pKi 48
⤷ pKi 7.4 – 7.7 [48]
[des-Arg10]icatibant Peptide Hs Antagonist 6.6 – 8.4 pKi 9,48
⤷ pKi 6.6 – 8.4 [9,48]
[des-Arg10]icatibant Peptide Rn Antagonist 7.4 – 7.6 pKi 48
⤷ pKi 7.4 – 7.6 [48]
R-715 Peptide Mm Antagonist 7.4 pKi 55
⤷ pKi 7.4 [55]
compound 11 [PMID: 12812482] Small molecule or natural product Rn Antagonist 7.2 pKi 78
⤷ pKi 7.2 [78]
JMV1431 Peptide Click here for species-specific activity table Hs Antagonist 7.1 pKi 2
⤷ pKi 7.1 [2]
NPC 17731 Peptide Click here for species-specific activity table Hs Antagonist 6.9 pKi 53
⤷ pKi 6.9 [53]
icatibant Peptide Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.4 – 7.0 pKi 9,48
⤷ pKi 6.4 – 7.0 [9,48]
B-9430 Peptide Click here for species-specific activity table Mm Antagonist 6.6 pKi 55
⤷ pKi 6.6 [55]
[Leu8,des-Arg9]bradykinin Peptide Hs Antagonist 5.8 – 7.2 pKi 3,6,9,48,58
⤷ pKi 5.8 – 7.2 [3,6,9,48,58]
icatibant Peptide Approved drug Click here for species-specific activity table Immunopharmacology Ligand Rn Antagonist 6.1 – 6.4 pKi 48
⤷ pKi 6.1 – 6.4 [48]
Ac-Lys-[MeAla6,Leu8,des-Arg9]bradykinin Peptide Hs Antagonist 6.2 pKi 55
⤷ pKi 6.2 [55]
[Leu9,des-Arg10]kallidin Peptide Hs Antagonist 8.9 pIC50 58
⤷ pIC50 8.9 [58]
chroman 28 Small molecule or natural product Hs Antagonist 8.5 pIC50 20
⤷ pIC50 8.5 [20]
chroman 28 Small molecule or natural product Rn Antagonist 8.3 – 8.5 pIC50 20
⤷ pIC50 8.3 – 8.5 [20]
View species-specific antagonist tables
Antagonist Comments
B-9958 is an aminopeptidase N substrate [35]. B-10356 is an aminopeptidase N inhibitor [35].
The classical antagonists, [Leu8,des-Arg9]bradykinin and [Leu9,des-Arg10]kallidin, act as partial agonists at the mouse B1 receptors [1,55]. Moreover, the B1 receptor antagonist [Leu8, des-Arg9]bradykinin behaves as partial agonist on the cloned dog B1 receptor [46] and caused a transient fall in blood pressure in anaesthetized dogs [61].
Immunopharmacology Comments
Bradykinin is a vasoactive, pain inducing and pro-inflammatory kinin released during acute inflammation, and its receptors, B1 and B2, are expressed on eosinophils, and neutrophils.
Cell Type Associations
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   eosinophil (CL:0000771)
neutrophil (CL:0000775)
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Chemotaxis & migration
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family
Gq/G11 family 		Adenylyl cyclase inhibition
Phospholipase C stimulation
References:  6
Tissue Distribution Click here for help
Human brain glioblastoma.
Species:  Human
Technique:  Immunohistochemistry.
References:  63
Human brain endothelial cells during inflammatory response. Signalling via theB1 receptor can regulate blood-brain barrier permeability and chemokine production.
Species:  Human
Technique:  RT-PCR, Western blot.
References:  70
Human colon.
Species:  Human
Technique:  Pharmacological bioassay.
References:  19
Prostatic intraepithelial neoplasia and malignant lesions.
Species:  Human
Technique:  Immunohistochemistry.
References:  81
T lymphocytes.
Species:  Human
Technique:  RT-PCR, Western blot.
References:  71
Gastric mucosa.
Species:  Human
Technique:  Immunohistochemistry.
References:  12
Lung fibroblasts.
Species:  Human
Technique:  Immunohistochemistry.
References:  73
Macrophages and CD4+ T cells: B1 receptor is upregulated on these cells in the pancreas of type 1 diabetic rats. B1R blockade exerts anti-diabetic action by preventing the infiltration of these immune cells in the pancreas and by preserving the integrity of Langerhans islets β-cells.
Species:  Rat
Technique:  Macrophages, CD4+ T lymphocytes
References:  82
Dorsal root ganglion primary afferent terminations.
Species:  Rat
Technique:  Immunohistochemistry.
References:  31
Laminae 1 and 2 of the dorsal horn of the spinal cord, peripheral nerve terminals in the bladder, dorsal root ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  85
Thalamus and hypothalamus > cortical regions and hippocampus.
Species:  Rat
Technique:  Autoradiography and in situ hybridization.
References:  13
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 human monocyte-derived dendritic cells endogenously expressing the B1 receptor.
Species:  Human
Tissue:  Monocyte-derived dendritic cells.
Response measured:  Increase in intracellular Ca2+.
References:  10
Measurement of intracellular Ca2+ in rat mesangial cells endogenously expressing the B1 receptor.
Species:  Rat
Tissue:  Mesangial cells.
Response measured:  Elevation of intracellular Ca2+.
References:  8
Measurement of phosphorylation of MAP kinase in rat vascular smooth muscle cells endogenously expressing the B1 receptor.
Species:  Rat
Tissue:  Vascular smooth muscle cells.
Response measured:  Phosphorylation of MAP kinase.
References:  17
Cigarette smoke-induced B1 receptor promotes NADPH oxidase activity in cultured human alveolar epithelial cells.
Species:  Human
Tissue:  Human alveolar epithelial A549 cells.
Response measured:  Increase of superoxide anion.
References:  80
Measurement of contractile responses in human umbilical veins endogenously expressing the B1R.
Species:  Human
Tissue:  Isolated umbilical veins.
Response measured:  Contraction.
References:  37,72
Physiological Functions Click here for help
Inhibition of arterial smooth muscle cell migration.
Species:  Human
Tissue:  Arterial smooth muscle.
References:  60
Activation of neutrophil recruitment.
Species:  Human
Tissue:  Neutrophils isolated from peripheral blood.
References:  26
Modulation of blood pressure.
Species:  Rat
Tissue:  In vivo.
References:  25
Modulation of hyperalgesia.
Species:  Rat
Tissue:  In vivo.
References:  31
Mediation of acute nociception.
Species:  Rat
Tissue:  In vivo.
References:  18
B1 blocking inhibits plasma extravasation in streptozotocin-induced diabetic rats.
Species:  Rat
Tissue:  In vivo.
References:  52
Modulation of vascular permeability of the skin and retina of type 1 diabetic rats.
Species:  Rat
Tissue:  In vivo.
References:  51
Modulation of antigen-induced pulmonary inflammation in mice.
Species:  Mouse
Tissue:  In vivo.
References:  28
B1 receptor blockade causes antinociception in induced hyperalgesia.
Species:  Rat
Tissue:  In vivo.
References:  66
Prevention of the insulitis and renal damage in a model of insulin-dependent diabetes.
Species:  Rat
Tissue:  In vivo.
References:  86
Control of inflammatory pain conditions.
Species:  Mouse
Tissue:  In vivo.
References:  30
Colocalisation and functional interaction between B1 receptor and inducible nitric oxide synthase (iNOS) in rat diabetic retina.
Species:  Rat
Tissue:  Retina
References:  65
Close interaction and reciprocal regulatory mechanism between B1R and TRPV1 on astrocytes and nociceptors in rat neuropathic pain.
Species:  Rat
Tissue: 
References:  15
B1R is co-localized with NADPH oxidase (NOX1 and NOX2) on endothelial and vascular smooth muscle cells and macrophages in rat diabetic blood vessels and B1R stimulation increases superoxide anion production.
Species:  Rat
Tissue:  Endothelial cells, vascular smooth muscle cells, macrophages.
References:  43
B1 receptor was found on astrocytes in a mouse brain tumour, and uncontrolled tumour growth occurs in B1 receptor knockout mice or SSR240612-treated mice, which was blunted by B2 receptor blockade or deletion.
Species:  Mouse
Tissue:  Tumour-derived astrocytes.
References:  63
B1 receptor antagonism abrogates amyloidosis, cerebrovascular and memory deficits in a mouse model of Alzheimer's disease.
Species:  Mouse
Tissue:  In vivo
References:  49
B1 receptor blockade is of therapeutic value in models of type 2 diabetes, obesity and insulin resistance (mouse and rat).
Species:  Mouse
Tissue:  In vivo
References:  22-24,27,79
B1R is expressed in platelets and plays a primary role in inflammation, organ damage, and lethal thrombosis in a rat model of septic shock in diabetes.
Species:  Rat
Tissue: 
References:  83
Upregulation of B1R in endothelial and glial cells in rat diabetic retina and a rat model of age-related macular degeneration. Therapeutic value of eye-drop application of a B1R antagonist in both ocular diseases.
Species:  Rat
Tissue: 
References:  40-42
Attenuation of cardiac remodeling.
Species:  Rat
Tissue:  In vivo.
References:  59
Activation of B1 receptors in the kindled rat hippocampus results in increase extracellular glutamate levels.
Species:  Rat
Tissue:  Kindled hippocampus.
References:  57
Physiological Consequences of Altering Gene Expression Click here for help
B1 receptor knockout mice display hypoalgesia and altered inflammatory responses when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  68
Diabetic hyperalgesia is absent in streptozotocin-induced type 1 diabetic B1 receptor knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  32-34
B1 knockout mice display reduced pancreatic vascular permeability when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  4
B1 knockout mice display reduced nerve injury-induced neuropathic pain when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  29
Mice lacking both the B1 and B2 receptor are normotensive and protected from endotoxin- induced hypotension when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  14
B1 receptor knockout mice display worsened myocardial ischemia when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  50
B1 knockout mice display altered inflammatory responses following intestinal ischemia and reperfusion injury, when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  76
Mice lacking both the B1 and B2 receptor are normotensive and protected from endotoxin- induced hypotension when compared to the wild type.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells
References:  14
B1 knockout mice display lower fasting plasma glucose concentrations but exhibit higher glycemia after feeding when compared to wild-type mice. B1 knockout mice also present pancreas abnormalities, which lead to hypoinsulinemia and reduced insulin release after a glucose load.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  4
Xenobiotics Influencing Gene Expression Click here for help
B1 receptor expression is induced by cigarette-smoke in rat airways.
Species:  Rat
Tissue:  Lung slices.
Technique:  Western blot
References:  54
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
Bdkrb1tm1Bdr Bdkrb1tm1Bdr/Bdkrb1tm1Bdr
involves: 129P2/OlaHsd		 MGI:88144  MP:0002498 abnormal acute inflammation PMID: 10859349 
Bdkrb2/Bdkrb1tm1Mki Bdkrb2/Bdkrb1tm1Mki/Bdkrb2/Bdkrb1tm1Mki
involves: C57BL/6J		 MGI:88144  MP:0002135 abnormal kidney morphology PMID: 17452647 
Bdkrb1tm1Bdr Bdkrb1tm1Bdr/Bdkrb1tm1Bdr
involves: 129P2/OlaHsd		 MGI:88144  MP:0002734 abnormal mechanical nociception PMID: 10859349 
Bdkrb2/Bdkrb1tm1Mki Bdkrb2/Bdkrb1tm1Mki/Bdkrb2/Bdkrb1tm1Mki
involves: C57BL/6J		 MGI:88144  MP:0004756 abnormal proximal convoluted tubule morphology PMID: 17452647 
Bdkrb1tm1Bdr Bdkrb1tm1Bdr/Bdkrb1tm1Bdr
involves: 129P2/OlaHsd		 MGI:88144  MP:0002733 abnormal thermal nociception PMID: 10859349 
Bdkrb2/Bdkrb1tm1Mki Bdkrb2/Bdkrb1tm1Mki/Bdkrb2/Bdkrb1tm1Mki
involves: C57BL/6J		 MGI:88144  MP:0005566 decreased blood urea nitrogen level PMID: 17452647 
Bdkrb1tm1Bdr Bdkrb1tm1Bdr/Bdkrb1tm1Bdr
involves: 129P2/OlaHsd		 MGI:88144  MP:0001982 decreased chemically-elicited antinociception PMID: 10859349 
Bdkrb1tm2Bdr|Bdkrb2tm1Jfh Bdkrb1tm2Bdr/Bdkrb1tm2Bdr,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S7/SvEvBrd * C57BL/6		 MGI:102845  MGI:88144  MP:0005333 decreased heart rate PMID: 16497152 
Bdkrb1tm2Bdr|Bdkrb2tm1Jfh Bdkrb1tm2Bdr/Bdkrb1tm2Bdr,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S7/SvEvBrd * C57BL/6		 MGI:102845  MGI:88144  MP:0008874 decreased physiological sensitivity to xenobiotic PMID: 16497152 
Bdkrb1tm1Bdr Bdkrb1tm1Bdr/Bdkrb1tm1Bdr
involves: 129P2/OlaHsd		 MGI:88144  MP:0008734 decreased susceptibility to endotoxin shock PMID: 16497152 
Bdkrb1tm2Bdr|Bdkrb2tm1Jfh Bdkrb1tm2Bdr/Bdkrb1tm2Bdr,Bdkrb2tm1Jfh/Bdkrb2tm1Jfh
involves: 129S7/SvEvBrd * C57BL/6		 MGI:102845  MGI:88144  MP:0008734 decreased susceptibility to endotoxin shock PMID: 16497152 
Bdkrb1tm1Bdr Bdkrb1tm1Bdr/Bdkrb1tm1Bdr
involves: 129P2/OlaHsd		 MGI:88144  MP:0003043 hypoalgesia PMID: 10859349 
Bdkrb2/Bdkrb1tm1Mki Bdkrb2/Bdkrb1tm1Mki/Bdkrb2/Bdkrb1tm1Mki
involves: C57BL/6J		 MGI:88144  MP:0005565 increased blood urea nitrogen level PMID: 17452647 
Bdkrb2/Bdkrb1tm1Mki Bdkrb2/Bdkrb1tm1Mki/Bdkrb2/Bdkrb1tm1Mki
involves: C57BL/6J		 MGI:88144  MP:0005553 increased circulating creatinine level PMID: 17452647 
Bdkrb2/Bdkrb1tm1Mki Bdkrb2/Bdkrb1tm1Mki/Bdkrb2/Bdkrb1tm1Mki
involves: C57BL/6J		 MGI:88144  MP:0009763 increased sensitivity to induced morbidity/mortality PMID: 17452647 
Bdkrb1tm1Dgen Bdkrb1tm1Dgen/Bdkrb1tm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:88144  MP:0002169 no abnormal phenotype detected
Bdkrb1tm1(BDKRB1)Jfh Bdkrb1tm1(BDKRB1)Jfh/Bdkrb1tm1(BDKRB1)Jfh
involves: 129 * C57BL/6		 MGI:88144  MP:0002169 no abnormal phenotype detected PMID: 16497152 
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The B1 receptor polymorphism -699 G/C has been associated with renal disease.
References:  7
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The -699 G/C polymorphism has been found to be a predictor of cardiovascular risk in hypertension.
References:  21
General Comments
B1 and B2 receptors are overexpressed in the hippocampus of humans with temporal lobe epilepsy [67]. B1 receptor is overexpressed in the retina of humans affected with the wet form of age-related macular degeneration [64], and in the retina of diabetic patients [11].

References

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74. Ritchie TJ, Dziadulewicz EK, Culshaw AJ, Müller W, Burgess GM, Bloomfield GC, Drake GS, Dunstan AR, Beattie D, Hughes GA et al.. (2004) Potent and orally bioavailable non-peptide antagonists at the human bradykinin B(1) receptor based on a 2-alkylamino-5-sulfamoylbenzamide core. J Med Chem, 47 (19): 4642-4. [PMID:15341478]

75. Savard M, Côté J, Tremblay L, Neugebauer W, Regoli D, Gariépy S, Hébert N, Gobeil Jr F. (2016) Safety and pharmacokinetics of a kinin B1 receptor peptide agonist produced with different counter-ions. Biol Chem, 397 (4): 365-72. [PMID:26565554]

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79. Talbot S, Dias JP, El Midaoui A, Couture R. (2016) Beneficial effects of kinin B1 receptor antagonism on plasma fatty acid alterations and obesity in Zucker diabetic fatty rats. Can J Physiol Pharmacol, 94 (7): 752-7. [PMID:27172260]

80. Talbot S, Lin JC, Lahjouji K, Roy JP, Sénécal J, Morin A, Couture R. (2011) Cigarette smoke-induced kinin B1 receptor promotes NADPH oxidase activity in cultured human alveolar epithelial cells. Peptides, 32 (7): 1447-56. [PMID:21600945]

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82. Tidjane N, Gaboury L, Couture R. (2016) Cellular localisation of the kinin B1R in the pancreas of streptozotocin-treated rat and the anti-diabetic effect of the antagonist SSR240612. Biol Chem, 397 (4): 323-36. [PMID:26841446]

83. Tidjane N, Hachem A, Zaid Y, Merhi Y, Gaboury L, Girolami JP, Couture R. (2015) A primary role for kinin B1 receptor in inflammation, organ damage, and lethal thrombosis in a rat model of septic shock in diabetes. Eur J Inflamm, 13 (1): 40-52. [PMID:26413099]

84. Wood MR, Kim JJ, Han W, Dorsey BD, Homnick CF, DiPardo RM, Kuduk SD, MacNeil T, Murphy KL, Lis EV et al.. (2003) Benzodiazepines as potent and selective bradykinin B1 antagonists. J Med Chem, 46 (10): 1803-6. [PMID:12723943]

85. Wotherspoon G, Winter J. (2000) Bradykinin B1 receptor is constitutively expressed in the rat sensory nervous system. Neurosci Lett, 294 (3): 175-8. [PMID:11072143]

86. Zuccollo A, Navarro M, Frontera M, Cueva F, Carattino M, Catanzaro OL. (1999) The involvement of kallikrein-kinin system in diabetes type I (insulitis). Immunopharmacology, 45 (1-3): 69-74. [PMID:10614992]

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