Synonyms: Fluothane®
halothane is an approved drug (FDA (1958))
Compound class:
Synthetic organic
Comment: Halothane is a volatile anaesthetic which causes rapid anaesthesia, but requires use of additional nitrous oxide and/or neuromuscular blocking agents to be fully effective.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Blin S, Chatelain FC, Feliciangeli S, Kang D, Lesage F, Bichet D. (2014)
Tandem pore domain halothane-inhibited K+ channel subunits THIK1 and THIK2 assemble and form active channels. J Biol Chem, 289 (41): 28202-12. [PMID:25148687] |
2. Gray AT, Zhao BB, Kindler CH, Winegar BD, Mazurek MJ, Xu J, Chavez RA, Forsayeth JR, Yost CS. (2000)
Volatile anesthetics activate the human tandem pore domain baseline K+ channel KCNK5. Anesthesiology, 92 (6): 1722-30. [PMID:10839924] |
3. Kelemen B, Lisztes E, Vladár A, Hanyicska M, Almássy J, Oláh A, Szöllősi AG, Pénzes Z, Posta J, Voets T et al.. (2020)
Volatile anaesthetics inhibit the thermosensitive nociceptor ion channel transient receptor potential melastatin 3 (TRPM3). Biochem Pharmacol, 174: 113826. [PMID:31987857] |
4. Kulkarni RS, Zorn LJ, Anantharam V, Bayley H, Treistman SN. (1996)
Inhibitory effects of ketamine and halothane on recombinant potassium channels from mammalian brain. Anesthesiology, 84 (4): 900-9. [PMID:8638845] |
5. Lazarenko RM, Willcox SC, Shu S, Berg AP, Jevtovic-Todorovic V, Talley EM, Chen X, Bayliss DA. (2010)
Motoneuronal TASK channels contribute to immobilizing effects of inhalational general anesthetics. J Neurosci, 30 (22): 7691-704. [PMID:20519544] |
6. Lesage F, Terrenoire C, Romey G, Lazdunski M. (2000)
Human TREK2, a 2P domain mechano-sensitive K+ channel with multiple regulations by polyunsaturated fatty acids, lysophospholipids, and Gs, Gi, and Gq protein-coupled receptors. J Biol Chem, 275 (37): 28398-405. [PMID:10880510] |
7. Meadows HJ, Randall AD. (2001)
Functional characterisation of human TASK-3, an acid-sensitive two-pore domain potassium channel. Neuropharmacology, 40 (4): 551-9. [PMID:11249964] |
8. Patel AJ, Honoré E, Lesage F, Fink M, Romey G, Lazdunski M. (1999)
Inhalational anesthetics activate two-pore-domain background K+ channels. Nat Neurosci, 2 (5): 422-6. [PMID:10321245] |
9. Patel AJ, Honoré E, Maingret F, Lesage F, Fink M, Duprat F, Lazdunski M. (1998)
A mammalian two pore domain mechano-gated S-like K+ channel. EMBO J, 17 (15): 4283-90. [PMID:9687497] |
10. Talley EM, Bayliss DA. (2002)
Modulation of TASK-1 (Kcnk3) and TASK-3 (Kcnk9) potassium channels: volatile anesthetics and neurotransmitters share a molecular site of action. J Biol Chem, 277 (20): 17733-42. [PMID:11886861] |
11. Washburn CP, Sirois JE, Talley EM, Guyenet PG, Bayliss DA. (2002)
Serotonergic raphe neurons express TASK channel transcripts and a TASK-like pH- and halothane-sensitive K+ conductance. J Neurosci, 22 (4): 1256-65. [PMID:11850453] |
12. Weigl LG, Schreibmayer W. (2001)
G protein-gated inwardly rectifying potassium channels are targets for volatile anesthetics. Mol Pharmacol, 60 (2): 282-9. [PMID:11455015] |