GR-127935

GR-127935
Clinical data
ATC code	none;
Identifiers
	IUPAC name N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1-1'-biphenyl-4-carboxamide;
CAS Number	148672-13-3 ;
PubChem CID	107780;
IUPHAR/BPS	14;
ChemSpider	96935;
UNII	2LLH6CEB40;
ChEBI	CHEBI:64114;
ChEMBL	ChEMBL15928 ;
CompTox Dashboard (EPA)	DTXSID90164044 ;
Chemical and physical data
Formula	C29H31N5O3
Molar mass	497.599 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES n5oc(C)nc5-c(cc2C)ccc2-c(cc3)ccc3C(=O)Nc(ccc1OC)cc1N4CCN(C)CC4;
	InChI InChI=1S/C29H31N5O3/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34/h5-12,17-18H,13-16H2,1-4H3,(H,31,35); Key:YDBCEBYHYKAFRX-UHFFFAOYSA-N;
	(what is this?) (verify)

GR-127935 is a drug which acts as a selective antagonist at the serotonin receptors 5-HT_1B and 5-HT_1D.^[1] It has little effect when given by itself but blocks the antiaggressive effect of 5-HT_1B agonists,^[2] and alters release of serotonin in the brain,^[3] as well as reducing drug-seeking behaviour in cocaine addicted rats.^[4]

References

^ Skingle M, Beattie DT, Scopes DI, Starkey SJ, Connor HE, Feniuk W, Tyers MB (1996). "GR127935: a potent and selective 5-HT1D receptor antagonist". Behavioural Brain Research. 73 (1–2): 157–61. doi:10.1016/0166-4328(96)00089-7. PMID 8788495. S2CID 34394584.
^ Bannai M, Fish EW, Faccidomo S, Miczek KA (August 2007). "Anti-aggressive effects of agonists at 5-HT1B receptors in the dorsal raphe nucleus of mice". Psychopharmacology. 193 (2): 295–304. doi:10.1007/s00213-007-0780-5. PMID 17440711. S2CID 6766784.
^ Rex A, Voigt JP, Wicke KM, Fink H (January 2008). "In vivo/ex vivo and behavioural study on central effects of 5-HT1B/1D and 5-HT1A antagonists in guinea pigs". Pharmacology Biochemistry and Behavior. 88 (3): 196–204. doi:10.1016/j.pbb.2007.07.016. PMID 17888505. S2CID 26577695.
^ Przegaliński E, Gołda A, Filip M (2008). "Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats". Pharmacological Reports. 60 (6): 798–810. PMID 19211971.

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[pmid8788495-1] Skingle M, Beattie DT, Scopes DI, Starkey SJ, Connor HE, Feniuk W, Tyers MB (1996). "GR127935: a potent and selective 5-HT1D receptor antagonist". Behavioural Brain Research. 73 (1–2): 157–61. doi:10.1016/0166-4328(96)00089-7. PMID 8788495. S2CID 34394584.

[pmid17440711-2] Bannai M, Fish EW, Faccidomo S, Miczek KA (August 2007). "Anti-aggressive effects of agonists at 5-HT1B receptors in the dorsal raphe nucleus of mice". Psychopharmacology. 193 (2): 295–304. doi:10.1007/s00213-007-0780-5. PMID 17440711. S2CID 6766784.

[pmid17888505-3] Rex A, Voigt JP, Wicke KM, Fink H (January 2008). "In vivo/ex vivo and behavioural study on central effects of 5-HT1B/1D and 5-HT1A antagonists in guinea pigs". Pharmacology Biochemistry and Behavior. 88 (3): 196–204. doi:10.1016/j.pbb.2007.07.016. PMID 17888505. S2CID 26577695.

[pmid19211971-4] Przegaliński E, Gołda A, Filip M (2008). "Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats". Pharmacological Reports. 60 (6): 798–810. PMID 19211971.

[1]

[2]

[3]

[4]

v t e Treatment of drug dependence (N07B)
Nicotine dependence	Bupropion^# Cytisine Lobeline Mecamylamine Varenicline AATooltip Adrenergic agonist (Clonidine)
Alcohol dependence	AD inhibitor Disulfiram Acamprosate Calcium carbimide Hydrogen cyanamide General anesthetics Nitrous oxide Opioid antagonists Naltrexone Nalmefene Topiramate AATooltip Adrenergic agonist (Clonidine) Baclofen Phenibut
Opioid dependence	AATooltip Adrenergic agonist (Clonidine Lofexidine) Ibogaine Opioids Buprenorphine (+naloxone) Levacetylmethadol Methadone Dihydrocodeine Dihydroetorphine Hydromorphone (extended-release) Morphine (extended-release) Opioid antagonists (Naltrexone Nalmefene)
Benzodiazepine dependence	AATooltip Adrenergic agonist (Clonidine) Benzodiazepines (Diazepam Lorazepam Chlordiazepoxide Oxazepam) Barbiturates (Phenobarbital)

See also

References