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;
ChEBI	CHEBI:64114;
ChEMBL	CHEMBL15928 ;
Chemical and physical data
Formula	C29H31N5O3
Molar mass	497.587 g/mol
3D model (Jmol)	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 ;
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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[edit]

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

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

[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.

[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.

[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.

[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 : PR. 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 Adrenergic agonist (AA): (Clonidine)

Alcohol dependence	AD inhibitor (Disulfiram Calcium carbimide) Acamprosate Opioid antagonists (Naltrexone Nalmefene) Topiramate AA (Clonidine) Baclofen Metadoxine

Opioid dependence	AA (Clonidine Lofexidine) Ibogaine Opioids Buprenorphine (+naloxone) Levacetylmethadol Methadone Dihydrocodeine Dihydroetorphine Hydromorphone (extended-release) Morphine (extended-release) Opioid antagonists (Naltrexone Nalmefene)

Benzodiazepine dependence	AA (Clonidine) Benzodiazepines (Diazepam Lorazepam Chlordiazepoxide Oxazepam) Barbiturates (Phenobarbital)

Amphetamine dependence	Amphetamine Bupropion Topiramate

Cocaine dependence	Bupropion Topiramate

GR-127935

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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^Y
PubChem CID	107780
IUPHAR/BPS	14
ChemSpider	96935
ChEBI	CHEBI:64114
ChEMBL	CHEMBL15928^N
Chemical and physical data
Formula	C₂₉H₃₁N₅O₃
Molar mass	497.587 g/mol
3D model (Jmol)	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
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