GR-127935

GR-127935 is a drug which acts as a selective antagonist at the serotonin receptors 5-HT1B and 5-HT1D.[1] It has little effect when given by itself but blocks the antiaggressive effect of 5-HT1B agonists,[2] and alters release of serotonin in the brain,[3] as well as reducing drug-seeking behaviour in cocaine addicted rats.[4]

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
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H31N5O3
Molar mass497.599 g·mol−1
3D model (JSmol)
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
 NY (what is this?)  (verify)

See also

References
  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.
  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.
  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.
  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.


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