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GR-127935

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GR-127935
Clinical data
ATC code
  • none
Identifiers
  • 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
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H31N5O3
Molar mass497.587 g/mol g·mol−1
3D model (JSmol)
  • n5oc(C)nc5-c(cc2C)ccc2-c(cc3)ccc3C(=O)Nc(ccc1OC)cc1N4CCN(C)CC4
  (verify)

GR-127,935 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]

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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  2. ^ Bannai M, Fish EW, Faccidomo S, Miczek KA (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  3. ^ Rex A, Voigt JP, Wicke KM, Fink H (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  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.{{cite journal}}: CS1 maint: multiple names: authors list (link)


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