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GR-127,935
Systematic (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
Identifiers
CAS number 148672-13-3
ATC code  ?
PubChem 107780
Chemical data
Formula C 29H31N5O3  
Mol. mass 497.587 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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 anti-aggressive 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]

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. PMID 8788495.  
  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.  
  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.  
  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.  
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