N-[4-Methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1-biphen

• CAT Number: M101327
• CAS Number: 148642-42-6
• Molecular Formula: C29H32ClN5O3
• Molecular Weight: 534.057
• Purity: ≥95%
• Target: 5-HT Receptor
• Solubility: Soluble to 100 mM in sterile water
• Storage: Desiccate at RT
• IUPAC Name: N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide;hydrochloride
• InChI: InChI=1S/C29H31N5O3.ClH/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);1H
• InChIKey: SRVVUYIJVBLEJI-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC(=C1)C2=NOC(=N2)C)C3=CC=C(C=C3)C(=O)NC4=CC(=C(C=C4)OC)N5CCN(CC5)C.Cl

GR 127935 HCl (Cat.No:M101327) is a potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). GR 127935 HCl displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types.

Reference

1: Sánchez-Maldonado C, López-Sánchez P, Anguiano-Robledo L, Leopoldo M, Lacivita E, Terrón JA. GR-127935-sensitive mechanism mediating hypotension in anesthetized rats: are 5-HT5B receptors involved? J Cardiovasc Pharmacol. 2015 Apr;65(4):335-41. doi: 10.1097/FJC.0000000000000200. PubMed PMID: 25502305.2: Uphouse L, Hiegel C, Guptarak J, Maswood N. Progesterone reduces the effect of the serotonin 1B/1D receptor antagonist, GR 127935, on lordosis behavior. Horm Behav. 2009 Jan;55(1):169-74. doi: 10.1016/j.yhbeh.2008.09.011. PubMed PMID: 18952090; PubMed Central PMCID: PMC2665997.3: Chaouloff F, Courvoisier H, Moisan MP, Mormède P. GR 127935 reduces basal locomotor activity and prevents RU 24969-, but not D-amphetamine-induced hyperlocomotion, in the Wistar-Kyoto hyperactive (WKHA) rat. Psychopharmacology (Berl). 1999 Jan;141(3):326-31. PubMed PMID: 10027515.4: Harrison AA, Parsons LH, Koob GF, Markou A. RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist. Psychopharmacology (Berl). 1999 Jan;141(3):242-50. PubMed PMID: 10027505.5: Chaouloff F, Aguerre S, Mormede P. GR 127935 and (+)-WAY 100135 do not affect TFMPP-induced inhibition of 5-HT synthesis in the midbrain and hippocampus of Wistar-Kyoto rats. Neuropharmacology. 1998 Sep;37(9):1159-67. PubMed PMID: 9833646.6: Villalón CM, Centurión D, Luján-Estrada M, Terrón JA, Sánchez-López A. Mediation of 5-HT-induced external carotid vasodilatation in GR 127935-pretreated vagosympathectomized dogs by the putative 5-HT7 receptor. Br J Pharmacol. 1997 Apr;120(7):1319-27. PubMed PMID: 9105708; PubMed Central PMCID: PMC1564589.7: De Vries P, Heiligers JP, Villalón CM, Saxena PR. Blockade of porcine carotid vascular response to sumatriptan by GR 127935, a selective 5-HT1D receptor antagonist. Br J Pharmacol. 1996 May;118(1):85-92. PubMed PMID: 8733580; PubMed Central PMCID: PMC1909483.8: O/’Neill MF, Fernández AG, Palacios JM. GR 127935 blocks the locomotor and antidepressant-like effects of RU 24969 and the action of antidepressants in the mouse tail suspension test. Pharmacol Biochem Behav. 1996 Mar;53(3):535-9. PubMed PMID: 8866952.