GR 125,743

• CAT Number: I007024
• CAS Number: 148547-33-5
• Molecular Formula: C25H28N4O2
• Molecular Weight: 416.53
• Purity: ≥95%
• Synonyms: GR 125,743; GR125,743; GR-125,743.;N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-methyl-4-pyridin-4-ylbenzamide
• Target: Neuronal Signaling
• Solubility: Soluble in DMSO
• Storage: Store at RT
• InChI: InChI=1S/C25H28N4O2/c1-18-16-20(4-6-22(18)19-8-10-26-11-9-19)25(30)27-21-5-7-24(31-3)23(17-21)29-14-12-28(2)13-15-29/h4-11,16-17H,12-15H2,1-3H3,(H,27,30)
• InChIKey: GNOXPYACARZYMW-UHFFFAOYSA-N
• SMILES: O=C(NC1=CC=C(OC)C(N2CCN(C)CC2)=C1)C3=CC=C(C4=CC=NC=C4)C(C)=C3

GR 125,743 (CAT: I007024) is a selective antagonist of the 5-HT1B receptor, which is a subtype of the serotonin receptor. It has been studied for its potential therapeutic applications in the treatment of migraine, anxiety, and depression. By blocking the 5-HT1B receptor, GR 125,743 can modulate serotonin signaling in the brain, leading to altered neurotransmitter activity. This selective antagonism of the 5-HT1B receptor may contribute to its effects on pain perception, mood regulation, and anxiety. Further research is ongoing to explore the potential of GR 125,743 as a therapeutic agent in various neurological and psychiatric disorders.

Reference

1:Eur J Pharmacol. 1997 May 30;327(2-3):247-56. Binding profile of the novel 5-HT1B/1D receptor antagonist, [3H]GR 125,743, in guinea-pig brain: a comparison with [3H]5-carboxamidotryptamine.Audinot V,Lochon S,Newman-Tancredi A,Lavielle G,Millan MJ, PMID: 9200567
Abstract: Native brain 5-HT1B/1D) receptors were studied using the novel antagonist, [3H]GR 125,743 (N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-3-methyl-4-(4-pyri dyl)benzamide). In guinea-pig striatal membranes, [3H]GR 125,743 displayed rapid association (t1/2 = 4.5 min), high (90%) specific binding and high affinity (K(d) = 0.29 nM), although B(max) values (fmol/mg protein) varied according to brain region-striatum: 199; frontal cortex: 89; hippocampus: 79; cerebellum: 26. In frontal cortex, the B(max) determined with [3H]5-CT ([3H]carboxamidotryptamine) was significantly higher (178; P < 0.05), suggesting that it also labels other binding sites. In striatal membranes, guanylylimidodiphosphate (GppNHp) inhibited [3H]5-CT but not [3H]GR 125,743 binding, suggesting that the latter has antagonist properties. Nevertheless, in competition binding experiments, the pK(i) values obtained with [3H]GR 125,743 and [3H]5-CT for 20 serotonergic ligands, including L 694,247 (2-[5-[3-(4-methylsulphonylamino)benzyl-1,2,4-oxadiazol-5-yl ]-1H-indole-3-yl]ethylamine), GR46,611 (3-[3-(2-dimethylamino-ethyl)-1H-indol-6-yl]-N-(4-methoxybenzyl)acrylami de), sumatriptan and alniditan, were highly correlated (r = 0.99). Ketanserin and ritanserin showed low affinity for [3H]GR 125,743 binding to guinea-pig striatal sites (K(i) = 12600 and 369 nM), suggesting that 5-HT1B (rather than 5-HT1D) receptors are predominantly labelled in this tissue. The present data indicate that [3H]GR 125,743 is a useful tool for studying native 5-HT1B/1D receptors.