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• W2019010159 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-pyridyl)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 (Kd=0.29 nM), although Bmax values (fmol/mg protein) varied according to brain region-striatum: 199; frontal cortex: 89; hippocampus: 79; cerebellum: 26. In frontal cortex, the Bmax 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 pKi 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), GR 46,611 (3-[3-(2-dimethylamino-ethyl)-1H-indol-6-yl]-N-(4-methoxybenzyl)acrylamide), 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 (Ki=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." @default.
• W2019010159 created "2016-06-24" @default.
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• W2019010159 date "1997-05-01" @default.
• W2019010159 modified "2023-10-12" @default.
• W2019010159 title "Binding profile of the novel 5-HT1B/1D receptor antagonist, [3H]GR125,743, in guinea-pig brain: a comparison with [3H]5-carboxamidotryptamine" @default.
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• W2019010159 doi "https://doi.org/10.1016/s0014-2999(97)89668-9" @default.
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