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Bartoszyk GD, van Amsterdam C, Bottcher H, Seyfried CA: EMD 281014, a new selective serotonin 5-HT2A receptor antagonist. . Eur J Pharmacol. 2003 Jul 25;473(2-3):229-30.
The 5-HT2A receptor ligand 7-[4-[2-(4-fluoro-phenyl)-ethyl]-piperazine-1-carbonyl]-1H-indole-3-carbon itrile HCl (EMD 281014) selectively binds to human (h) and rat 5-HT2A receptors (IC50 values 0.35 and 1 nM, respectively; vs. 1334 nM for h5-HT2C) and inhibited 5-HT-stimulated [35S] guanosine 5'-O-3-thiotriphosphate (GTPgammaS)-accumulation in h5-HT2A transfected Chinese hamster ovary cells (IC50 9.3 nM). |
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