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GR125743 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D.1 It binds to the 5-HT1B and 5-HT1D receptors in HeLa cells expressing the human receptors (Kds = 1.02 and 6.2 nM, respectively). Radiolabeled forms of GR125743 have been used to evaluate other potential ligands of the 5-HT1B and 5-HT1D receptors.
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1. Characterization of human serotonin 1D and 1B receptors using [3H]-