Chimeric receptor analysis of the ketanserin binding site in the human 5-Hydroxytryptamine1D receptor: importance of the second extracellular loop and fifth transmembrane domain in antagonist binding.


The 5-hydroxytryptamine (5-HT)1B/1D receptor subtypes are involved in the regulation of 5-HT release and have gained particular interest because of their apparent role in migraine. Although selective antagonists for both receptor subtypes recently have been developed, the receptor domains involved in the pharmacological specificity of these antagonists are… (More)


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