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Although certain antiparkinson agents interact with serotonin (5-HT) receptors, little information is available concerning functional actions. Herein, we characterized efficacies of apomorphine, bromocriptine, cabergoline, lisuride, piribedil, pergolide, roxindole, and terguride at human (h)5-HT_1A, h5-HT_1B, and h5-HT_1D receptors [guanosine 5′-O-(3-[³⁵S]thio)triphosphate ([³⁵S]GTPγS) binding], and at h5-HT_2A, h5-HT_2B, and h5-HT_2C receptors (depletion of membrane-bound [³H]phosphatydilinositol). All drugs stimulated h5-HT_1A receptors with efficacies (compared with 5-HT, 100%) ranging from modest (apomorphine, 35%) to high (cabergoline, 93%). At h5-HT_1B receptors, efficacies varied from mild (terguride, 37%) to marked (cabergoline, 102%) and potencies were modest (pEC₅₀ values of 5.8–7.6): h5-HT_1D sites were activated with a similar range of efficacies and greater potency (7.1–8.5). Piribedil and …