Abstract
Restrictive cardiac valvulopathies observed in Parkinson patients treated with the ergoline dopamine agonist pergolide have recently been associated with the agonist efficacy of the drug at 5-hydroxytryptamine 2B (5-HT 2B) receptors. To evaluate whether agonism at 5-HT 2B receptors is a phenomenon of the class of the ergolines, we studied 5-HT 2B receptor-mediated relaxation in porcine pulmonary arteries to five ergolines which are used as antiparkinsonian drugs. Pergolide and cabergoline were potent full agonists in this tissue (pEC 50 8.42 and 8.72). Bromocriptine acted as a partial agonist (pEC 50 6.86). Lisuride and terguride, however, failed to relax the arteries but potently antagonized 5-HT-induced relaxation (p K B 10.32 and 8.49). Thus, agonism at 5-HT 2B receptors seems not to be a class effect of the ergolines.
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