Agonism at 5-HT2B receptors is not a class effect of the ergolines

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-hydroxytryptamine2B (5-HT2B) receptors. To evaluate whether agonism at 5-HT2B receptors is a phenomenon of the class of the ergolines, we studied 5-HT2B 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 (pEC50 8.42 and 8.72). Bromocriptine acted as a partial agonist (pEC50 6.86). Lisuride and terguride, however, failed to relax the arteries but potently antagonized 5-HT-induced relaxation (pKB 10.32 and 8.49). Thus, agonism at 5-HT2B receptors seems not to be a class effect of the ergolines.