Agonist profile of ergometrine (ergonovine) on a population of postsynaptic α-adrenoceptors

Ergometrine (0.02-5 microM) produced concentration-related contractions of the mouse anococcygeus muscle, which were unaffected by cocaine (2 microM) or by pretreatment of mice with 6-hydroxydopamine. Contractions were reduced by alpha-adrenoceptor antagonists; the rank order of potency was prazosin greater than phentolamine greater than yohimbine. With phenoxybenzamine as antagonist, the estimated dissociation constant (KD) for ergometrine was 0.41 microM. It is concluded that ergometrine causes direct activation of postsynaptic alpha 1-adrenoceptors, and it is suggested that it acts on the same subtype of the receptor as imidazoline agonists.