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  • Title: Effects of ergotamine and dihydroergotamine on 5-hydroxytryptamine-2A receptors in the isolated rat aorta.
    Author: Kalkman HO, Schneider F.
    Journal: Pharmacology; 1996 Dec; 53(6):351-5. PubMed ID: 9032799.
    Abstract:
    Ergotamine contracted isolated rat aorta rings with an intrinsic activity of 50% of that of 5-hydroxytryptamine. (5-HT, 0.1 mmol/l). Dihydroergotamine did not contract the tissue, but insurmountably blocked contraction in response to ergotamine and 5-HT. The 5-HT2A receptor antagonist, ketanserin (0.1 mumol/l), inhibited ergotamine (pKB 8.0) and 5-HT (pKB 8.1) induced contractions. These results indicate that in the rat aorta ergotamine is a partial 5-HT2A receptor agonist, whilst dihydroergotamine is an insurmountable 5-HT2A receptor antagonist. The present data could explain why ergotamine displays more cardiovascular and uterotonic side effects than dihydroergotamine.
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