(−)-amidephrine, a selective agonist for α1-adrenoceptors

Add time:09/25/2019    Source:sciencedirect.com

The α-adrenoceptor activity of (−)-amidephrine in the isolated vas deferens of the rat was characterized. In this preparation (−)-amidephrine showed a selective activity on α1-adrenoceptors, and failed to exert any effect on α2-adrenoceptors. The α1-adrenoceptors antagonists prazosin (pA2 8.19 and 8.48) and E-643 (pA2 8.36 and 8.25) inhibited the agonist activity of (−)-amidephrine and (−)-phenylephrine. The pA2 values obtained did not differ significantly, indicating that the two agonists exert their effect on the same receptor. The slopes of Schild plots were not significantly different from 1, suggesting that the inhibition was truly competetive in nature.

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