Erowid References Database
Kalkman HO, Harms YM, Van Gelderen EM, Batink HD, Timmermans WM, Van Zwieten PA.
“Hypotensive activity of serotonin antagoinists; correlation with
alpha1-adrenoceptor and serotonin receptor blockade”.
Life Sci.. 1983;32:1499-1505.
For a series of 12 serotonin antagonists, largely varying in potency, the decrease in diastolic pressure was determined after intravenous injection into pentobarbitone-anaesthetized normotensive rats. The hypotensive activity of these antagonists was correlated with their affinity for alpha1-adrenoceptors, established by [3 H]prazosin radioligand displacement, and the 5-HT2 serotonergic receptor, determined by inhibition of specific [3H]mianserin binding. The radioligand binding assays were performed since they correspond to the in viva antagonistic potencies of the antagonists at n- and 5-HT2-receptors, respectively. A close correlation (r = 0.963) was found between the affinity for alpha-adrenoceptors and hypotensive activity. On the other hand, a negative correlation of lower statistical quality (r = -0.808) existed between the affinity for 5-HT-receptors and the depressor potency. In this series of 12 compounds, the new antihypertensive drug ketanserin is included for which-it has been speculated that it lowers blood pressure by virtue of its serotonin and agonistic activity. The results of the present study, however, point towards alpha1-adrenolytic potency as an important mechanism in the hypotensive action of the drug.
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