Effects of ring fluorination on the adrenergic properties of phenylephrine.

摘要: Abstract The adrenergic properties of 2-, 4- and 6-fluorophenylephrine (2-FPE, 4-FPE, 6-FPE) were compared to those phenylephrine (PE). order affinities these compounds for α 1 -adrenoceptors as determined by displacement [ 3 H]prazosin H]WB-4101 binding brain membranes was the same potencies eliciting two -adrenergic metabolic responses in guinea-pig cerebral cortical synaptoneurosomes, namely stimulation phosphatidylinositol turnover potentiation 2-chloroadenosine-induced accumulation cyclic AMP. In all cases 6-FPE> PE> 4-FPE> 2-FPE. 2 H]clonidine membrane PE ⩾4-FPE = contrast, inhibition forskolin-stimulated adenylate cyclase activity human platelet via an -adrenoceptor 6-FPE ≈ > 4-FPE ⪢ FPEs partial agonists epinephrine platelets. β-adrenoceptors H]dihydroalprenolol are 2-FPE ⩾ 6-FPE. had positive chronotropic inotropic effects isolated atria apparently through activation a β-adrenoceptor, since pindolol blocked response while prazosin did not. appeared less active than other PEs atria. fat cell membranes, more potent stimulating inactive. Both, cells isoproterenol. Of three FPEs, represents selective agonist α-adrenoceptors s-adrenoceptors PE, and, particular, α-agonists.