Characterization of β-Adrenoceptors in Pig Basilar Artery from Functional and Radioligand Binding Studies

[摘要] References(16)Cited-By(9)β-Adrenoceptors in pig basilar arteries were investigated by measuring the relaxation responses to norepinephrine and by a radioligand binding assay with [3H]-dihydroalprenolol (DHA). Norepinephrine induced concentration-dependent relaxations. The relaxation responses were independent of the presence of endothelial cells, and they were competitively antagonized by (±)-propranolol, atenolol, butoxamine and ICI 118, 551. Specific [3H]-DHA binding to β-adrenoceptors was saturable, reversible and high affinity (Kd=1.4 nM), with a Bmax of 48.7 fmol/mg protein. Computer analysis of inhibition of [3H]DHA binding by atenolol, butoxamine and ICI 118, 551 gave a β1:β2-adrenoceptor ratio of approximately 65:35. The pA2 values of these antagonists were significantly correlated with the Ki values for β1-adrenoceptor determined by the radioligand binding assay. The present findings indicate that the relaxation responses to norepinephrine are predominantly mediated through the stimulation of β1-adrenoceptors on vascular smooth muscle cells in a pig basilar artery.

[学科分类] 药理学

[关键词] Basilar artery (pig);Relaxation;β1-Adrenoceptor;Norepinephrine;[3H]-Dihydroalprenolol