CHARACTERIZATION OF β-ADRENOCEPTORS IN THE DOG SAPHENOUS VEIN

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In vitro experiments were carried out on strips of the dog saphenous vein to characterize β-adrenoceptors mediating relaxation. Four β-adrenoceptor agonists, isoproterenol, salbutamol, procaterol and α-(3, 4, 5-trimethoxyphenethylaminomethyl)-3, 4-dihydroxybenzylalcohol hydrochloride (T-1583), all produced concentration-dependent relaxation of venous strips contracted by 10-6 M methoxamine. These four drugs behaved as full agonists. In producing venous relaxation, procaterol was about 2.5 times more potent, and salbutamol and T-1583 were 7 and 98 times less potent than isoproterenol, on a molar basis. The concentrationrelaxation response curves to the four agonists were shifted in a parallel way to the right by (t-butyl-amino-3-ol-2-propyl)oximino-9 fluorene hydrochloride (IPS 339), a selective β2-adrenoceptor antagonist, and by practolol. However, pA2-values for IPS 339 against the four agonists were all nearly 11.0, whereas those for practolol were all nearly 5.7. We conclude that β-adrenoceptors in the dog saphenous vein mediating relaxation are predominantly of the β2 type.
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