Mol Pharmacol 12: 568–580Ĭepelik J, Cernohorsky M (1981) The effects of adrenergic agonists and antagonists on the adenylate cyclase in albino rabbit ciliary processes. Invest Ophthalmol Vis Sci 19: 203–207īylund DB, Snyder SH (1976) Beta-adrenergic receptor binding in membrane preparations from mammalian brain.
Br J Pharmacol 66: 445Pīromberg BB, Gregory DS, Sears ML (1980) Beta-adrenergic receptors in ciliary processes of the rabbit. Lancet 1: 1080–1081īoudot JP, Cavero I, Fenard S, Lefevre-Borg F, Manoury P, Roach AG (1979) Preliminary studies on SL 75212, a new potent cardioselective betaadrenoceptor antagonist. Br J Pharmacol 69: 292P-293Pīlack JW, Crowther AF, Shanks RG, Smith LH, Dornhorst AC (1964) A new adrenergic beta-receptor antagonist. Exp Eye Res 31: 471–477īilski A, Dorries S, Fitzgerald JD, Jessup R, Tucker H, Wale J (1980) ICI 118,551, a potent beta 2-adrenoceptor antagonist. J Med Chem (in press)īhargava G, Makman MH, Katzman R (1980) Distribution of beta-adrenergic receptors and isoproterenol-stimulated cyclic AMP formation in monkey iris and ciliary body. Life Sci 12: 107–119īaldwin JJ, Denny GH, Gross DM, Hirschmann R, Freedman MB, Ponticello GS, Sweet CS (1983) Beta 1-selective adrenoceptor antagonists: examples of the 2- imidazole class. Acta Pharmacol Toxicol 25: 9–40Īblad B, Carlsson E, Ek L (1973) Pharmacological studies of two new cardioselective adrenergic beta-receptor antagonists. Consequently, the above three observations reinforce the notion that rabbit-iris ciliary bodies contain β-adrenergic receptors predominantly of the β 2-subtype.Īblad B, Brogard M, Ek L (1967) Pharmacological properties of H56/28 - a beta-adrenergic receptor antagonist. Finally, for the above β-adrenoceptor antagonists, a highly significant correlation was obtained for displacement of radioligand to ocular tissues (pKi values) relative to antagonism (pA 2 values) of isoproterenol-induced guinea-pig tracheal relaxation but not guinea-pig atrial chronotropic effects. Similar radioligand displacement by β-adrenoceptor antagonists was in the order of potency: alprenolol ≧ bupranolol = oxprenolol = timolol = propranolol > ICI 118,551 = IPS 339 ≫ betaxolol > metoprolol.
Potencies for the displacement of 3H-dihydroalprenolol radioligand binding to membranes obtained from rabbit-iris ciliary bodies by β-adrenoceptor agonists was in the order: isoproterenol ≧ epinephrine > salbutamol > terbutaline > tazolol > norepinephrine. Direct comparison of drug interaction with intraocular relative to extraocular β-adrenergic receptors was used to test the hypothesis that the receptors in ocular tissues are of the β 2-subtype.
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