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1 The aim of the current study was to characterize the alpha(1)-adrenergic receptors (alpha(1)-ARs) present in the isolated tunica media of aorta, in normotensive Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats during the course of ageing and hypertension (rats of 1, 3, 6 and 12 months of age). In all vessels, endothelium was removed. 2 In isolated aortic rings, phenylephrine increased contraction in a concentration- and age-dependent manner and was impaired in old SHR compared with WKY rats. 3 The alpha(1)-AR selective antagonist prazosin showed high affinity (pA(2)) in vessels from both rat strains. 4 The potency of the alpha(1A)-AR selective antagonists, RS 100329 (5-methyl-3-[3-[4-[2-(2,2,2,-trifluoroethoxy) phenyl]-1-piperazinyl] propyl]-2,4-(1H)-pyrimidinedione) and 5-methylurapidil in antagonizing aortic phenylephrine-responses was low. 5 The alpha(1D)-AR selective antagonist, BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1 piperazynil] ethyl]-8-azaspiro [4.5] decane-7,9-dione) potently blocked phenylephrine-induced responses in aorta from both strains and at all ages. 6 Adventitia removal decreased E(max) in older rats and modified the relative affinity (pD(2)), but did not affect the affinity of the selective antagonists. 7 The results suggest that aorta tunica alpha(1D)-AR is the main subtype involved in phenylephrine-induced contraction of rat aorta, while alpha(1A)-AR plays only a minor role. 8 Ageing and hypertension did not modify alpha(1)-ARs in the blood vessel and the tunica adventitia does not seem to participate in contraction, even though alpha(1)-ARs are expressed.

Dr. Gómez Zamudio J.

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