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Atypical beta-adrenoceptors of rat thoracic aorta.

机译:大鼠胸主动脉的非典型β肾上腺素受体。

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The possible existence of atypical beta-adrenoceptors in vascular smooth muscle of rat isolated thoracic aorta was investigated. Isoprenaline (10(-8)-10(-4) M) produced concentration-dependent relaxation of phenylephrine (10(-5) M) precontracted rings of endothelium-denuded rat aorta in vitro. Isoprenaline-induced relaxation was resistant to blockade by atenolol (10(-6) M). But, propranolol (2 x 10(-7) M) caused a non-competitive inhibition and SR 59230A (6.6 x 10(-6) M), a beta3-adrenoceptor selective antagonist, failed to produce additional antagonism in presence of propranolol. BRL 37344 (10(-8)-10(-4) M), a beta3-selective agonist, did not relax ring segments precontracted with phenylephrine (10(-5) M) in the absence of endothelium. The non-conventional partial agonist (-)-cyanopindolol (5 x 10(-6)-10(-4) M) induced a marked relaxation in phenylephrine (10(-5)M) precontracted aortic rings without endothelium. This vasodilation was resistant to blockade by propranolol (2 x 10(-7) M) and SR 59230A (10(-5) M). Salbutamol (10(-8)-10(-4) M) produced concentration-dependent relaxation in isolated endothelium-denuded aortic rings precontracted with phenylephrine (10(-5) M). Propranolol (2 x 10(-7) M), but not atenolol (10(-6) M), inhibited this relaxant response. It is concluded that in endothelium-denuded thoracic aorta, salbutamol acts through beta2-adrenoceptors whereas isoprenaline seems to activate both beta2-adrenoceptors and an atypical beta-adrenergic receptor. This atypical beta-adrenoceptor is distinct from putative beta3-adrenoceptor and maybe resembles the reported fourth cardiac beta-adrenoceptor.
机译:研究大鼠离体胸主动脉血管平滑肌中可能存在非典型β-肾上腺素能受体。异丙肾上腺素(10(-8)-10(-4)M)在体外产生浓度依赖性的去氧肾上腺素(10(-5)M)预缩环的内皮剥夺大鼠主动脉。异丙肾上腺素诱导的松弛对阿替洛尔(10(-6)M)的阻滞具有抵抗力。但是,普萘洛尔(2 x 10(-7)M)引起非竞争性抑制,而β3-肾上腺素受体选择性拮抗剂SR 59230A(6.6 x 10(-6)M)在普萘洛尔的存在下无法产生额外的拮抗作用。 BRL 37344(10(-8)-10(-4)M)是一种β3选择性激动剂,在没有内皮的情况下,不会松弛与苯肾上腺素(10(-5)M)预收缩的环段。非常规的部分激动剂(-)-氰基吲哚洛尔(5 x 10(-6)-10(-4)M)引起去氧肾上腺素(10(-5)M)预收缩的主动脉环明显松弛,而没有内皮。这种血管舒张可抵抗普萘洛尔(2 x 10(-7)M)和SR 59230A(10(-5)M)的阻断作用。沙丁胺醇(10(-8)-10(-4)M)在与去氧肾上腺素(10(-5)M)预收缩的孤立的内皮剥除的主动脉环中产生浓度依赖性的弛豫。普萘洛尔(2 x 10(-7)M),但阿替洛尔(10(-6)M)没有抑制这种松弛反应。结论是,在内皮剥脱的胸主动脉中,沙丁胺醇通过β2肾上腺素受体起作用,而异戊二烯似乎同时激活β2肾上腺素受体和非典型的β肾上腺素受体。这种非典型的β-肾上腺素受体不同于假定的β3-肾上腺素受体,并且可能类似于已报道的第四种心脏β-肾上腺素受体。

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