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非典型β-肾上腺素能受体亚型介导兔海绵体舒张。

Atypical beta-adrenoceptor subtypes mediate relaxations of rabbit corpus cavernosum.

作者信息

Teixeira Cleber E, Baracat Juliana S, Zanesco Angelina, Antunes Edson, De Nucci Gilberto

机构信息

Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas, São Paulo, Brazil.

出版信息

J Pharmacol Exp Ther. 2004 May;309(2):587-93. doi: 10.1124/jpet.103.062026. Epub 2004 Jan 29.

Abstract

This study was performed to characterize the beta-adrenoceptor population in rabbit isolated corpus cavernosum (RbCC) by using nonselective and selective beta-adrenoceptor agonists and antagonists in functional assays. Metaproterenol, ritodrine, fenoterol, and 8-hydroxy-5-[(1R)-1-hydroxy-2-[N-[(1R)-2-(rho-methoxyphenyl)-1-methylethyl]amino]ethyl]carbostyril (TA 2005) (3-100 nmol each) dose dependently relaxed the RbCC preparations. These relaxations were markedly reduced by N(omega)-nitro-L-arginine methyl ester (L-NAME; 10 microM) and 1H-[1,2,4]-oxadiazolo-[4,3,-a]quinoxalin-1-one (ODQ) (10 microM), whereas the adenylyl cyclase inhibitor SQ 22,536 [9-(2-tetrahydrofuryl) adenine] (10 microM) had no effect. In contrast, neither L-NAME nor ODQ affected the isoproterenol-induced RbCC relaxations, but SQ 22,536 abolished this response. Sildenafil (1 microM) significantly potentiated the relaxations induced by beta(2)-agonists without affecting the isoproterenol-evoked relaxations. Rolipram (10 microM) enhanced the relaxations elicited by isoproterenol but had no effect on those induced by the selective beta(2) agonists. Propranolol and (+/-)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride (ICI 118,551) determined a rightward shift in the concentration-response curves to isoproterenol in a noncompetitive manner with a reduction of maximum response at the highest antagonist concentration, with the slope values significantly different from unity. Propranolol and ICI 118,551 had no effect on the relaxations elicited by fenoterol, TA 2005, metaproterenol, and ritodrine. Atenolol and 1-[2-((3-carbamoyl-4-hydroxy)phenoxy) ethylamino]-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl)-phenoxy]-2-propanol methanesulfonate (CGP 20712A) (0.1-10 microM) failed to affect the relaxations induced by all tested beta-adrenoceptor agonists. Our study revealed the existence of two atypical beta-adrenoceptors in the rabbit erectile tissue. Isoproterenol relaxes the rabbit cavernosal tissue by activating atypical beta-adrenoceptors coupled to adenylyl cyclase pathway, whereas the selective beta(2)-adrenoceptor agonists relax the RbCC tissue through another atypical beta-adrenoceptor subtype coupled to nitric oxide release from the sinusoidal endothelium.

摘要

本研究旨在通过在功能试验中使用非选择性和选择性β-肾上腺素能受体激动剂及拮抗剂,对兔离体海绵体(RbCC)中的β-肾上腺素能受体群体进行表征。间羟异丙肾上腺素、利托君、非诺特罗和8-羟基-5-[(1R)-1-羟基-2-[N-[(1R)-2-(对甲氧基苯基)-1-甲基乙基]氨基]乙基]咔唑醇(TA 200)(各3 - 100 nmol)均能剂量依赖性地使RbCC制剂松弛。N(ω)-硝基-L-精氨酸甲酯(L-NAME;10 μM)和1H-[1,2,4]-恶二唑并-[4,3,-a]喹喔啉-1-酮(ODQ)(10 μM)能显著减弱这些松弛作用,而腺苷酸环化酶抑制剂SQ 22,536 [9-(2-四氢呋喃基)腺嘌呤](10 μM)则无作用。相反,L-NAME和ODQ均不影响异丙肾上腺素诱导的RbCC松弛作用,但SQ 22,536可消除此反应。西地那非(1 μM)能显著增强β2-激动剂诱导的松弛作用,而不影响异丙肾上腺素引起的松弛作用。咯利普兰(10 μM)可增强异丙肾上腺素诱导产生的松弛作用,但对选择性β2-激动剂诱导的松弛作用无影响。普萘洛尔和(±)-1-[2,3-(二氢-7-甲基-1H-茚-4-基)氧基]-3-[(1-甲基乙基)氨基]-2-丁醇盐酸盐(ICI 118,551)以非竞争性方式使异丙肾上腺素浓度-反应曲线右移,在最高拮抗剂浓度时最大反应降低,斜率值显著不同于1。普萘洛尔和ICI 118,551对非诺特罗、TA 2005、间羟异丙肾上腺素和利托君诱导的松弛作用无影响。阿替洛尔和1-[2-((3-氨基甲酰基-4-羟基)苯氧基)乙氨基]-3-[4-(1-甲基-4-三氟甲基-2-咪唑基)-苯氧基]-2-丙醇甲磺酸盐(CGP 20712A)(0.1 - 10 μM)未能影响所有测试的β-肾上腺素能受体激动剂诱导的松弛作用。我们的研究揭示了兔勃起组织中存在两种非典型β-肾上腺素能受体。异丙肾上腺素通过激活与腺苷酸环化酶途径偶联的非典型β-肾上腺素能受体使兔海绵体组织松弛,而选择性β2-肾上腺素能受体激动剂则通过与从窦状内皮释放一氧化氮偶联的另一种非典型β-肾上腺素能受体亚型使RbCC组织松弛。

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