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体内使用β-肾上腺素受体拮抗剂治疗是否会改变体外人腺苷酸环化酶的反应性?

Does treatment with beta-adrenoceptor antagonists in vivo alter human adenylate cyclase responsiveness in vitro?

作者信息

Michel M C, Klüppel M, Philipp T, Brodde O E

机构信息

Department of Medicine, University of Essen, Germany.

出版信息

Br J Clin Pharmacol. 1991 Jul;32(1):105-9. doi: 10.1111/j.1365-2125.1991.tb05620.x.

Abstract
  1. Treatment with beta-adrenoceptor antagonists in vivo can alter adenylate cyclase responsiveness in the human heart. We have determined the effects of treatment with four different beta-adrenoceptor antagonists in vivo on the responsiveness of lymphocyte and platelet adenylate cyclase in vitro in healthy volunteers. 2. Propranolol (non-selective, 4 x 40 mg day), bisoprolol (beta 1-selective, 1 x 10 mg day), and ICI 118.551 (beta 2-selective, 3 x 25 mg day) were tested as drugs without and pindolol (non-selective, 2 x 5 mg day) as a drug with intrinsic sympathomimetic activity. Adenylate cyclase stimulation by GTP, prostaglandin E1 and forskolin was determined before, after a 7 day treatment period and 7 days after drug withdrawal. 3. Neither treatment with or withdrawal of any of the beta-adrenoceptor antagonists altered adenylate cyclase responsiveness. 4. We conclude that adenylate cyclase responsiveness in circulating blood cells underlies different regulatory mechanisms than that in solid tissues such as the human heart. Our data suggest that circulating blood cells do not always reflect alterations in solid tissues.
摘要
  1. 体内使用β-肾上腺素能受体拮抗剂治疗可改变人心脏中的腺苷酸环化酶反应性。我们已经确定了在健康志愿者体内使用四种不同的β-肾上腺素能受体拮抗剂治疗对体外淋巴细胞和血小板腺苷酸环化酶反应性的影响。2. 普萘洛尔(非选择性,每日4次,每次40毫克)、比索洛尔(β1选择性,每日1次,每次10毫克)和ICI 118.551(β2选择性,每日3次,每次25毫克)作为无内在拟交感活性的药物进行测试,吲哚洛尔(非选择性,每日2次,每次5毫克)作为具有内在拟交感活性的药物进行测试。在7天治疗期之前、之后以及停药7天后,测定GTP、前列腺素E1和福斯高林对腺苷酸环化酶的刺激作用。3. 使用或停用任何一种β-肾上腺素能受体拮抗剂均未改变腺苷酸环化酶反应性。4. 我们得出结论,循环血细胞中的腺苷酸环化酶反应性与实体组织(如人心脏)中的反应性具有不同的调节机制。我们的数据表明,循环血细胞并不总是反映实体组织中的变化。

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