慢性β1肾上腺素能受体拮抗剂治疗可使人类右心房中的β2肾上腺素能受体敏感化，但使M2毒蕈碱受体脱敏。
Chronic beta 1-adrenoceptor antagonist treatment sensitizes beta 2-adrenoceptors, but desensitizes M2-muscarinic receptors in the human right atrium.
作者信息
Motomura S, Deighton N M, Zerkowski H R, Doetsch N, Michel M C, Brodde O E
机构信息
Biochemical Research Laboratory, Medizinische Klinik & Poliklinik, University of Essen, F.R.G.
出版信息
Br J Pharmacol. 1990 Oct;101(2):363-9. doi: 10.1111/j.1476-5381.1990.tb12715.x.
Abstract
- In 64 patients undergoing coronary artery bypass grafting the effects of chronic beta 1-adrenoceptor antagonist (metoprolol, atenolol, bisoprolol) treatment on right atrial beta-adrenoceptor and muscarinic M2-receptor number and functional responsiveness were investigated. 2. The beta 1-adrenoceptor antagonists increased right atrial beta 1-adrenoceptor number, did not affect beta 2-adrenoceptor number, and decreased muscarinic M2-receptor number. 3. Concomitantly, activation of right atrial adenylate cyclase by 10 microM GTP, 10 microM isoprenaline and 1 microM forskolin was enhanced and inhibition by 100 microM carbachol was diminished. 4. On isolated, electrically driven right atria the beta 1-adrenoceptor-mediated positive inotropic effect of noradrenaline was - even with beta 1-adrenoceptor number increased - not altered, while the beta 2-adrenoceptor-mediated effect of procaterol was markedly enhanced. However, the carbachol-induced negative inotropic effect was decreased. 5. It is concluded that chronic beta 1-adrenoceptor antagonist treatment increases beta 1-adrenoceptor number and concomitantly sensitizes beta 2-adrenoceptor function, but desensitizes muscarinic M2-receptor function in the human heart.
摘要
- 在64例接受冠状动脉旁路移植术的患者中，研究了慢性β1肾上腺素能受体拮抗剂（美托洛尔、阿替洛尔、比索洛尔）治疗对右心房β肾上腺素能受体和毒蕈碱M2受体数量及功能反应性的影响。2. β1肾上腺素能受体拮抗剂增加了右心房β1肾上腺素能受体数量，不影响β2肾上腺素能受体数量，并降低了毒蕈碱M2受体数量。3. 同时，10微摩尔GTP、10微摩尔异丙肾上腺素和1微摩尔福斯高林对右心房腺苷酸环化酶的激活作用增强，而100微摩尔卡巴胆碱的抑制作用减弱。4. 在离体电驱动右心房上，即使β1肾上腺素能受体数量增加，去甲肾上腺素的β1肾上腺素能受体介导的正性肌力作用也未改变，而丙卡特罗的β2肾上腺素能受体介导的作用则明显增强。然而，卡巴胆碱诱导的负性肌力作用减弱。5. 结论是，慢性β1肾上腺素能受体拮抗剂治疗增加了β1肾上腺素能受体数量，并同时使β2肾上腺素能受体功能敏感化，但使人心肌中的毒蕈碱M2受体功能脱敏。
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