-3受体激动剂

E. Bachus, P. Ponikowski
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引用次数: 1

摘要

β -3肾上腺素能受体(β3-AR)与β1 -和β 2 (β1/2)-肾上腺素能受体相比,在人体组织中分布更为广泛,包括膀胱、大脑、脂肪组织和心血管系统。因此,β3- AR是广泛治疗领域的潜在药物靶点,包括心血管和非心血管领域,包括膀胱过动症(OAB)、抑郁症、代谢综合征、肥胖和心力衰竭(HF)。对β3-AR具有选择性的受体激动剂包括CL 316,243、胺米格隆(SR58611A)、mirabegron (m -178)和vibegron (RVT-901)。然而,在心衰中,关于β3-AR激动剂可能的肌力作用的研究结果仍然模棱两可,一些作者报道心衰和β3-AR拮抗剂的负肌力作用也在研究中。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Beta-3 Receptor Agonists
Beta-3 adrenergic receptors (β3-AR) have a more widespread tissue distribution in the human body as compared to beta1- and beta2 (β1/2)-adrenergic receptors, including in the bladder, brain, adipose tissue and cardiovascular system. Thus, β3- AR are potential drug targets for a wide range of therapeutic areas, both cardiovascular and non-cardiovascular including overactive bladder (OAB), depression, metabolic syndrome, obesity and heart failure (HF).  β3-AR agonists that are selective to the β3-AR include CL 316,243, amibegron (SR58611A), mirabegron (YM-178) and vibegron (RVT-901). However, in HF, study results regarding a possible inotropic effect of β3-AR agonists remain equivocal and some authors report a negative inotropic effect in HF and β3-AR antagonists are also under study.
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