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JoVE Core
Pharmacology
肾上腺素受体(肾上腺素受体):分类
肾上腺素受体(肾上腺素受体):分类
JoVE Core
Pharmacology
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JoVE Core Pharmacology
Adrenergic Receptors (Adrenoceptors): Classification

6.2: 肾上腺素受体(肾上腺素受体):分类

5,093 Views
01:27 min
September 22, 2023
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Please note that some of the translations on this page are AI generated. Click here for the English version.

Overview

肾上腺素受体,或肾上腺素受体,对自主神经递质去甲肾上腺素和其他内源性儿茶酚胺激动剂作出反应。根据药理反应,它们被分为两个主要家族α和β,并根据其位置,诱发反应和对特定激动剂或拮抗剂的亲和力进一步细分。

strong>α-肾上腺素受体

α-肾上腺素受体分为两个主要亚型:α1和α2。α1肾上腺素受体主要位于平滑肌中的突触后效应细胞上,具有三个亚型:α1A,α1B和α1D。α2肾上腺素受体位于突触前肾上腺素能神经元,脂肪细胞,血小板和平滑肌中,具有三个亚型:α2A,α2B和α2C。

ꞵ-肾上腺素受体

ꞵ-肾上腺素受体有三个亚型:ꞵ1,ꞵ2和ꞵ;3。α1肾上腺素受体位于效应器官的突触后部位,如心脏,大脑和脂肪细胞。而在突触前,它们位于肾上腺能和胆碱能神经末梢,肾小球旁囊泡细胞和睫状上皮细胞中。α2肾上腺素受体位于突触后的效应细胞,心脏和平滑肌中。它们也存在于脂肪细胞和心脏组织的突触后部位。

肾上腺素受体是膜结合G蛋白偶联受体

α1肾上腺素受体刺激活化磷脂酶C,产生IP3和DAG作为第二信使。α2肾上腺素受体的活化抑制腺苷酸环化酶(降低cAMP水平)并调节Ca2+和K+离子通道。所有类型的α-肾上腺素受体都会激活腺苷酸环化酶。

α1肾上腺素受体刺激会收缩血管,增加唾液分泌,舒张胃肠道平滑肌,并增加肝糖原分解。然而,α2肾上腺素受体的刺激则抑制自主神经递质去甲肾上腺素和乙酰胆碱的传输和释放,血小板聚集,血管平滑肌收缩和胰岛素释放。刺激α1肾上腺素受体会增加心率和收缩力。α肾上腺素受体刺激会引起支气管扩张,血管扩张,内脏平滑肌松弛,肝糖原分解和肌肉震颤。α3 肾上腺素受体刺激负责膀胱逼尿肌的脂肪分解、产热和松弛。

Transcript

肾上腺素能受体或肾上腺素能受体对儿茶酚胺激动剂(如 NA、Adr 和 ISO)有反应。

所有肾上腺素能受体都是具有 7 个跨膜螺旋的 G 蛋白偶联受体。

儿茶酚胺结合诱导受体的构象变化。这允许 G 蛋白激活,从而改变第二信使的产生。

肾上腺素能受体根据对各种儿茶酚胺激动剂的敏感性分为 α 肾上腺素能受体和 β 肾上腺素能受体。

与 Adr 和 NA 相比,α-肾上腺素能受体对 ISO 的反应较弱。α-肾上腺素能受体进一步分为 α1 和 α2 亚型。

ꞵ-肾上腺素能受体对 ISO 的敏感性高于 Adr 和 NA。ꞵ-肾上腺素能受体细分为 ꞵ1、ꞵ2 和 ꞵ3 亚型。

由肾上腺素能神经元支配的效应器官通常具有主要的肾上腺素能受体亚型。例如,尽管骨骼肌脉管系统同时具有 α1 和 ꞵ2 肾上腺素能感受器,但 ꞵ2 亚型占主导地位。

Explore More Videos

肾上腺素能受体 肾上腺素能受体 去甲肾上腺素 儿茶酚胺 α1 肾上腺素能受体 α2 肾上腺素能受体 β1 肾上腺素能受体 β2 肾上腺素能受体 β3 肾上腺素能受体 G 蛋白偶联受体 磷脂酶 C CAMP 血管收缩 肌肉松弛 脂肪分解 产热

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