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β-肾上腺素受体对肾上腺素、去甲肾上腺素和异丙肾上腺素具有不同的敏感性。激动剂的效力顺序如下:
异丙肾上腺素 > 肾上腺素 > 去甲肾上腺素
神经递质与这些受体的结合会导致腺苷酸环化酶的活化,从而增加细胞内cAMP的浓度并调节细胞内的钙离子通道。它们进一步被分为β;1、β;2和β;3亚型。
β;1-肾上腺素受体:β;1-肾上腺素受体对肾上腺素和去甲肾上腺素的亲和力相等。它们位于心脏和脑组织、脂肪细胞的突触后位置,以及胆碱能和肾上腺素能神经末梢的突触前位置,还有肾细胞上。激动β;1-肾上腺素受体会导致心肌收缩力增加、心动过速、脂肪分解和肾素产生增加。
β;2-肾上腺素受体:β;2受体对肾上腺素的亲和力较高,位于心脏和血管平滑肌的突触后位置。它们的刺激会导致支气管扩张、血管扩张、外周阻力降低、肝脏和肌肉中胰高血糖素释放和糖原分解的增加,以及女性子宫松弛。
β;3-肾上腺素受体:β;3受体对去甲肾上腺素的敏感性较高,位于心脏和脂肪细胞的突触后位置,与β;1-肾上腺素受体和代谢活性一起调节脂肪分解。
与 Adr 和 NA 相比,β 肾上腺素能受体或 β-肾上腺素能受体对 ISO 的反应更强。
刺激后,所有 β-肾上腺素能受体都会激活腺苷酸环化酶,导致 cAMP 产生增加和钙通道调节。
这些受体根据各种因素进一步分为三个亚型。
β1 受体对 Adr 和 NA 的亲和力几乎相等。它们主要位于心脏组织、脂肪细胞和肾细胞中。
它们的刺激会导致心动过速、脂肪分解和肾素生成。
β2 受体对 Adr 的亲和力高于 NA。它们位于突触后心血管、呼吸系统和泌尿生殖系统的平滑肌中。它们导致支气管扩张、血管舒张、外周阻力降低、膀胱松弛和怀孕子宫。
β3 受体对 NA 的敏感性高于 Adr。它们位于突触后脂肪细胞和膀胱上。它们调节代谢活动和脂肪分解,并放松膀胱的逼尿肌。
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