Brodde O E
J Recept Res. 1983;3(1-2):151-62. doi: 10.3109/10799898309041930.
Regulation of human beta 2-adrenergic receptors in lymphocytes (determined by (+/-)-125iodocyanopindolol (ICYP) binding) and alpha 2-adrenergic receptors in platelets (determined by 3H-yohimbine binding) was studied. While beta 2-adrenergic receptor number did not change with age, a significant negative correlation between the number of alpha 2-adrenergic receptors and age was found; plasma catecholamines, on the contrary, were elevated in the elderly. In healthy women during normal menstrual cycle the number of alpha 2-adrenergic receptors decreased with increasing plasma estradiol levels. Incubation of lymphocyte membranes with isoprenaline (100 microM) and of platelet membranes with clonidine (1-100 microM) led to a reduction of the number of beta 2- and alpha 2-receptors, respectively, without changes in the KD-values. Treatment of hypertensive patients with clonidine (3x150 micrograms/die) for 7 days reduced the number of alpha 2-adrenergic receptors in platelets. In platelet membranes from such treated patients inhibition of 3H-yohimbine binding by clonidine and adrenaline was not affected by 10(-4)M GTP. It is concluded, that human alpha- and beta-adrenergic receptors undergo regulatory mechanisms similar to those recently described for adrenergic receptors in a variety of animal models.
研究了淋巴细胞中人类β2 - 肾上腺素能受体（通过（±）-125碘氰吲哚洛尔（ICYP）结合测定）和血小板中α2 - 肾上腺素能受体（通过3H - 育亨宾结合测定）的调节情况。β2 - 肾上腺素能受体数量不随年龄变化，而α2 - 肾上腺素能受体数量与年龄呈显著负相关；相反，老年人血浆儿茶酚胺水平升高。在正常月经周期的健康女性中，α2 - 肾上腺素能受体数量随血浆雌二醇水平升高而减少。用异丙肾上腺素（100μM）孵育淋巴细胞膜，用可乐定（1 - 100μM）孵育血小板膜，分别导致β2 - 和α2 - 受体数量减少，而KD值无变化。用可乐定（3×150μg/天）治疗高血压患者7天，可使血小板中α2 - 肾上腺素能受体数量减少。在经如此治疗患者的血小板膜中，10（-4）M GTP不影响可乐定和肾上腺素对3H - 育亨宾结合的抑制作用。得出结论，人类α - 和β - 肾上腺素能受体经历的调节机制类似于最近在多种动物模型中描述的肾上腺素能受体的调节机制。
