催产素受体系统:结构、功能、和监管。

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Gimpl G, Fahrenholz F

催产素受体系统:结构、功能、和监管。

杂志启4月2001,81 (2):629 - 83。doi: 10.1152 / physrev.2001.81.2.629。

PubMed ID

11274341 (在PubMed

]

文摘

neurohypophysial肽催产素(OT)和OT-like激素促进繁殖在所有脊椎动物在几个水平。OT基因表达的主要网站是magnocellular下丘脑室旁和视上核的神经元。为了应对各种刺激如吮吸,分娩,或某些类型的压力,脑垂体后叶的加工OT肽释放进入体循环。这样的刺激也导致在细胞核内的OT的释放。此外,oxytocinergic整个中枢神经系统神经元显示广泛的预测。然而,不也是合成外围组织,如子宫、胎盘、羊膜、黄体素、睾丸,和心脏。OT受体是一个典型的类我G protein-coupled受体主要是通过G (q)蛋白磷脂酶C-beta耦合。高亲和性受体状态需要镁(2 +)和胆固醇,这可能函数变构调节器。agonist-binding地区的受体已经被诱变和分子建模和特征不同于对手的结合位点。的功能和生理调节系统是强烈依赖于类固醇。 However, this is, unexpectedly, only partially reflected by the promoter sequences in the OT receptor gene. The classical actions of OT are stimulation of uterine smooth muscle contraction during labor and milk ejection during lactation. While the essential role of OT for the milk let-down reflex has been confirmed in OT-deficient mice, OT's role in parturition is obviously more complex. Before the onset of labor, uterine sensitivity to OT markedly increases concomitant with a strong upregulation of OT receptors in the myometrium and, to a lesser extent, in the decidua where OT stimulates the release of PGF(2 alpha). Experiments with transgenic mice suggest that OT acts as a luteotrophic hormone opposing the luteolytic action of PGF(2 alpha). Thus, to initiate labor, it might be essential to generate sufficient PGF(2 alpha) to overcome the luteotrophic action of OT in late gestation. OT also plays an important role in many other reproduction-related functions, such as control of the estrous cycle length, follicle luteinization in the ovary, and ovarian steroidogenesis. In the male, OT is a potent stimulator of spontaneous erections in rats and is involved in ejaculation. OT receptors have also been identified in other tissues, including the kidney, heart, thymus, pancreas, and adipocytes. For example, in the rat, OT is a cardiovascular hormone acting in concert with atrial natriuretic peptide to induce natriuresis and kaliuresis. The central actions of OT range from the modulation of the neuroendocrine reflexes to the establishment of complex social and bonding behaviors related to the reproduction and care of the offspring. OT exerts potent antistress effects that may facilitate pair bonds. Overall, the regulation by gonadal and adrenal steroids is one of the most remarkable features of the OT system and is, unfortunately, the least understood. One has to conclude that the physiological regulation of the OT system will remain puzzling as long as the molecular mechanisms of genomic and nongenomic actions of steroids have not been clarified.

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