Stomati M, Genazzani A D, Petraglia F, Genazzani A R
Department of Obstetrics and Gynecology, University of Pisa, Italy.
Eur J Contracept Reprod Health Care. 1998 Mar;3(1):21-8. doi: 10.3109/13625189809167481.
The brain is one of the specific target tissues for sex steroid hormones. Estrogens, progestins and androgens are able to induce several effects in brain areas of the central nervous system (CNS), through the binding with specific receptors. Specific receptors for gonadal steroids have been identified in the amygdala, hippocampus, basal forebrain cortex, cerebellum, locus ceruleus, midbrain rafe nuclei, glial cells, pituitary gland, hypothalamus and central gray matter. At the hypothalamic level, the principal target for sex steroids is those neurons producing the pulsatile release of the gonadotropin releasing hormone (GnRH), localized in the mediobasal hypothalamus and the arcuate nucleus. The GnRH release depends on the complex and co-ordinated interrelationships among gonadal steroids, pituitary gonadotropins and neuroactive transmitters, such as the noradrenaline, dopamine, opioid peptides (beta-endorphin), acetylcholine, serotonin, gamma-aminobutyrric acid, corticotropin releasing hormone and neuropeptide Y. The interplay of these control mechanisms is governed by peripheral feedback signals; as well as the input from higher brain centers they may modify the GnRH secretion. The anterior pituitary lobe is the best known target tissue for endogenous or exogenous sex steroid hormones, because it is possible to detect luteinizing hormone (LH) and follicle stimulating hormone (FSH) levels in blood, as the expression of the pituitary cells' activity. The synthesis and release of FSH and LH by the gonadotropic cells depend upon the peripheral control of gonadal hormones and the GnRH hypothalamic release. In summary, during a woman's reproductive life, the interaction between neurotransmitters, neuropeptides and gonadal hormones modulates the hypothalamo-pituitary-gonadal axis by acting selectively on the synthesis and release of GnRH and of pituitary gonadotropic hormones. The increased use of oral contraceptives in the last 30 years and, in general, of sex steroid hormone derivative therapies, has led to the study of the biochemical and metabolic properties of the different progestin molecules available in hormonal therapies by focusing attention on the interactions between estrogens and progestins in the modulation of the hypothalamo-pituitary-gonadal axis. The different kinds of estrogen and progestin molecules used in oral contraceptives inhibit the ovulatory process and may interfere with other sex steroid hormone receptors, thus exerting multiple effects in each target tissue.
大脑是性类固醇激素的特定靶组织之一。雌激素、孕激素和雄激素能够通过与特定受体结合，在中枢神经系统（CNS）的脑区诱导多种效应。在杏仁核、海马体、基底前脑皮质、小脑、蓝斑、中脑缝际核、神经胶质细胞、垂体、下丘脑和中央灰质中已鉴定出性腺类固醇的特异性受体。在下丘脑水平，性类固醇的主要靶标是那些产生促性腺激素释放激素（GnRH）脉冲式释放的神经元，这些神经元位于下丘脑内侧基底部和弓状核。GnRH的释放取决于性腺类固醇、垂体促性腺激素和神经活性递质之间复杂且协调的相互关系，如去甲肾上腺素、多巴胺、阿片肽（β-内啡肽）、乙酰胆碱、5-羟色胺、γ-氨基丁酸、促肾上腺皮质激素释放激素和神经肽Y。这些控制机制的相互作用受外周反馈信号支配；除了来自大脑高级中枢的输入外，它们可能会改变GnRH的分泌。垂体前叶是内源性或外源性性类固醇激素最知名的靶组织，因为可以检测血液中的黄体生成素（LH）和卵泡刺激素（FSH）水平，作为垂体细胞活性的表现。促性腺细胞合成和释放FSH和LH取决于性腺激素的外周控制和下丘脑GnRH的释放。总之，在女性的生殖生命过程中，神经递质、神经肽和性腺激素之间的相互作用通过选择性地作用于GnRH和垂体促性腺激素的合成与释放，调节下丘脑-垂体-性腺轴。在过去30年中，口服避孕药以及一般的性类固醇激素衍生疗法的使用增加，促使人们通过关注雌激素和孕激素在调节下丘脑-垂体-性腺轴中的相互作用，来研究激素疗法中可用的不同孕激素分子的生化和代谢特性。用于口服避孕药的不同种类的雌激素和孕激素分子会抑制排卵过程，并可能干扰其他性类固醇激素受体，从而在每个靶组织中发挥多种作用。
