催产素和血管加压素 V1a 受体配体结合亲和力是否存在性别差异?

IF 3.6 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pharmacological Reports Pub Date : 2024-04-01 Epub Date: 2024-03-13 DOI:10.1007/s43440-024-00577-6
Jack H Taylor, H Elliott Albers
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引用次数: 0

摘要

背景:有大量证据表明,最常见的受体系统之一 G 蛋白偶联受体(GPCR)的功能存在性别差异。在 GPCR 介导的分子信号传导途径上,男性和女性可能在许多方面存在差异,其中首先是配体和受体之间相互作用的稳定性或其结合亲和力。在这里,我们研究了催产素(OT)和血管加压素(AVP)在催产素受体(OTR)和血管加压素 V1a 受体(V1aR)上的结合亲和力,这两种受体在与社会行为相关的脑区都大量存在:为了研究配体-受体结合亲和力在性别和发情周期上的差异,我们选择了雄性(n = 6)叙利亚仓鼠(Mesocricetus auratus)、发情当天的雌性(E雌性,n = 6)和发情第二天的雌性(D2雌性,n = 6)进行研究。将仓鼠的大脑装在载玻片上,进行竞争结合和饱和结合试验:结果:我们发现雌雄仓鼠的 OT 和 AVP 的结合亲和力非常相似。然而,根据雌性动物处于排卵周期的发情期还是绝经期,它们的受体和配体特异性存在微小差异:这些数据表明,在仓鼠和其他物种体内观察到的 OT 和 AVP 作用中的许多性别差异,可能并不是结合亲和力的性别差异造成的。
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Are there sex differences in oxytocin and vasopressin V1a receptors ligand binding affinities?

Background: There is substantial evidence for sex differences in the functioning of one of the most common receptor systems; G protein-coupled receptors (GPCRs). There are many points along the GPCR-mediated molecular signaling pathway at which males and females may differ, one of the first of which, chronologically, is in the stability of the interaction between the ligand and the receptor, or its binding affinity. Here we investigate the binding affinities of oxytocin (OT) and vasopressin (AVP) at the oxytocin receptor (OTR) and the vasopressin V1a receptor (V1aR), both of which are present in numerous in brain regions associated with social behavior.

Method: In order to investigate sex- and estrous cycle-dependent differences in ligand-receptor binding affinity, male (n = 6) Syrian hamsters (Mesocricetus auratus), females on the day of estrus (E females, n = 6), and females on the second day of diestrus (D2 females n = 6) were chosen for study. Brains from hamsters were mounted on slides and competition and saturation binding assays were conducted.

Results: We report a remarkable similarity in the binding affinities of OT and AVP in males and females. Small differences were detected, however, in receptor and ligand specificity in females depending on whether they were in the estrous or diestrous stage of their ovulatory cycle.

Conclusion: These data suggest that sex differences in binding affinity are not a likely source of the many sex differences that have been observed in the effects of OT and AVP in hamsters and other species.

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来源期刊
Pharmacological Reports
Pharmacological Reports 医学-药学
CiteScore
8.40
自引率
0.00%
发文量
91
审稿时长
6 months
期刊介绍: Pharmacological Reports publishes articles concerning all aspects of pharmacology, dealing with the action of drugs at a cellular and molecular level, and papers on the relationship between molecular structure and biological activity as well as reports on compounds with well-defined chemical structures. Pharmacological Reports is an open forum to disseminate recent developments in: pharmacology, behavioural brain research, evidence-based complementary biochemical pharmacology, medicinal chemistry and biochemistry, drug discovery, neuro-psychopharmacology and biological psychiatry, neuroscience and neuropharmacology, cellular and molecular neuroscience, molecular biology, cell biology, toxicology. Studies of plant extracts are not suitable for Pharmacological Reports.
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