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神经行为学研究中的雌激素受体β激动剂

Estrogen receptor beta agonists in neurobehavioral investigations.

作者信息

Choleris Elena, Clipperton Amy E, Phan Anna, Kavaliers Martin

机构信息

University of Guelph, Department of Psychology, MacKinnon Building, Guelph, Ontario, N1G 2W1, Canada.

出版信息

Curr Opin Investig Drugs. 2008 Jul;9(7):760-73.

Abstract

Neurobehavioral investigations into the functions of estrogen receptor (ER)alpha and ERbeta have utilized 'knockout' mice, phytoestrogens and, more recently, ER-specific agonists. Feeding, sexual, aggressive and social behavior, anxiety, depression, drug abuse, pain perception, and learning (and associated synaptic plasticity) are affected by ERalpha and ERbeta in a manner that is dependent upon the specific behavior studied, gender and developmental stage. Overall, ERalpha and ERbeta appear to function together to foster sociosexual behavior while inhibiting behaviors that, if occurring at the time of behavioral estrous, may compete with reproduction (eg, feeding). Recently developed pharmacological tools have limited selectivity and availability to the research community at large, as they are not commercially available. The development of highly selective, commercially available ERbeta-specific antagonists would greatly benefit preclinical and applied research.

摘要

针对雌激素受体(ER)α和ERβ功能的神经行为学研究采用了“基因敲除”小鼠、植物雌激素,以及最近的ER特异性激动剂。进食、性行为、攻击和社交行为、焦虑、抑郁、药物滥用、疼痛感知和学习(以及相关的突触可塑性)受到ERα和ERβ的影响,其方式取决于所研究的特定行为、性别和发育阶段。总体而言,ERα和ERβ似乎共同发挥作用,促进社会性行为,同时抑制那些如果在行为发情期发生可能与繁殖竞争的行为(如进食)。最近开发的药理学工具对广大研究群体来说选择性和可用性有限,因为它们没有商业销售。开发高选择性、可商业获得的ERβ特异性拮抗剂将极大地有益于临床前研究和应用研究。

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