mGlu2/3 受体激动剂（LY354740）在焦虑症中的作用。

IF 3.3 3区心理学 Q1 BEHAVIORAL SCIENCES Pharmacology Biochemistry and Behavior Pub Date : 2024-07-18 DOI:10.1016/j.pbb.2024.173826

Darryle D. Schoepp

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引用次数: 0

摘要

焦虑中的 mGlu2/3 受体（LY354740） mGlu2/3 受体被激活后，会降低与焦虑有关的边缘突触上的谷氨酸兴奋。口服活性激动剂化合物 LY354740（或原药 LY544344）在压力/焦虑的动物和人体模型中具有活性。后来的临床研究显示，该化合物对患者的广泛性焦虑症有疗效，在临床上验证了这一机制。然而，由于在长期毒理学研究中出现了啮齿动物癫痫发作，该化合物被终止研究。

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mGlu2/3 receptor agonist (LY354740) in anxiety

mGlu2/3 Receptors (LY354740) in Anxiety mGlu2/3 receptors when activated decrease glutamate excitation on limbic synapses involved in anxiety. The orally active agonist compound LY354740 (or prodrug LY544344) was active in animal and human models of stress/anxiety. Later clinical studies showed efficacy in generalized anxiety in patients, validating this mechanism clinically. However, the compound was terminated due to rodent seizures in long-term toxicology studies.

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来源期刊

Pharmacology Biochemistry and Behavior 医学-行为科学

CiteScore

6.40

自引率

2.80%

发文量

122

审稿时长

38 days

期刊介绍： Pharmacology Biochemistry & Behavior publishes original reports in the areas of pharmacology and biochemistry in which the primary emphasis and theoretical context are behavioral. Contributions may involve clinical, preclinical, or basic research. Purely biochemical or toxicology studies will not be published. Papers describing the behavioral effects of novel drugs in models of psychiatric, neurological and cognitive disorders, and central pain must include a positive control unless the paper is on a disease where such a drug is not available yet. Papers focusing on physiological processes (e.g., peripheral pain mechanisms, body temperature regulation, seizure activity) are not accepted as we would like to retain the focus of Pharmacology Biochemistry & Behavior on behavior and its interaction with the biochemistry and neurochemistry of the central nervous system. Papers describing the effects of plant materials are generally not considered, unless the active ingredients are studied, the extraction method is well described, the doses tested are known, and clear and definite experimental evidence on the mechanism of action of the active ingredients is provided.