Recent advances in the medicinal chemistry of group II and group III mGlu receptors. Issue 3 (26th January 2017)

• Record Type: Journal Article
• Authors: Jin, Chaobin; Ma, Shutao
• Is Part Of: MedChemComm. Volume 8:Issue 3(2017)
• Page Start: 501
• Page End: 515
• Publication Date: 2017-01-26
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c6md00612d
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : This review summarizes recent advancements in the discovery of group II and group III mGluR allosteric modulators and agonists/antagonists, with a focus on their structures, biological activity, and selectivity. Abstract : Metabotropic glutamate receptors (mGlu receptors) belong to the G-protein-coupled receptors superfamily. They are divided into three groups, in which group II and group III belong to presynaptic receptors that negatively modulate glutamate and γ-aminobutyric acid (GABA) release when activated. In this review, we introduce not only the functions of mGlu receptors, but also the group II and group III allosteric modulators and agonists/antagonists reported over the past five years according to a classification of their structures, with a specific focus on their biological activity and selectivity. In particular, the structure of these compounds and the future directions of ideal candidates are highlighted.