Medicinal chemistry of ρ GABAC receptors

Author:

Ng Clarissa KL1,Kim Hye-lim1,Gavande Navnath1,Yamamoto Izumi1,Kumar Rohan J1,Mewett Kenneth N2,Johnston Graham AR2,Hanrahan Jane R1,Chebib Mary

Affiliation:

1. Faculty of Pharmacy A15, The University of Sydney, NSW, Australia 2006

2. Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology D06, The University of Sydney, NSW, Australia 2006

Abstract

The inhibitory neurotransmitter, GABA, is a low-molecular-weight molecule that can achieve many low-energy conformations, which are recognized by GABA receptors and transporters. In this article, we assess the structure–activity relationship profiles of GABA analogs at the ionotropic ρ GABAC receptor. Such studies have significantly contributed to the design and development of potent and selective agonists and antagonists for this subclass of GABA receptors. With these tools in hand, the role of ρ GABAC receptors is slowly being realized. Of particular interest is the development of selective phosphinic acid analogs of GABA and their potential use in sleep disorders, inhibiting the development of myopia, and in improving learning and memory.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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