title: Medicinal chemistry of ρ GABAC receptors.
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 GABA(C) 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 GABA(C) 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.
authors.affiliation: Faculty of Pharmacy A15, The University of Sydney, NSW, Australia.
authors.forename: Clarissa K L
authors.initials: CK
authors.lastname: Ng
authors.forename: Hye-lim
authors.initials: HL
authors.lastname: Kim
authors.forename: Navnath
authors.initials: N
authors.lastname: Gavande
authors.forename: Izumi
authors.initials: I
authors.lastname: Yamamoto
authors.forename: Rohan J
authors.initials: RJ
authors.lastname: Kumar
authors.forename: Kenneth N
authors.initials: KN
authors.lastname: Mewett
authors.forename: Graham A R
authors.initials: GA
authors.lastname: Johnston
authors.forename: Jane R
authors.initials: JR
authors.lastname: Hanrahan
authors.forename: Mary
authors.initials: M
authors.lastname: Chebib
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D018755:GABA Agonists / Q000737:chemistry; D018756:GABA Antagonists / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D018079:Receptors, GABA / Q000737:chemistry* / Q000378:metabolism*; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000378:metabolism
chemical_list: D018755:GABA Agonists; D018756:GABA Antagonists; C087200:GABA-C receptor; D018079:Receptors, GABA; D005680:gamma-Aminobutyric Acid