International Union of Pharmacology. XV. Subtypes of γ-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function

EA Barnard, P Skolnick, RW Olsen, H Mohler… - Pharmacological …, 1998 - ASPET
EA Barnard, P Skolnick, RW Olsen, H Mohler, W Sieghart, G Biggio, C Braestrup…
Pharmacological reviews, 1998ASPET
This article does not aim to review in detail the properties of-aminobutyric acidA (GABAA) b
receptors, because recent accounts of that topic are available. In this same journal, a review
of the binding properties and pharmacology of these receptors has been published
(Sieghart, 1995). Other reviews have dealt with their ion channel properties as well as their
pharmacology (Mac-Donald and Olsen, 1994; Mohler et al., 1996a, b), whereas others have
concentrated on their molecular biology and protein structure (Wisden and Seeburg, 1992; …
This article does not aim to review in detail the properties of-aminobutyric acidA (GABAA) b receptors, because recent accounts of that topic are available. In this same journal, a review of the binding properties and pharmacology of these receptors has been published (Sieghart, 1995). Other reviews have dealt with their ion channel properties as well as their pharmacology (Mac-Donald and Olsen, 1994; Mohler et al., 1996a, b), whereas others have concentrated on their molecular biology and protein structure (Wisden and Seeburg, 1992; Smith and Olsen, 1995; Stephenson, 1995; McK-ernan and Whiting, 1996). Further, two recent books have provided many short review articles on the functional, behavioral, and psychopharmacological aspects of GABA receptors (Tanaka and Bowery, 1996; Enna and Bowery, 1997) and an account of these latter aspects will not be repeated here.
Building on that background, we will consider here how our knowledge of GABAA receptor structure and function could lead to a classification system. Such a system is not immediately obvious from those previous accounts, as it probably would have been with a onesubunit receptor of the G-protein-coupled class. It is surely no accident that all the present series of NCIUPHAR reports in Pharmacological Reviews on the nomenclature of individual receptor types have so far concerned G protein-coupled receptors. c Certainly the G protein-coupled receptor class covers by far the largest numbers of receptor types; it includes most of the cases in which known clinical drug applications can be related so directly to those types that they have given a great impetus to the receptor analyses. However, beyond those considerations, a major reason for the success in classification of those types must surely be the distinction which can be made therein between the subtypes of a receptor, based on the fact that each will be created by a single polypeptide with a pharmacology which is encoded solely by its own sequence. This is not to say that the classification of any of the receptors previously surveyed in this series has been entirely obvious or without complexities. Nonetheless, the problems involved are
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