A GABAB Mystery: The Search for Pharmacologically Distinct GABAB Receptors
Abstract
The classification of neurotransmitter receptors into distinct pharmacological subtypes is of major importance in drug discovery. This quest is particularly important for neurotransmitter systems that are widely distributed. Because γ-aminobutyric acid (GABA) receptors, both GABAA and GABAB, are found throughout the neuroaxis, they are likely involved in all central nervous system functions. Accordingly, the therapeutic promise of GABAB receptor manipulation depends upon the identification of subtypes than can be specifically targeted.
The preponderance of GABAergic activity in rat brain is revealed by in situ hybridization of mRNA that encodes the GABABR1 receptor. The development of drugs that can usefully modulate GABAB receptor activity hinges in part on efforts to identify and target pharmacologically distinguishable receptor subtypes.
[Image courtesy of Nature (www.nature.com) and B. Bettler. Nature 386, 239–246 (1997)]
- © American Society for Pharmacology and Experimental Theraputics 2001
