Molecular insight develops our understanding of the GABA(B) receptor.
The GABA(B) receptor has been cloned and shown to consist of a heterodimer of two 7-transmembrane receptor subunits. Cloning of the receptor has allowed detailed analysis of the pharmacology in recombinant assays and has also generated a range of high-throughput functional assays suitable for compound screening. Detailed analysis of the distribution of the receptor at the mRNA and protein level has also been completed. As yet, no molecular subtypes of the receptor have been identified and the challenge for drug development remains the identification of compounds with desired therapeutic benefit combined with a low side effect profile.
Marshall
F H
FH
Molecular Pharmacology Department, Glaxo Wellcome Research and Development, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK. fhm27375@glaxowellcome.co.uk