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The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.

Abstract：

:1. The aim of this study was to characterize the pharmacological profile of the GABA(B1)/GABA(B2) heterodimeric receptor expressed in Chinese hamster ovary (CHO) cells. We have compared receptor binding affinity and functional activity for a series of agonists and antagonists. 2. The chimeric G-protein, G(qi5), was used to couple receptor activation to increases in intracellular calcium for functional studies on the Fluorimetric Imaging Plate Reader (FLIPR), using a stable GABA(B1)/GABA(B2)/G(qi5) CHO cell line. [(3)H]-CGP-54626 was used in radioligand binding studies in membranes prepared from the same cell line. 3. The pharmacological profile of the recombinant GABA(B1/B2) receptor was consistent with that of native GABA(B) receptors in that it was activated by GABA and baclofen and inhibited by CGP-54626A and SCH 50911. 4. Unlike native receptors, the GABA(B1)/GABA(B2)/G(qi5) response was not inhibited by high microMolar concentration of phaclofen, saclofen or CGP 35348. 5. This raises the possibility that the GABA(B1)/GABA(B2)/G(qi5) recombinant receptor may represent the previously described GABA(B) receptor subtype which is relatively resistant to inhibition by phaclofen.

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Wood MD,Murkitt KL,Rice SQ,Testa T,Punia PK,Stammers M,Jenkins O,Elshourbagy NA,Shabon U,Taylor SJ,Gager TL,Minton J,Hirst WD,Price GW,Pangalos M

doi

10.1038/sj.bjp.0703682

subject

Has Abstract

pub_date

2000-11-01 00:00:00

pages

1050-4

issue

6

eissn

0007-1188

issn

1476-5381

journal_volume

131

pub_type

杂志文章

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