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| ROLE OF THE BETA-SUBUNIT IN DETERMINING THE PHARMACOLOGY OF HUMAN GAMMA-AMINOBUTYRIC-ACID TYPE-A RECEPTORS |
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| Author(s): HADINGHAM KL, WINGROVE PB, WAFFORD KA, BAIN C, KEMP JA, PALMER KJ, WILSON AW, WILCOX AS, SIKELA JM, RAGAN CI, WHITING PJ |
| Source: MOLECULAR PHARMACOLOGY Volume: 44 Issue: 6 Pages: 1211-1218 Published: DEC 1993 |
| Times Cited: 177 References: 49 |
| Abstract: A cDNA encoding the human gamma-aminobutyric acid (GABA)A receptor beta2 subunit has been cloned and sequenced. The deduced amino acid sequence of this cDNA shows only a single amino acid change from the rat sequence (Asn-347 in rat, serine in human). Using polymerase chain reaction amplification of human-specific products from human x rodent somatic cell hybrid DNAs, the gene has been assigned to human chromosome 6. By expressing recombinant human GABA(A) receptors containing different beta subunits (beta1, beta2, or beta3) in both transfected cells and XenoPus oocytes, we have been able to determine the influence of the beta subunit on the pharmacology of the receptor. For a number of benzodiazepine binding site compounds, a barbiturate, and several neurosteroids, neither the affinity nor the efficacy of the compounds is influenced by the type of beta subunit present in the receptor molecule. These data suggest that the beta subunit does not significantly influence the benzodiazepine, barbiturate, or steroid site pharmacologies of human GABA(A) receptor subtypes. |
| Document Type: Article |
| Language: English |
Addresses:
1. MERCK SHARP & DOHME LTD, POB 1675, HARLOW CM20 2PT, ESSEX ENGLAND
2. UNIV COLORADO, HLTH SCI CTR, DEPT PHARMACOL, DENVER, CO 80262 USA |
| Publisher: WILLIAMS & WILKINS, 351 WEST CAMDEN ST, BALTIMORE, MD 21201-2436 |
| Subject Category: Pharmacology & Pharmacy |
| IDS Number: MN466 |
| ISSN: 0026-895X |
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