| Autor: |
M D, Wood, K L, Murkitt, S Q, Rice, T, Testa, P K, Punia, M, Stammers, O, Jenkins, N A, Elshourbagy, U, Shabon, S J, Taylor, T L, Gager, J, Minton, W D, Hirst, G W, Price, M, Pangalos |
| Rok vydání: |
2000 |
| Předmět: |
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| Zdroj: |
British journal of pharmacology. 131(6) |
| ISSN: |
0007-1188 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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