Sundaram, H. and Newmantancredi, A. and Strange, P.G (1993) Characterization of recombinant human serotonin 5HT1A receptors expressed in Chinese hamster ovary cells. [3H]spiperone discriminates between the G-protein-coupled and -uncoupled forms. Biochemical Pharmacology, 45 (5). pp. 1003-1009. ISSN 0006-2952.
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Abstract
5HT1A serotonin (5-hydroxytryptamine) receptors have been characterized by ligand binding in a recombinant Chinese Hamster Ovary cell line expressing the human receptor gene. The agonist ligand (H-3]2-(N,N-dipropylamino)-8-hydroxy-1,2,3,4-tetrahydronaphthalene ([H-3]8-OH-DPAT) and the antagonist [H-3]spiperone were used. For both radioligands the binding sites labelled have the properties of 5HT1A receptors and most antagonists show roughly equal affinities for the receptors labelled by either [H-3]8-OH-DPAT or [H-3]spiperone. Agonists, however, show higher affinities for the sites labelled by [H-3]8-OH-DPAT and the antagonist spiperone conversely shows a higher affinity for the sites labelled by [H-3]spiperone. Whereas [H-3]8-OH-DPAT binding is inhibited by guanosine triphosphate (GTP) the binding of [H-3]spiperone is increased by GTP. A model is proposed for the results whereby [H-3]8-OH-DPAT labels a form of the receptor coupled to a G-protein and [H-3]spiperone labels a form of the receptor uncoupled from G-proteins (or possibly coupled to a different G-protein).
| Item Type: | Article |
|---|---|
| Subjects: | R Medicine > RM Therapeutics. Pharmacology R Medicine > RS Pharmacy and materia medica |
| Divisions: | Faculties > Science Technology and Medical Studies > School of Biosciences |
| Depositing User: | O.O. Odanye |
| Date Deposited: | 20 Jul 2009 22:39 |
| Last Modified: | 20 Jul 2009 22:39 |
| Resource URI: | http://kar.kent.ac.uk/id/eprint/20706 (The current URI for this page, for reference purposes) |
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