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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Neelands, Torben R. Jarvis, Michael F. Faltynek, Connie R. Burgard, Edward C. Niforatos, Wende Mcdonald, Heath A. Lynch, Kevin J. Uchic, Marie E. |
| Description | Author Affiliation: Neelands TR ( Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, R04PM, AP9A, Abbott Park, IL 60064-6123, USA.) |
| Abstract | (1) Rapid desensitization of ligand-gated ion channel receptors can alter the apparent activity of receptor modulators, as well as make detection of fast-channel activation difficult. Investigation of the antagonist pharmacology of ATP-sensitive homomeric P2X3 receptors is limited by agonist-evoked fast-desensitization kinetics. (2) In the present studies, chimeric receptors were created using the coding sequence for the N-terminus and the first transmembrane domain of either the nondesensitizing human P2X2a or fast-desensitizing P2X3 receptor joined to the sequence encoding the extracellular loop, second transmembrane domain, and C-terminus of the other receptor (designated P2X2-3 and P2X3-2, respectively). These clones were stably transfected into 1321N1 astrocytoma cells for biophysical and pharmacological experiments using both electrophysiological and calcium-imaging methods. (3) Chimeric P2X2-3 and P2X3-2 receptors were inwardly rectifying and agonist responses showed desensitization properties similar to the wild-type human P2X2a and P2X3 receptors, respectively. (4) The P2X2-3 chimera displayed an agonist pharmacological profile similar to the P2X3 wild-type receptor being activated by low concentrations of both ATP and alpha,beta-meATP. In contrast, the P2X3-2 chimera had markedly reduced sensitivity to both agonists. (5) The P2X3 receptor antagonists TNP-ATP and A-317491 were shown to be potent, competitive antagonists of the P2X2-3 chimera (Ki=2.2 and 52.1 nm, respectively), supporting the hypothesis that rapid receptor desensitization can mask the competitive antagonism of wild-type homomeric P2X3 receptors. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 1 |
| Volume Number | 140 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 2003-09-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Adenosine Triphosphate Analogs & Derivatives Pharmacology Phenols Polycyclic Compounds Purinergic P2 Receptor Antagonists Receptors, Purinergic P2 Metabolism Chemistry Binding, Competitive Drug Effects Physiology Cell Line, Tumor Dose-Response Relationship, Drug Purinergic P2 Receptor Agonists Receptors, Purinergic P2X3 Comparative Study |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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