| Autor: |
William H. Bunnelle, Tino Dyhring, Jens Halvard Grønlien, David J. Anderson, Peter Curzon, John Malysz, Gunnar M. Olsen, Kirsten Thorin-Hagene, Clark A. Briggs, Paige Kerr, Hilde Ween, Murali Gopalakrishnan, Daniel B. Timmermann, Dan Peters |
| Rok vydání: |
2009 |
| Předmět: |
|
| Zdroj: |
British Journal of Pharmacology. 158:1486-1494 |
| ISSN: |
0007-1188 |
| DOI: |
10.1111/j.1476-5381.2009.00426.x |
| Popis: |
Background and purpose: Several agonists of the α7 nicotinic acetylcholine receptor (nAChR) have been developed for treatment of cognitive deficits. However, agonist efficacy in vivo is difficult to reconcile with rapid α7 nAChR desensitization in vitro; and furthermore, the correlation between in vitro receptor efficacy and in vivo behavioural efficacy is not well delineated. The possibility that agonists of this receptor actually function in vivo as inhibitors via desensitization has not been finally resolved. Experimental approach: Two structurally related α7 nAChR agonists were characterized and used to assess the degree of efficacy required in a behavioural paradigm. Key results: NS6784 activated human and rat α7 nAChR with EC50s of 0.72 and 0.88 µM, and apparent efficacies of 77 and 97% respectively. NS6740, in contrast, displayed little efficacy at α7 nAChR ( |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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