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Synthesis and activity of substituted carbamates as potentiators of the alpha4beta2 nicotinic acetylcholine receptor |
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| Authors: | Springer Stephanie K Woodin Katrina S Berry Virginia Boezio Alessandro A Cao Lei Clarkin Kristie Harmange Jean-Christophe Hierl Markus Knop Johannes Malmberg Annika B McDermott Jeff S Nguyen Hung Q Waldon Daniel Albrecht Brian K McDonough Stefan I |
| Affiliation: | Department of Medicinal Chemistry, Amgen Inc., 1 Kendall Square, Building 1000, Cambridge, MA, USA. stephanie.springer@amgen.com |
| Abstract: | The synthesis and structure-activity relationship of a series of carbamate potentiators of alpha4beta2 nAChR is reported herein. These compounds were highly selective for alpha4beta2 over other nAChR subtypes. In addition, compounds increased the response of alpha4beta2 nAChRs to acetylcholine, as measured with patch-clamp electrophysiology. |
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