Synthesis and activity of substituted carbamates as potentiators of the alpha4beta2 nicotinic acetylcholine receptor

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 m...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-10, Vol.18 (20), p.5643-5647
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholine - chemistry Calcium - chemistry Carbamates - chemistry Chemistry, Pharmaceutical - methods Drug Design Humans Models, Chemical Nervous System - metabolism Neurons - metabolism Patch-Clamp Techniques Pyrazoles - chemistry Pyridines - chemistry Receptors, Nicotinic - chemistry Receptors, Nicotinic - metabolism Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2008.08.092