Designing Calcium Release Channel Inhibitors with Enhanced Electron Donor Properties: Stabilizing the Closed State of Ryanodine Receptor Type 1

New drugs with enhanced electron donor properties that target the ryanodine receptor from skeletal muscle sarcoplasmic reticulum (RyR1) are shown to be potent inhibitors of single-channel activity. In this article, we synthesize derivatives of the channel activator 4-chloro-3-methyl phenol (4-CmC) a...

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Veröffentlicht in:	Molecular pharmacology 2012-01, Vol.81 (1), p.53-62
Hauptverfasser:	Ye, Yanping, Yaeger, Daniel, Owen, Laura J., Escobedo, Jorge O., Wang, Jialu, Singer, Jeffrey D., Strongin, Robert M., Abramson, Jonathan J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Calcium Channel Blockers - chemical synthesis Calcium Channel Blockers - metabolism Calcium Channel Blockers - pharmacology Calcium Channels - chemical synthesis Calcium Channels - metabolism Calcium Signaling - drug effects Calcium Signaling - physiology Drug Discovery - methods Electron Transport - physiology Muscle, Skeletal - cytology Muscle, Skeletal - metabolism Muscle, Skeletal - physiology Protein Stability - drug effects Rabbits Ryanodine Receptor Calcium Release Channel - chemical synthesis Ryanodine Receptor Calcium Release Channel - metabolism Thiazepines - chemistry Thiazepines - metabolism
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