P2X receptor chimeras highlight roles of the amino terminus to partial agonist efficacy, the carboxyl terminus to recovery from desensitization, and independent regulation of channel transitions

Abstract

Background: P2X receptor subtypes show differences in pharmacology. Results: Chimeric P2X receptors exhibit modified partial agonist action and recovery from desensitization. Conclusion: Interactions among the extracellular, transmembrane, and intracellular regions regulate channel properties. Significance: Agonist binding and transitions to channel opening (efficacy), behavior of the open channel, as well as recovery from desensitization can be controlled independently. © 2013 by The American Society for Biochemistry and Molecular Biology, Inc.