Litcius/Paper detail

The β-arrestin-biased β-adrenergic receptor blocker carvedilol enhances skeletal muscle contractility

Ji‐Hee Kim, Chad A. Grotegut, James W. Wisler, Lan Mao, Paul B. Rosenberg, Howard A. Rockman, Robert J. Lefkowitz

2020Proceedings of the National Academy of Sciences42 citationsDOIOpen Access PDF

Abstract

AR, stimulating β-arrestin-dependent but not G protein-dependent signaling. In this study, we investigated whether treatment with carvedilol could enhance skeletal muscle strength via β-arrestin-dependent pathways. In a murine model, we demonstrate chronic treatment with carvedilol, but not other β-blockers, indeed enhances contractile force in skeletal muscle and this is mediated by β-arrestin 1. Interestingly, carvedilol enhanced skeletal muscle contractility despite a lack of effect on skeletal muscle hypertrophy. Our findings suggest a potential unique clinical role of carvedilol to stimulate skeletal muscle contractility while avoiding the adverse effects with βAR agonists. This distinctive signaling profile could present an innovative approach to treating sarcopenia, frailty, and secondary muscle wasting.

Topics & Concepts

CarvedilolContractilitySkeletal muscleAgonistMetoprololArrestinClenbuterolInternal medicineEndocrinologyMuscle hypertrophyAdrenergic agonistMyocytePharmacologyMedicineReceptorHeart failureG protein-coupled receptorPharmacological Effects and AssaysReceptor Mechanisms and SignalingCardiovascular and exercise physiology