Propofol binds and inhibits skeletal muscle ryanodine receptor 1.

ABSTRACT:

Background

As the primary Ca²⁺ release channel in skeletal muscle sarcoplasmic reticulum (SR), mutations in type 1 ryanodine receptor (RyR1) or its binding partners underlie a constellation of muscle disorders, including malignant hyperthermia (MH). In patients with MH mutations, triggering agents including halogenated volatile anaesthetics bias RyR1 to an open state resulting in uncontrolled Ca²⁺ release, increased sarcomere tension, and heat production. Propofol does not trigger MH and is commonly used for patients at risk of MH. The atomic-level interactions of any anaesthetic with RyR1 are unknown.

Methods

RyR1 opening was measured by [³H]ryanodine binding in heavy SR vesicles (wild type) and single-channel recordings of MH mutant R615C R

SUBMITTER: Joseph TT 

PROVIDER: S-EPMC11488158 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature