Azemiopsin, a Selective Peptide Antagonist of Muscle Nicotinic Acetylcholine Receptor: Preclinical Evaluation as a Local Muscle Relaxant.

ABSTRACT: Azemiopsin (Az), a linear peptide from the Azemiops feae viper venom, contains no disulfide bonds, is a high-affinity and selective inhibitor of nicotinic acetylcholine receptor (nAChR) of muscle type and may be considered as potentially applicable nondepolarizing muscle relaxant. In this study, we investigated its preclinical profile in regard to in vitro and in vivo efficacy, acute and chronic toxicity, pharmacokinetics, allergenic capacity, immunotoxicity and mutagenic potency. The peptide effectively inhibited (IC₅₀ ~ 19 nM) calcium response of muscle nAChR evoked by 30 μM (EC₁₀₀) acetylcholine but was less potent (IC₅₀ ~ 3 μM) at α7 nAChR activated by 10 μM (EC₅₀) acetylcholine and had a low affinity to α4β2 and α3-containing nAChR, a

SUBMITTER: Shelukhina IV 

PROVIDER: S-EPMC5793121 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature