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

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

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...

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Bibliographic Details
Main Authors: Irina V. Shelukhina, Maxim N. Zhmak, Alexander V. Lobanov, Igor A. Ivanov, Alexandra I. Garifulina, Irina N. Kravchenko, Ekaterina A. Rasskazova, Margarita A. Salmova, Elena A. Tukhovskaya, Vladimir A. Rykov, Gulsara A. Slashcheva, Natalya S. Egorova, Inessa S. Muzyka, Victor I. Tsetlin, Yuri N. Utkin
Format: Article
Language:English
Published: MDPI AG 2018-01-01
Series:Toxins
Subjects:
nicotinic acetylcholine receptor
azemiopsin
preclinical studies
toxicity
pharmacokinetics
myorelaxant
Key Contribution
Investigation of the preclinical profile of azemiopsin demonstrated its high affinity and specificity for muscle type nicotinic acetylcholine receptor as well as good muscle relaxant capacity. Toxicology studies in mice indicated that azemiopsin was well tolerated during chronic dosing and showed no immunotoxicity, allergenic or mutagenic activity, which made it a good candidate for application as a local muscle relaxant.
Online Access:http://www.mdpi.com/2072-6651/10/1/34

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http://www.mdpi.com/2072-6651/10/1/34

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