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Convallatoxin Enhance the Ligand-Induced Mu-Opioid Receptor Endocytosis and Attenuate Morphine Antinociceptive Tolerance in Mice

Convallatoxin Enhance the Ligand-Induced Mu-Opioid Receptor Endocytosis and Attenuate Morphine Antinociceptive Tolerance in Mice

Po-Kuan Chao, Hsiao-Fu Chang, Li-Chin Ou, Jian-Ying Chuang, Pin-Tse Lee, Wan-Ting Chang, Shu-Chun Chen, Shau-Hua Ueng, John Tsu-An Hsu, Pao-Luh Tao, Ping-Yee Law, Horace H Loh, Shiu-Hwa Yeh

Sci Rep. 2019 Feb 20;9(1):2405.

PMID: 30787373

Abstract:

Morphine is a unique opioid analgesic that activates the mu-opioid receptor (MOR) without efficiently promoting its endocytosis that may underlie side effects. Our objective was to discover a novel enhancer of ligand-induced MOR endocytosis and determine its effects on analgesia, tolerance and dependence. We used high-throughput screening to identify convallatoxin as an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Treatment of cells with convallatoxin enhanced morphine-induced MOR endocytosis through an adaptor protein 2 (AP2)/clathrin-dependent mechanism, attenuated morphine-induced phosphorylation of MOR, and diminished desensitization of membrane hyperpolarization. Furthermore, co-treatment with chronic convallatoxin reduced morphine tolerance in animal models of acute thermal pain and chronic inflammatory pain. Acute convallatoxin administration reversed morphine tolerance and dependence in morphine-tolerant mice. These findings suggest convallatoxin are potentially therapeutic for morphine side effects and open a new avenue to study MOR trafficking.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP508758	Convallatoxin		508-75-8	Price

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