Discovery of Potent and Selective Transient Receptor Potential Vanilloid 1 (TRPV1) Agonists with Analgesic Effects <i>In Vivo</i> Based on the Functional Conversion Induced by Altering the Orientation of the Indazole Core-Reference-Cited by-同舟云学术

Discovery of Potent and Selective Transient Receptor Potential Vanilloid 1 (TRPV1) Agonists with Analgesic Effects In Vivo Based on the Functional Conversion Induced by Altering the Orientation of the Indazole Core

Published:2022-08-25 Issue:17 Volume:65 Page:11658-11678
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Liang Qianqian¹^ORCID,Qiao Zhen¹,Zhou Qiqi²^ORCID,Xue Dengqi¹³,Wang KeWei⁴⁵,Shao Liming¹³^ORCID

Affiliation:

1. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China

2. Department of Pharmacology, Qilu Medical University, Zibo, Shandong 255300, China

3. State Key Laboratory of Medical Neurobiology, Fudan University, 138 Yixueyuan Road, Shanghai 200032, China

4. Departments of Pharmacology, School of Pharmacy, Qingdao University Medical College, #1 Ningde Road, Qingdao 266073, China

5. Institute of Innovative Drug Discovery, Qingdao University, 38 Dengzhou Road, Qingdao 266021, China

Funder

Ministry of Science and Technology of the People's Republic of China

Science and Technology Commission of Shanghai Municipality

National Natural Science Foundation of China

Natural Science Foundation of Shandong Province

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.2c00469

Reference46 articles.

1. TRP Channels and Pain

2. TRP ION CHANNELS AND TEMPERATURE SENSATION

3. The Cloned Capsaicin Receptor Integrates Multiple Pain-Producing Stimuli

4. An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors

5. Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide

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