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Discovery and Optimization of Highly Potent and Selective AT2R Antagonists to Relieve Peripheral Neuropathic Pain.


ABSTRACT: The angiotensin II type 2 receptor (AT2R) has attracted much attention as a potential target for the relief of neuropathic pain, which represents an area of unmet clinical need. A series of 1,2,3,4-tetrahydroisoquinolines with a benzoxazole side-chain were discovered as potent AT2R antagonists. Rational optimization resulted in compound 15, which demonstrated both excellent antagonistic activity against AT2R in vitro and analgesic efficacy in a rat chronic constriction injury model. Its favorable physicochemical properties and oral bioavailability make it a promising therapeutic candidate for neuropathic pain.

SUBMITTER: Guo Y 

PROVIDER: S-EPMC8210434 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature

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Discovery and Optimization of Highly Potent and Selective AT<sub>2</sub>R Antagonists to Relieve Peripheral Neuropathic Pain.

Guo Yanghui Y   Huang Xiangui X   Liao Weiwei W   Meng Lichen L   Xu Daiwang D   Ye Cheng C   Chen Lei L   Hu Taishan T  

ACS omega 20210528 23


The angiotensin II type 2 receptor (AT<sub>2</sub>R) has attracted much attention as a potential target for the relief of neuropathic pain, which represents an area of unmet clinical need. A series of 1,2,3,4-tetrahydroisoquinolines with a benzoxazole side-chain were discovered as potent AT<sub>2</sub>R antagonists. Rational optimization resulted in compound <b>15</b>, which demonstrated both excellent antagonistic activity against AT<sub>2</sub>R <i>in vitro</i> and analgesic efficacy in a rat  ...[more]

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