Discovery of 6α-Thiazolylcarboxamidonaltrexamine Derivative (NTZ) as a Potent and Central Nervous System Penetrant Opioid Receptor Modulator with Drug-like Properties for Potential Treatment of Opioid Use Disorder

The development of highly potent and selective μ opioid receptor (MOR) modulators with favorable drug-like properties has always been a focus in the opioid domain. Our previous efforts led to the discovery of a lead compound designated as NAT, a potent centrally acting MOR modulator. However, the fa...

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المؤلف الرئيسي:	Boshi Huang (3080169) (author)
مؤلفون آخرون:	Hongguang Ma (5105198) (author), Piyusha P. Pagare (4433698) (author), Mengchu Li (8108468) (author), Rolando E. Mendez (12210748) (author), James C. Gillespie (12210745) (author), Justin L. Poklis (4117759) (author), Matthew S. Halquist (1331493) (author), David L. Stevens (1878574) (author), William L. Dewey (306219) (author), Dana E. Selley (1448944) (author), Yan Zhang (8098) (author)
منشور في:	2024
الموضوعات:	Biochemistry Medicine Genetics Neuroscience Pharmacology Biotechnology Immunology Cancer Science Policy Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified previous efforts led alleviating withdrawal symptoms 16 new analogs opioid use disorder favorable admet profile several key drug ntz shows promise like properties suggested lead compound designated 6 </ b like properties vivo </ potential lead opioid domain favorable drug thiophene ring thiazolylcarboxamidonaltrexamine derivative taken together potential treatment nitrogen atom cns permeability antagonistic effect activity cliff
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Discovery of 6α-Thiazolylcarboxamidonaltrexamine Derivative (NTZ) as a Potent and Central Nervous System Penetrant Opioid Receptor Modulator with Drug-like Properties for Potential Treatment of Opioid Use Disorder

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