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

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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Bibliographic Details
Main Author: Boshi Huang (3080169) (author)
Other Authors: 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)
Published: 2024
Subjects:
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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