Ontology highlight
ABSTRACT:
SUBMITTER: Zheng Y
PROVIDER: S-EPMC6344324 | biostudies-literature | 2018 Dec
REPOSITORIES: biostudies-literature
Zheng Yi Y Obeng Samuel S Wang Huiqun H Stevens David L DL Komla Essie E Selley Dana E DE Dewey William L WL Akbarali Hamid I HI Zhang Yan Y
ACS chemical neuroscience 20180723 12
Two 6β- N-heterocyclic naltrexamine derivatives, NAP and NMP, have been identified as peripherally selective mu opioid receptor (MOR) antagonists. To further enhance the peripheral selectivity of both compounds, the 17-amino group and the nitrogen atom of the pyridine ring in both NAP and NMP were methylated to obtain dMNAP and dMNMP, respectively. Compared with NAP and NMP, the binding affinities of dMNAP and dMNMP shifted to MOR and KOR (kappa opioid receptor) dual selective and they acted as ...[more]