Structural comparisons of meptazinol with opioid analgesics.
OBJECTIVE
To investigate the mechanism of action of a potent analgesic, (+/-)-meptazinol.


METHODS
The structures of meptazinol enantiomers were compared with opioid pharmacophore and tramadol.


RESULTS
Neither enantiomer of meptazinol fitted any patterns among the opioid pharmacophore and tramadol, although they did share some structural and pharmacological similarities. However, the structure superpositions implied that both enantiomers of meptazinol might share some similar analgesic mechanisms with typical opiate analgesics.


CONCLUSIONS
Meptazinol should have a different mechanism of action to known analgesics, which would be helpful in further investigations of meptazinol in the search for non-addictive analgesics.
Li
Wei
W
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China.
Hao
Jing-lai
JL
Tang
Yun
Y
Chen
Yan
Y
Qiu
Zhui-bai
ZB
D000701:Analgesics, Opioid / Q000737:chemistry* / Q000494:pharmacology; D008621:Meptazinol / Q000737:chemistry* / Q000494:pharmacology; D008968:Molecular Conformation; D015394:Molecular Structure; D009020:Morphine / Q000737:chemistry / Q000494:pharmacology; D021281:Quantitative Structure-Activity Relationship; D013237:Stereoisomerism; D014147:Tramadol / Q000737:chemistry / Q000494:pharmacology
D000701:Analgesics, Opioid; D008621:Meptazinol; D014147:Tramadol; D009020:Morphine