The chiral opioid analgesic tramadol was patented (1962) as a cis- and trans-racemates mixture. A first chiral switch led to the (+/-)-cis-(1RS,2RS) racemate, patented and approved as Tramal (1980), preferred over the (+)-cis-(1R,2R)-enantiomer. Consecutive chiral switches of (+/-)-cis-tramadol to (+)-cis-(1R,2R)-tramadol/salts were patented. This Viewpoint calls for developing (+)-cis-(1R,2R)-tramadol medicines and recognizing tramadol medicines as potential psychedelics to overcome the spreading tramadol crisis.
Chiral switches of tramadol hydrochloride, a potential psychedelic drug. Past and future / Agranat, Israel; D'Acquarica, Ilaria. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - (2024). [10.1021/acsmedchemlett.4c00322]
Chiral switches of tramadol hydrochloride, a potential psychedelic drug. Past and future
D'Acquarica, Ilaria
2024
Abstract
The chiral opioid analgesic tramadol was patented (1962) as a cis- and trans-racemates mixture. A first chiral switch led to the (+/-)-cis-(1RS,2RS) racemate, patented and approved as Tramal (1980), preferred over the (+)-cis-(1R,2R)-enantiomer. Consecutive chiral switches of (+/-)-cis-tramadol to (+)-cis-(1R,2R)-tramadol/salts were patented. This Viewpoint calls for developing (+)-cis-(1R,2R)-tramadol medicines and recognizing tramadol medicines as potential psychedelics to overcome the spreading tramadol crisis.| File | Dimensione | Formato | |
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