Isolation, identification and synthesis of a metabolite of tazadolene succinate.
Metabolism of tazadolene (1), a novel non-opioid analgesic with antidepressant properties, affords the 4-hydroxy and 3-methoxy-4-hydroxy derivatives (phenyl ring) of the drug, and N-[2-(phenylmethylene)cyclohexyl]-beta-alanine (4). The isolation, identification and synthesis of the latter metabolite is described.
D000700:Analgesics / Q000138:chemical synthesis / Q000378:metabolism*; D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000378:metabolism*; D001384:Azetidines / Q000138:chemical synthesis / Q000378:metabolism*; D001385:Azetines / Q000378:metabolism*; D001711:Biotransformation; D055598:Chemical Phenomena; D002621:Chemistry; D004285:Dogs; D008401:Gas Chromatography-Mass Spectrometry; D008297:Male; D051379:Mice; D011817:Rabbits; D051381:Rats
D000700:Analgesics; D000928:Antidepressive Agents; D001384:Azetidines; D001385:Azetines; C048351:tazadolene succinate