Xorphanol (INN) (developmental code name TR-5379 or TR-5379M), also known as xorphanol mesylate (USAN), is an opioidanalgesic of the morphinan family that was never marketed.[1][2][3]
Xorphanol produces potent analgesia, and was originally claimed to possess a minimal potential for dependence or abuse.[12][13][14] Moreover, side effects in animal studies were relatively mild, with only sedation and nausea being prominent, although it also produced convulsions at the highest dose tested.[15] However, human trials revealed additional side effects such as headaches and euphoria, and this was the subject of a lawsuit between the drug's inventors and the company to which they had licensed the marketing rights, which claimed that these side effects had not been revealed to them during the license negotiations.[16] As a result of this dispute, the drug was never marketed commercially.
^Cowan A, Zhu XZ, Mosberg HI, Porreca F (1986). "Central infusion of rats with agents selective for different types of opioid receptor". NIDA Research Monograph. 67: 132–7. PMID3018570.
^Howes JF, Villarreal JE, Harris LS, Essigmann EM, Cowan A (February 1985). "Xorphanol". Drug and Alcohol Dependence. 14 (3–4): 373–80. doi:10.1016/0376-8716(85)90068-7. PMID4039650.
^Porter MC, Hartnagel RE, Clemens GR, Kowalski RL, Bare JJ, Halliwell WE, Kitchen DN (1983). "Preclinical toxicity and teratogenicity studies with the narcotic antagonist analgesic drug TR5379M". Fundamental and Applied Toxicology. 3 (5): 478–82. doi:10.1016/S0272-0590(83)80023-2. PMID6642105.
