Thiorphan is a enkephalinase (CD10) and metalloproteinase (MMP) inhibitor that displays antinociceptive activity. The compound can inhibit neutral endopeptidase CD10 and has antiapoptotic and proliferative protective effects. Research shows that thiorphan has the ability to block the degradation of the luteinizing hormone releasing hormone (LHRH). At higher concentrations, (14 μM) this compound has been shown to inhibit the activity of angiotensin-converting enzyme (ACE).
1. Roques, B.P., et al. 1980. Nature. 288: 286-288. PMID: 7001254 2. Reche, I., et al. 1998. Neuropharmacology. 37: 215-222. PMID: 9680246 3. Yang, X., et al. 1998. Pharm. Res. 15: 1480-1484. PMID: 9755904 4. Eriksson, U., et al. 2005. J. Biotechnol. 119: 76-86. PMID: 16046243 5. Amantini, C., et al. 2008. J. Pharmacol. Exp. Ther. 327: 215-225. PMID: 18621988
Soluble in ethanol (50 mg/ml), a mixture of methanol , chloroform (1:1) (50 mg/ml), DMSO, and methanol. Insoluble in water.
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Eriksson et alEriksson et al. (PubMed ID 16046243) used thiorphan (DL) to inactivate metalloproteinase activity involved in autocrine regulation of Trichoplusia ni cell proliferation. -SCBT Publication Review
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