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Dimemorfan
Cough suppressant
Cough suppressant
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Dimemorfan (INN; JAN dimemorfan phosphate; also known as dimemorphan and 3,17-dimethylmorphinan; brand names Astomin, Dastosirr, and Tusben) is an antitussive (cough suppressant) of the morphinan family that is widely used in Japan and is also marketed in Spain and Italy. It was developed by Yamanouchi Pharmaceutical (now Astellas Pharma) and introduced in Japan in 1975. It was later introduced in Spain in 1981 and Japan in 1985.
Side effects
Adverse effects include nausea, somnolence, dry mouth, and decreased appetite.
Pharmacology
Dimemorfan is an analogue of dextromethorphan (DXM) and its active metabolite dextrorphan (DXO), and similarly to them, acts as a potent agonist of the σ1 receptor (Ki = 151 nM). However, unlike DXM and DXO, it does not act significantly as an NMDA receptor antagonist (Ki = 16,978 nM), and for this reason, lacks dissociative effects, thereby having reduced side effects and abuse potential in comparison. Similarly to DXM and DXO, dimemorfan has only relatively low affinity for the σ2 receptor (Ki = 4,421 nM).
References
References
- (14 November 2014). "The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies". Springer.
- (15 January 2015). "Textbook of Palliative Medicine and Supportive Care, Second Edition". CRC Press.
- (1997). "The nonnarcotic antitussive drug dimemorfan: a review". Clinical Therapeutics.
- (1 January 2005). "Lexi-Comp's Drug Information Handbook International: With Canadian and International Drug Monographs". Lexi-Comp.
- (1991). "Drugs Available Abroad, 1st Edition". Derwent Publications Ltd..
- (November 2009). "The pharmacology of sigma-1 receptors". Pharmacology & Therapeutics.
- (20 April 2012). "Therapeutic Targets: Modulation, Inhibition, and Activation". John Wiley & Sons.
- (March 1999). "Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan". Brain Research.
- (April 2005). "The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan". British Journal of Pharmacology.
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