Dimemorfan (INN) (or dimemorphan) (brand names Astomin, Dastosirr, Tusben), or dimemorfan phosphate (JAN), also known as 3,17-dimethylmorphinan, is an antitussive (cough suppressant) of the morphinan family that is widely used in Japan and is also marketed in Spain and Italy.[1][2][3][4] It was developed by Yamanouchi Pharmaceutical (now Astellas Pharma) and introduced in Japan in 1975.[3] It was later introduced in Spain in 1981 and Japan in 1985.[5]
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| Trade names | Astomin, Datosin, Gentus |
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| ECHA InfoCard | 100.048.134 |
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| Formula | C18H25N |
| Molar mass | 255.405 g·mol−1 |
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Side effects
Adverse effects include nausea, somnolence, dry mouth, and decreased appetite.[5]
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).[6][7] 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.[8][9] Similarly to DXM and DXO, dimemorfan has only relatively low affinity for the σ2 receptor (Ki = 4,421 nM).[7]