Drug intelligence / Profile preview

dimethoxanate

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Dimethoxanate is a small molecule drug of the phenothiazine class used as a cough suppressant. It was introduced in several European countries in the early to mid-20th century and marketed under various brand names. Its primary mechanism of action is believed to involve binding to the sigma-1 receptor in the brain (IC50 = 41 nM), which may contribute to its antitussive effects. In addition to suppressing cough, dimethoxanate may have analgesic, local anesthetic, and central nervous system depressant properties but can also cause side effects such as nausea and vomiting. The drug was withdrawn from the US market by the FDA in 1975 due to insufficient evidence of efficacy[1][3][5].

Brand names
CotheraCotraneAtussPerlatossTossizid
Other names
DimetoxanatoDimethoxanatum
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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