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Dimebon + dextromethorphan
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dimebon + dextromethorphan is a combination of two small molecule drugs. Dimebon (also known as latrepirdine) is an antihistamine originally used in Russia for allergic rhinitis and later investigated for neurodegenerative diseases such as Alzheimer's disease. Its mechanism of action is pleiotropic and not fully established but includes antagonism at the Histamine H1 receptor, inhibition of N-methyl-D-aspartate receptor, low-affinity inhibition of L-type voltage-gated calcium channel, and Acetylcholinesterase inhibition[6][8]. Dextromethorphan is a cough suppressant widely used in over-the-counter medications; it acts primarily as an N-methyl-D-aspartate receptor antagonist and Sigma-1 receptor agonist with additional activity as a nonselective Serotonin transporter (SERT) inhibitor and α3/β4 nicotinic acetylcholine receptor antagonist[2][5]. The combination has not been approved or widely studied together for any specific indication.
- Brand names
- Robitussin
- Other names
- DimebonLatrepirdineDMDXM
02
Targets
AcetylcholinesteraseHRH1 (Histamine H1 Receptor)LTCC (Voltage-gated calcium channel (L-type))NMDAR (Glutamate receptor ionotropic, NMDA)SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)Nicotinic Acetylcholine Receptor
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