Synonyms: Dimebolin, Latrepirdine, Pf-01913539
Chemical Name: 3,6-dimethyl-9-(2-methyl-pyridyl-5)-ethyl-1,2,3,4-tetrahydro-γ-carboline dihydrochloride
Therapy Type: Small Molecule
Target Type: Unknown
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Inactive)
Company: Medivation, Inc.
Approved for: Anti-histamine use in Russia
Dimebon is an antihistamine compound with a long history of clinical use in Russia.
Dimebon has been reported to modulate the activity of a variety of channels and neurotransmitter systems, including L-type calcium channels (Lermontova et al., 2001), AMPA and NMDA glutamate receptors (Grigorev et al., 2003), α-adrenergic receptors (α1A, α1B, α1D, and α2A), histamine H1 and H2 receptors and serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors (Wu et al., 2008). Dimebon also has been proposed to exert neuroprotective effects by blocking mitochondrial permeability transition pores (Bachurin et al., 2003).
- Lermontova NN, Redkozubov AE, Shevtsova EF, Serkova TP, Kireeva EG, Bachurin SO. Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca(2+) channels. Bull Exp Biol Med. 2001 Nov;132(5):1079-83. PubMed.
- Grigorev VV, Dranyi OA, Bachurin SO. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med. 2003 Nov;136(5):474-7. PubMed.
- Wu J, Li Q, Bezprozvanny I. Evaluation of Dimebon in cellular model of Huntington's disease. Mol Neurodegener. 2008 Oct 21;3 PubMed.
- Bachurin SO, Shevtsova EP, Kireeva EG, Oxenkrug GF, Sablin SO. Mitochondria as a target for neurotoxins and neuroprotective agents. Ann N Y Acad Sci. 2003 May;993:334-44; discussion 345-9. PubMed.
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