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Dimebolin is a neuroprotective agent.1,2,3 It binds to histamine H1 and H2 receptors (IC50s = 3.8 and 287 nM, respectively), as well as α1A-, α1B-, α1D-, and α2A-adrenergic receptors (ARs), imidazoline I2 receptors, and the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 (Kis = 8-313 nM).4 It also inhibits NMDA-evoked currents and voltage-gated calcium channels in mouse primary striatal neurons (IC50s = 10 and 50 μM, respectively).1 Dimebolin (50 μM) inhibits glutamate-induced apoptosis in primary striatal neurons derived from the YAC128 transgenic mouse model of Huntington’s disease. It inhibits cell death induced by amyloid-β (25-35) (Item No. 24155) in cerebellar granule cells when used at a concentration of 25 μM.2 Dimebolin (1 mg/kg) inhibits decreases in two-way active avoidance reaction (TWAA) acquisition in a rat model of Alzheimer’s disease induced by 1-ethyl-1-(2-hydroxyethyl) aziridinium (AF64A).3
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1. Evaluation of dimebon in cellular model of Huntington’s disease. Mol. Neurodegener. 3, 15 (2008).
2. Dimebon and tacrine inhibit neurotoxic action of β-
3. Dimebon improves learning in animals with experimental Alzheimer’s disease. B. Exp. Biol. Med. 129(6), 640-642 (2000).
4. From anti-