Cayman Dimebolin

Dimebolin is a neuroprotective agent.^,, It binds to histamine H₁ and H₂ receptors (IC₅₀s = 3.8 and 287 nM, respectively), as well as α_1A-, α_1B-, α_1D-, and α_2A-adrenergic receptors (ARs), imidazoline I₂ receptors, and the serotonin (5-HT) receptor subtypes 5-HT_2A, 5-HT_2C, 5-HT₆, and 5-HT₇ (K_is = 8-313 nM). It also inhibits NMDA-evoked currents and voltage-gated calcium channels in mouse primary striatal neurons (IC₅₀s = 10 and 50 μM, respectively). 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. ) in cerebellar granule cells when used at a concentration of 25 μM. 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).

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