Coluracetam(MKC-231) is a new choline uptake enhancer. IC50 value: Target: in vitro: MKC-231 (10(-10)-10(-6) moll) significantly increased high affinity choline uptake (HACU) when it was incubated with the hippocampal synaptosomes of ethylcholine mustard aziridinium ion (AF64A) treated rats, but not of normal rats. MKC-231 did not affect theAChEactivity, [3H]- quinuclidinyl benzilate binding, and [3H]-pirenzepine binding [1]. in vivo: Oral administration of MKC-231 (1-10 mg/kg) significantly improved the learning deficits in the Morris' water maze of AF64A-treated rats, but it did not produce any significant side effects, like tremor, salivation or hypothermia, which were observed in rats treated with high doses of tacrine [1]. In acute behavioral experiments, MKC-231 and THA had no significant effect on AF64A-induced memory deficits at any doses tested (0.3, 1.0 and 3.0 mg/kg), whereas Dup 996, at a dose of 1.0 mg/kg, significantly improved memory deficits. In chronic experiments, MKC-231 improved memory deficit at all doses tested (0.3, 1.0, or 3.0 mg/kg p.o., once daily for 11 days) and Dup 996 did so only at a dose of 3.0 mg/kg, whereas THA did not improve memory deficit at any doses tested [2].

341.40

Solid

C₁₉H₂₃N₃O₃

135463-81-9

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 20 mg/mL(58.58 mM)

H₂O : 0.4 mg/mL(1.17 mM;Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

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