Coluracetam CAS 135463-81-9

Coluracetam CAS 135463-81-9
CAS No.: 135463-81-9
Molecular Formula: C19H23N3O3
Molecular Weight: 341.40
Target: iGluR
Pathway: Membrane Transporter/Ion Channel; Neuronal Signaling
Solubility: DMSO : ≥ 20 mg/mL (58.58 mM); H2O : 0.4 mg/mL (1.17 mM;
Need ultrasonic and warming

BIOLOGICAL ACTIVITY:
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 the AChE activity, [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].
References:
[1]. Bessho T, et al. Effect of the novel high affinity choline uptake enhancer 2-(2-oxopyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b] quinolin-4-
yl)acetoamide on deficits of water maze learning in rats. Arzneimittelforschung. 1996 Apr;46(4):369-73.
[2]. Murai S, et al. MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by
ethylcholine aziridinium ion in mice. J Neural Transm Gen Sect. 1994;98(1):1-13.
CAIndexNames:
1-Pyrrolidineacetamide, 2-oxo-N-(5,6,7,8-tetrahydro-2,3-dimethylfuro[2,3-b]quinolin-4-yl)-
SMILES:
O=C(NC1=C2C(OC(C)=C2C)=NC3=C1CCCC3)CN4C(CCC4)=O

Caution: Product has not been fully validated for medical applications. For research use only.

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