Coluracetam
| Coluracetam[1] | |
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N-(2,3-dimethyl-5,6,7,8- tetrahydrofuro[2,3-b] quinolin-4-yl)-2- (2-oxopyrrolidin-1-yl)acetamide |
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| Identifiers | |
| CAS number | 135463-81-9  |
| PubChem | 214346 |
| ChemSpider | 185836 |
| ChEMBL | CHEMBL37935 |
| Jmol-3D images | Image 1 Image 2 |
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| Properties | |
| Molecular formula | C19H23N3O3 |
| Molar mass | 341.4 g mol−1 |
| Pharmacology | |
| Routes of administration |
Oral |
 (verify) (what is:  / ?)Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) |
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| Infobox references |
Coluracetam (BCI-540) is a nootropic drug of the racetam family.[2] Coluracetam (formerly known as MKC-231) was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depression disorder (MDD), after being awarded a "Qualifying Therapeutic Discovery Program Grant" by the state of California.[3] Findings from its Phase 2a clinical trials have suggested that it would be an ideal medication for co-morbid MDD with generalized anxiety disorder (GAD).[4] BrainCells Inc is currently out-licensing the drug for this purpose.[5] It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.
[edit] Mechanism of Action
Coluracetam enhances high-affinity choline uptake (HACU) which is the rate-limiting step of acetylcholine (ACh) synthesis, and is the only known choline uptake enhancer to currently exist. Studies have shown Coluracetam to improve learning impairment on a single oral dose given to rats which have been exposed to cholinergic neurotoxins. Subsequent studies have shown that it may induce long-lasting procognitive effects by changing the choline transporter regulation system.[6]
[edit] See also
[edit] References
- ^ Coluracetam - Compound Summary, PubChem.
- ^ Bessho, T; Takashina, K; Tabata, R; Ohshima, C; Chaki, H; Yamabe, H; Egawa, M; Tobe, A et al. (1996). "Effect of the novel high affinity choline uptake enhancer 2-(2-oxopyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro2,3-b quinolin-4-yl)acetoamide on deficits of water maze learning in rats". Arzneimittel-Forschung 46 (4): 369–73. PMID 8740080.
- ^ Qualifying Therapeutic Discovery Project Grants for the State of California, IRS.gov.
- ^ BrainCells Inc. Announces Results From Exploratory Phase 2a Trial of BCI-540
- ^ Pipeline,BCI-540, BCI-540 (coluracetam).
- ^ MKC-231, a choline-uptake enhancer: long-lasting cognitive improvement after repeated administration in AF64A-treated rats., Pubmed.
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