Coluracetam

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Coluracetam[1]
Coluracetam.svg Coluracetam3d.png
Identifiers
CAS number 135463-81-9 YesY
PubChem 214346
ChemSpider 185836 YesY
ChEMBL CHEMBL37935 YesY
Jmol-3D images Image 1
Image 2
Properties
Molecular formula C19H23N3O3
Molar mass 341.40 g mol−1
Pharmacology
Routes of
administration
Oral
Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
 YesY (verify) (what is: YesY/N?)
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.

Mechanism of Action[edit]

Coluracetam enhances high-affinity choline uptake which is the rate-limiting step of acetylcholine (ACh) synthesis. 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]

See also[edit]

References[edit]

  1. ^ Coluracetam - Compound Summary, PubChem.
  2. ^ Bessho, T; Takashina, K; Tabata, R; Ohshima, C; Chaki, H; Yamabe, H; Egawa, M; Tobe, A; Saito, K (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. 
  3. ^ Qualifying Therapeutic Discovery Project Grants for the State of California, IRS.gov.
  4. ^ BrainCells Inc. Announces Results From Exploratory Phase 2a Trial of BCI-540
  5. ^ [Pipeline,BCI-540], BCI-540 (coluracetam).
  6. ^ MKC-231, a choline-uptake enhancer: long-lasting cognitive improvement after repeated administration in AF64A-treated rats., Pubmed.