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.

Coluracetam has been shown to reverse the loss of choline acetyltransferase production in the medial septal nucleus of rats exposed to PCP, and is considered a potential therapeutic drug for schizophrenia.[6]

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.[7]

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. ^ Shirayama, Y; Yamamoto, A; Nishimura, T; Katayama, S; Kawahara, R (2007). "Subsequent exposure to the choline uptake enhancer MKC-231 antagonizes phencyclidine-induced behavioral deficits and reduction in septal cholinergic neurons in rats". European Neuropsychopharmacology 17 (9): 616–26. doi:10.1016/j.euroneuro.2007.02.011. PMID 17467960.  edit
  7. ^ MKC-231, a choline-uptake enhancer: long-lasting cognitive improvement after repeated administration in AF64A-treated rats., Pubmed.