Coluracetam

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Coluracetam
Coluracetam.svg
Coluracetam3d.png
Systematic (IUPAC) name
N-(2,3-Dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxo-1-pyrrolidinyl)acetamide
Identifiers
CAS Number 135463-81-9
ATC code None
PubChem CID: 214346
ChemSpider 185836
Chemical data
Formula C19H23N3O3
Molecular mass 341.404 g/mol
  • Cc1c(oc2c1c(c3c(n2)CCCC3)NC(=O)CN4CCCC4=O)C
  • InChI=1S/C19H23N3O3/c1-11-12(2)25-19-17(11)18(13-6-3-4-7-14(13)20-19)21-15(23)10-22-9-5-8-16(22)24/h3-10H2,1-2H3,(H,20,21,23)
  • Key:PSPGQHXMUKWNDI-UHFFFAOYSA-N

Coluracetam (INN) (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family.[1] It 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 depressive disorder (MDD), which was preceded by being awarded a "Qualifying Therapeutic Discovery Program Grant" by the state of California.[2] Findings from phase IIa clinical trials have suggested that it would be a potential medication for comorbid MDD with generalized anxiety disorder (GAD).[3] BrainCells Inc is currently[when?] out-licensing the drug for this purpose.[4][full citation needed] It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.[medical citation needed]

Coluracetam has been shown to reverse the loss of choline acetyltransferase production in the medial septal nucleus of rats exposed to phencyclidine (PCP), and is considered a potential therapeutic drug for schizophrenia.[5]

Mechanism of action

Coluracetam enhances high-affinity choline uptake (HACU),[6] 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 in cholinergic neurotoxin-treated rats by changing the choline transporter regulation system.[7]

See also

References

  1. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ Qualifying Therapeutic Discovery Project Grants for the State of California, IRS.gov.
  3. ↑ BrainCells Inc. Announces Results From Exploratory Phase 2a Trial of BCI-540 Archived November 21, 2011 at the Wayback Machine
  4. ↑ [Pipeline,BCI-540], BCI-540 (coluracetam).
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  7. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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