[h=1]Coluracetam[/h][TABLE="class: infobox, width: 22"]
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[TD]C[SUB]19[/SUB]H[SUB]23[/SUB]N[SUB]3[/SUB]O[SUB]3[/SUB][/TD]
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[TH="align: left"]Molar mass[/TH]
[TD]341.404 g/mol[/TD]
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Coluracetam (INN) (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family.[SUP][1][/SUP] 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.[SUP][2][/SUP] Findings from phase IIa clinical trials have suggested that it would be a potential medication for comorbidMDD with generalized anxiety disorder (GAD).[SUP][3][/SUP]BrainCells Inc is currently[SUP][when?][/SUP] out-licensing the drug for this purpose.[SUP][4][/SUP][SUP][full citation needed][/SUP] It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.[SUP][medical citation needed][/SUP]
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.[SUP][5][/SUP]
[h=2]Mechanism of action[edit][/h]Coluracetam enhances high-affinity cholineuptake (HACU),[SUP][6][/SUP] 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.[SUP][7][/SUP]
<caption style="font-size: 19.25px; font-weight: bold; padding: 0.2em;">Coluracetam</caption><tbody>[TR]
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[TH="colspan: 2, align: center"]Clinical data[/TH]
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[TH="align: left"]ATC code[/TH]
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- None
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[TH="colspan: 2, align: center"]Identifiers[/TH]
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IUPAC name[show]
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- 135463-81-9
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- 214346
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[TH="align: left"]ChemSpider[/TH]
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- 185836
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[TH="colspan: 2, align: center"]Chemical and physical data[/TH]
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[TH="align: left"]Formula[/TH]
[TD]C[SUB]19[/SUB]H[SUB]23[/SUB]N[SUB]3[/SUB]O[SUB]3[/SUB][/TD]
[/TR]
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[TH="align: left"]Molar mass[/TH]
[TD]341.404 g/mol[/TD]
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[TH="align: left"]3D model (JSmol)[/TH]
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- Interactive image
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SMILES[show]
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InChI[show]
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</tbody>[/TABLE]
Coluracetam (INN) (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family.[SUP][1][/SUP] 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.[SUP][2][/SUP] Findings from phase IIa clinical trials have suggested that it would be a potential medication for comorbidMDD with generalized anxiety disorder (GAD).[SUP][3][/SUP]BrainCells Inc is currently[SUP][when?][/SUP] out-licensing the drug for this purpose.[SUP][4][/SUP][SUP][full citation needed][/SUP] It may also have potential use in prevention and treatment of ischemic retinopathy and retinal and optic nerve injury.[SUP][medical citation needed][/SUP]
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.[SUP][5][/SUP]
[h=2]Mechanism of action[edit][/h]Coluracetam enhances high-affinity cholineuptake (HACU),[SUP][6][/SUP] 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.[SUP][7][/SUP]
