Coluracetam (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

; development code BCI-540; formerly MKC-231) is a purported nootropic

agent Agent may refer to: Espionage, investigation, and law *, spies or intelligence officers * Law of agency, laws involving a person authorized to act on behalf of another ** Agent of record, a person with a contractual agreement with an insuranc ...

of the racetam family. It is contains a chemical group that is a bioisostere of the 9-amino-tetrahydroacridine family. It was initially developed and tested by the

Mitsubishi Tanabe Pharma Corporation Mitsubishi Tanabe Pharma Corporation is a Japanese pharmaceuticals company from Osaka, a subsidiary of Mitsubishi Chemical Holdings Corporation. was formed in 2001 from the merger of Mitsubishi-Tokyo Pharmaceuticals and Welfide Corporation. On ...

for

Alzheimer's disease Alzheimer's disease (AD) is a neurodegeneration, neurodegenerative disease that usually starts slowly and progressively worsens. It is the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in short-term me ...

. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into

major depressive disorder Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Introdu ...

(MDD), which was preceded by being awarded a "Qualifying Therapeutic Discovery Program Grant" by the state of California.Qualifying

Therapeutic Discovery Project">Qualifying Therapeutic Discovery Project
Grants for the State of California IRS.gov. Findings from Phases of clinical research#Phase II">phase IIa The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phase ...

clinical trials have suggested that it would be a potential medication for comorbidity, comorbid MDD with generalized anxiety disorder (GAD).BrainCells Inc. Announces Results From Exploratory Phase 2a Trial of BCI-540
BrainCells Inc is currently out-licensing the drug for this purpose. ipeline,BCI-540 BCI-540 (coluracetam). It may also have potential use in prevention and treatment of ischemic retinopathy and

retina The retina (from la, rete "net") is the innermost, light-sensitive layer of tissue of the eye of most vertebrates and some molluscs. The optics of the eye create a focused two-dimensional image of the visual world on the retina, which then ...

l and

optic nerve In neuroanatomy, the optic nerve, also known as the second cranial nerve, cranial nerve II, or simply CN II, is a paired cranial nerve that transmits visual system, visual information from the retina to the brain. In humans, the optic nerve i ...

injury. Coluracetam has been shown to reverse the loss of

choline acetyltransferase Choline acetyltransferase (commonly abbreviated as ChAT, but sometimes CAT) is a transferase enzyme responsible for the synthesis of the neurotransmitter acetylcholine. ChAT catalyzes the transfer of an acetyl group from the coenzyme acetyl-Co ...

production in the

medial septal nucleus The medial septal nucleus (MS) is one of the septal nuclei. Neurons in this nucleus give rise to the bulk of efferents from the septal nuclei. A major projection from the medial septal nucleus terminates in the hippocampal formation. It plays a ro ...

of rats exposed to phencyclidine (PCP), and is considered a potential therapeutic drug for

schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ...

Mechanism of action

Coluracetam enhances high-affinity choline uptake (HACU), which is the rate-limiting step of acetylcholine (ACh)

synthesis Synthesis or synthesize may refer to: Science Chemistry and biochemistry *Chemical synthesis, the execution of chemical reactions to form a more complex molecule from chemical precursors ** Organic synthesis, the chemical synthesis of organ ...

. Studies have shown coluracetam to improve

learning impairment Learning disability, learning disorder, or learning difficulty (British English) is a condition in the brain that causes difficulties comprehending or processing information and can be caused by several different factors. Given the "difficult ...

on a single oral dose given to rats which have been exposed to cholinergic

neurotoxin Neurotoxins are toxins that are destructive to nerve tissue (causing neurotoxicity). Neurotoxins are an extensive class of exogenous chemical neurological insultsSpencer 2000 that can adversely affect function in both developing and mature ner ...

s. Subsequent studies have shown that it may induce long-lasting procognitive effects in cholinergic neurotoxin-treated rats by changing the

choline transporter The high-affinity choline transporter (ChT) also known as solute carrier family 5 member 7 is a protein in humans that is encoded by the ''SLC5A7'' gene. It is a cell membrane transporter and carries choline into acetylcholine-synthesizing neuro ...

regulation system.

Legality

Australia

Coluracetam is a schedule 4 substance in Australia under the Poisons Standard (February 2020).Poisons Standard February 2020
comlaw.gov.au A schedule 4 substance is classified as "Prescription Only Medicine, or Prescription Animal Remedy – Substances, the use or supply of which should be by or on the order of persons permitted by State or Territory legislation to prescribe and should be available from a pharmacist on prescription."

References

{{Acetylcholine metabolism and transport modulators Racetams Acetamides Furans Experimental drugs

Mechanism of action

Legality

Australia

See also

References