Coluracetam
Summary of Coluracetam
Primary Information, Benefits, Effects, and Important Facts
Coluracetam (MKC-231) is a synthetic racetam drug purported to be a nootropic compound. It does not have a large body of evidence investigating it, but the mechanisms of action (as well as structute) appear to be very distinct from other racetam compounds like Piracetam or Aniracetam.
Coluracetam appears to interact with a process known as high affinity choline uptake (HACU for short), which is the rate-limiting step of drawing choline into a neuron for synthesis into the neurotransmitter acetylcholine. Increasing the HACU rate appears to increase the activity of cholinergic neurons, so it is a desired target for cognitive enhancement.
Interventions in rats (as there is no human evidence currently) support the usage of coluracetam at very low oral doses to preserve HACU that is otherwise impaired by the use of research drugs that are known to impair HACU. The limited evidence looking at the inherent effects of coluracetam on the HACU of normal neurons has failed to find any significant interaction.
Coluracetam has also been noted to associate with choline transporters physically, but it is not known exactly what it does once associated.
Overall, there is currently insufficient evidence to support the usage of coluracetam for cognitive enhancement. Further studies are needed to see if it has a therapeutic role in instances where HACU may be impaired (such as Alzheimer's disease).
Tired of misinformation? Get unbiased info on supplements.
At Examine.com, our incentives line up with yours — getting unbiased information. It’s why we don’t sell any advertising or supplements.
If you’re tired of wasting time and money on supplements that don’t work, our free Supplement Mini-Course will teach you about what works, what's a waste, and what to look out for when buying supplements.
Join the over 200,000 people who have gone through this course (saving themselves time, money, and stress).
Things To Know & Note
Primary Function:
Also Known As
MKC-231, BCI-540, 2-(2-oxopyrrolidin-1-yl)-N-(2, 3-dimethyl-5, 6, 7, 8-tetrahydrofuro2, 3-b quinolin-4-yl)acetoamide
Caution Notice
Examine.com Medical DisclaimerHow to Take Coluracetam
Recommended dosage, active amounts, other details
The animal research on coluracetam uses an oral dose of 300-3,000mcg/kg bodyweight, which is roughly translated into a human dose of 48-480mcg/kg or (for a 150lb person) 3.2-32.7mg overall.
It appears to have very rapid kinetics, with a peak in blood at around 30 minutes and on the decline within 3 hours. Due to this, supplementation may be time-dependent in relation to activity.
Research Breakdown on Coluracetam
Click on any below to expand the corresponding section. Click on to collapse it.
Click here to fully expand all sections or here to fully collapse them.
References
- ^ a b c d e f g Takashina K, et al. MKC-231, a choline uptake enhancer: (3) Mode of action of MKC-231 in the enhancement of high-affinity choline uptake. J Neural Transm. (2008)
- ^ a b c d e Bessho T, et al. MKC-231, a choline-uptake enhancer: (1) long-lasting cognitive improvement after repeated administration in AF64A-treated rats. J Neural Transm. (2008)
- ^ Simon JR, Atweh S, Kuhar MJ. Sodium-dependent high affinity choline uptake: a regulatory step in the synthesis of acetylcholine. J Neurochem. (1976)
- ^ Yamamura HI, Snyder SH. High affinity transport of choline into synaptosomes of rat brain. J Neurochem. (1973)
- ^ Rodríguez-Puertas R, et al. Selective cortical decrease of high-affinity choline uptake carrier in Alzheimer's disease: an autoradiographic study using 3H-hemicholinium-3. J Neural Transm Park Dis Dement Sect. (1994)
- ^ Rylett RJ, Ball MJ, Colhoun EH. Evidence for high affinity choline transport in synaptosomes prepared from hippocampus and neocortex of patients with Alzheimer's disease. Brain Res. (1983)
- ^ Slotkin TA, et al. Regulatory changes in presynaptic cholinergic function assessed in rapid autopsy material from patients with Alzheimer disease: implications for etiology and therapy. Proc Natl Acad Sci U S A. (1990)
- ^ Fisher A, et al. Long-term central cholinergic hypofunction induced in mice by ethylcholine aziridinium ion (AF64A) in vivo. J Pharmacol Exp Ther. (1982)
- ^ Takashina K, et al. MKC-231, a choline uptake enhancer: (2) Effect on synthesis and release of acetylcholine in AF64A-treated rats. J Neural Transm. (2008)
- ^ a b Bessho T, et al. Effect of the novel high affinity choline uptake enhancer 2-(2-oxopyrrolidin-1-yl)-N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro{2,3-b} quinolin-4-yl)acetoamide on deficits of water maze learning in rats. Arzneimittelforschung. (1996)
- ^ a b Murai S, et al. MKC-231, a choline uptake enhancer, ameliorates working memory deficits and decreased hippocampal acetylcholine induced by ethylcholine aziridinium ion in mice. J Neural Transm Gen Sect. (1994)
- ^ Morris BJ, Cochran SM, Pratt JA. PCP: from pharmacology to modelling schizophrenia. Curr Opin Pharmacol. (2005)
- ^ Shirayama Y, et al. Subsequent exposure to the choline uptake enhancer MKC-231 antagonizes phencyclidine-induced behavioral deficits and reduction in septal cholinergic neurons in rats. Eur Neuropsychopharmacol. (2007)
- ^ a b Akaike A, et al. Protective effect of MKC-231, a novel high affinity choline uptake enhancer, on glutamate cytotoxicity in cultured cortical neurons. Jpn J Pharmacol. (1998)
