Coluracetam is believed to have nootropic properties, but lacks pronounced cognitive enhancing effects.
Coluracetam enhances high affinity choline uptake (HACU). This is the process by which cholinergic neurons take up choline, which is acetylated in the cytoplasm to acetylcholine. Acetylcholine is the neurotransmitter associated with memory; acetylcholinesterase inhibitors are Alzheimer’s drugs.
Coluracetam increases cholinergic transmission indirectly by increasing choline uptake and acetylcholine synthesis. Another nootropic agent that affects this signaling pathway is Nicotine.
Coluracetam Half Life
When choosing a dosing schedule, it is important to know the half-life of a drug. The half-life refers to the interval of time it takes for the plasma concentration of a drug to be reduced by one half. Drugs with extremely short half lives are often abandoned by pharmaceutical companies because they’re duration of action is too short. The half life of coluracetam is relatively short.
[sunote notecolor=”#F2F2F2″ textcolor=”#66666″]Extrapolating from rodent studies, Coluracetam’s half-life is approximately 1 hour. Peak blood concentrations are attained 30 minutes after dosing. In rats, 14% of the peak coluracetam concentrations remained after 3 hours. Daily dosing of coluracetam does not affect these kinetics.[/sunote]
Coluracetam’s rapid half-life may not be indicative of the duration of its nootropic effects.
Since Coluracetam increases the available choline pool inside neurons, intracellular acetylcholine synthesis may be increased even after the drug has been metabolized and excreted.
Coluracetam vs Other Cholinergic Drugs
Coluracetam may have an advantage over other drugs that affect acetylcholine.
Acetylcholinesterase inhibitors nonspecifically increase the amount of acetylcholine in the synapse. Nicotinic and muscarinic agonists directly stimulate acetylcholine receptors. In contrast, since Coluracetam enhances the available pool of acetylcholine that can be released (via exocytosis) by a neuron, Coluracetam amplifies acetylcholine signaling without impairing the signal-to-noise ratio.
For example, non-specific amplification of neurotransmission can impair neural networks because the signal is lost (too much noise). Coluracetam boosts the activity of acetylcholine without directly interfering with the neuron’s regulation of acetylcholine release. Hence, Coluracetam will not result in inappropriate acetycholine release, unlike other drugs that affect this neurotransmitter system.