What do Catechol-O-methyltransferase (COMT) inhibitors do in the brain?

Catechol-O-methyltransferase (COMT) inhibitors are designed to prevent the breakdown of catecholamines, notably dopamine, in the brain. By inhibiting the activity of the COMT enzyme, these medications allow for increased levels of dopamine to remain in synaptic clefts and within neurons. This elevation in dopamine concentration can help alleviate symptoms in conditions like Parkinson's disease, where dopaminergic activity is diminished.

Dopamine plays a crucial role in several brain functions, including mood regulation, motivation, and motor control. Therefore, the main action of COMT inhibitors directly targets the metabolism of dopamine, enhancing its availability and effectiveness in neuronal signaling.

While serotonin, norepinephrine, and GABA are important neurotransmitters in the brain, they are not the primary targets of COMT inhibitors. Instead, the focus on dopamine metabolism makes these inhibitors particularly useful for therapeutic strategies aimed at improving dopaminergic function.