Osemozotan

Osemozotan (MKC-242) is a selective 5-HT_1A receptor agonist with some functional selectivity, acting as a full agonist at presynaptic and a partial agonist at postsynaptic 5-HT_1A receptors. 5-HT_1A receptor stimulation influences the release of various neurotransmitters including serotonin, dopamine, norepinephrine, and acetylcholine. 5-HT_1A receptors are inhibitory G protein-coupled receptor. Osemozotan has antidepressant, anxiolytic, antiobsessional, serenic, and analgesic effects in animal studies, , and is used to investigate the role of 5-HT_1A receptors in modulating the release of dopamine and serotonin in the brain, and their involvement in addiction to abused stimulants such as cocaine and methamphetamine.

Pharmacodynamics

The target of Osemozotan is 5-HT_1A receptors. This molecules bind with almost 1000 times greater affinity to 5-HT_1A receptors than most other 5-HT, dopamine, or adrenergic receptors. With repeated exposure of Osemozotan at the 5-HT_1A receptors, there seems to be no change in the number of receptors, which is not typically seen with pharmaceutical agonists.