Drug intelligence / Profile preview

MK-212

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-212 is a synthetic small molecule of the arylpiperazine family that acts as a serotonin receptor agonist. It is primarily characterized as a non-selective serotonin 5-HT₂ receptor agonist and more specifically as a relatively selective full agonist at the serotonin 5-HT₂C receptor. MK-212 also exhibits partial to full agonism at the serotonin 5-HT₂A and moderate-efficacy partial agonism at the serotonin 5-HT₂B receptors. Its potency for activating the 5‑HT₂C and 5‑HT₂B receptors is similar and about ten to thirty times higher than for activating the 5‑HT₂A receptor. The compound has low affinity for other serotonergic targets such as the serotonin 5‑HT₁A and 5‑HT₁B receptors. Pharmacologically, MK‑212 increases serum prolactin and cortisol in humans. It has been used experimentally in studies of neuroendocrine function, psychiatric disorders (including schizophrenia), substance use disorders (notably alcoholism), anxiety models in animals, and seizure research due to its serotonergic activity[1][2][3][6][8][10]. At typical doses studied in humans (up to ~40 mg orally), it does not produce classic hallucinogenic effects but can cause feelings of nausea or strangeness[1][6].

Other names
6-chloro-2-(1-piperazinyl)pyrazine2-chloro-6-(1-piperazinyl)pyrazineMK-212 hydrochlorideMK212 hydrochlorideMK 212 hydrochlorideCPP hydrochloride1-(6-chloro-2-pyrazinyl)piperazine hydrochloride
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR1B (5-Hydroxytryptamine Receptor 1B)HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR2C (5-hydroxytryptamine 2C receptor)

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