MK-212

Use and effects

MK-212 did not produce hallucinogenic effects in humans at doses of up to 40mg orally. However, in other research, it occasionally produced LSD-like effects in alcoholic patients at a dose of 20mg. In addition, subsequent studies found that MK-212 at 20mg significantly increased ratings of feeling high and feeling strange.

Interactions

Pharmacology

Pharmacodynamics

MK-212 is an agonist of the serotonin 5-HT2 receptors, including the serotonin 5-HT2C, 5-HT2B, and 5-HT2A receptors, in that order of potency. It is a full agonist of the serotonin 5-HT2C receptor, a moderate-efficacy partial agonist of the serotonin 5-HT2B receptor, and a partial to full agonist of the serotonin 5-HT2A receptor. The drug shows similar potency in activating the serotonin 5-HT2C and 5-HT2B receptors and around 10- to 30-fold lower relative potency in activating the serotonin 5-HT2A receptor. It also shows low affinity for the serotonin 5-HT1A and 5-HT1B receptors. THe comprehensive receptor interactions of MK-212 have been studied.

In a 1977 study by Clineschidt and colleagues, they dosed mice with varying concentrations of MK-212, and observed its effects. The result correlated very well to binding of indolealkylamine receptors, such as the serotonin and tryptamine receptors, which shows four characteristics. Namely, increased frequency of muscle twitching, increased twitching of the head, "an increase in the strength of the crossed extensor reflex in the acutely spinalized rat", and the cause of complex motor syndrome.

References

References

1. (1979). "MK-212: a serotonin-like agonist in the CNS". General Pharmacology.
2. (September 1990). "Prolactin and cortisol responses to MK-212, a serotonin agonist, in obsessive-compulsive disorder". Archives of General Psychiatry.
3. (2005). "Serotonergic 5-HT2C receptors as a potential therapeutic target for the design antiepileptic drugs". Curr Top Med Chem.
4. (December 2005). "Selective and nonselective serotonin antagonists block the aversive stimulus properties of MK212 and m-chlorophenylpiperazine (mCPP) in mice". Neuropharmacology.
5. (April 1988). "Stimulation of serum cortisol and prolactin secretion in humans by MK-212, a centrally active serotonin agonist". Biol Psychiatry.
6. (March 1992). "Effect of the serotonin agonist, MK-212, on body temperature in schizophrenia". Biol Psychiatry.
7. (August 1994). "The effect of apomorphine, MK-212 (6-chloro-2-[1-piperazinyl]-pyrazine) and placebo on smooth pursuit gain and corrective saccades in normal subjects". Neuropsychopharmacology.
8. (September 1999). "Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells". Br J Pharmacol.
9. (June 2002). "Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT(2A) and 5-HT(2C) receptors". Br J Pharmacol.
10. (2001). "Modulation of 5-HT(2A) receptor-mediated head-twitch behaviour in the rat by 5-HT(2C) receptor agonists". Pharmacol Biochem Behav.
11. (1988). "Functional correlates of serotonin 5-HT1 recognition sites". J Recept Res.
12. (July 2025). "The polypharmacology of psychedelics reveals multiple targets for potential therapeutics". Neuron.
13. (July 1977). "Central serotonin-like activity of 6-chloro-2-[1-piperazinyl]-pyrazine (CPP; MK-212)". European Journal of Pharmacology.