MK-212 did not producehallucinogenic effects in humans at doses of up to 40mgorally.[1] However, in other research, it occasionally producedLSD-like effects inalcoholic patients at a dose of 20mg.[1] In addition, subsequent studies found that MK-212 at 20mg significantly increased ratings of feeling high and feeling strange.[3][6][7]
In a 1977 study by Clineschidt and colleagues, they dosed mice with varying concentrations of MK-212, and observed its effects.[13]The result correlated very well to binding ofindolealkylaminereceptors, such as theserotonin andtryptamine receptors, which shows four characteristics. Namely, increased frequency ofmuscle twitching,increased twitching of the head,[8] "an increase in the strength of the crossed extensor reflex in the acutely spinalized rat", and the cause of complex motor syndrome.[13]
^abcdLowy MT, Meltzer HY (April 1988). "Stimulation of serum cortisol and prolactin secretion in humans by MK-212, a centrally active serotonin agonist".Biol Psychiatry.23 (8):818–828.doi:10.1016/0006-3223(88)90070-4.PMID3365458.The effects of MK-212 [6-chloro-2-(1-piperazinyl)-pyrazine] (10, 20, and 40 mg, orally), a centrally acting serotonin (5-HT) receptor agonist and placebo, on serum cortisol, prolactin, and growth hormone levels were studied in eight healthy men over 3-hr. [...] MK-212 was generally well tolerated by the subjects. Headache and nausea were observed at the higher doses, [...] It has been suggested that 5-HT2 receptor mechanisms may be involved in the mechanism of action of hallucinogenic agents (Glennon et al. 1984). None of the subjects reported hallucinations following any dose of MK-212. Interestingly, on occasion, alcoholic patients given a 20-mg dose of MK-212 have reported that MK-212 produces an LSD-like effect (Meltzer et al. unpublished observations). However, in rats trained to discriminate MK-212 from saline, LSD did not completely substitute for MK-212 (Cunningham et al. 1986). In addition, ketanserin failed to block the discriminative stimulus properties of MK-212.
^abBastani B, Nash JF, Meltzer HY (September 1990). "Prolactin and cortisol responses to MK-212, a serotonin agonist, in obsessive-compulsive disorder".Archives of General Psychiatry.47 (9):833–839.doi:10.1001/archpsyc.1990.01810210041006.PMID2203327.
^Isaac M (2005). "Serotonergic 5-HT2C receptors as a potential therapeutic target for the design antiepileptic drugs".Curr Top Med Chem.5 (1):59–67.doi:10.2174/1568026053386980.PMID15638778.
^Walker EA, Kohut SJ, Hass RW, Brown EK, Prabandham A, Lefever T (December 2005). "Selective and nonselective serotonin antagonists block the aversive stimulus properties of MK212 and m-chlorophenylpiperazine (mCPP) in mice".Neuropharmacology.49 (8):1210–1219.doi:10.1016/j.neuropharm.2005.07.015.PMID16165167.
^Lee HS, Bastani B, Friedman L, Ramirez L, Meltzer HY (March 1992). "Effect of the serotonin agonist, MK-212, on body temperature in schizophrenia".Biol Psychiatry.31 (5):460–470.doi:10.1016/0006-3223(92)90258-2.PMID1581424.
^Friedman L, Jesberger JA, Meltzer HY (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.11 (1):49–62.doi:10.1038/npp.1994.35.PMID7945744.
^abcVickers SP, Easton N, Malcolm CS, Allen NH, Porter RH, Bickerdike MJ, Kennett GA (2001). "Modulation of 5-HT(2A) receptor-mediated head-twitch behaviour in the rat by 5-HT(2C) receptor agonists".Pharmacol Biochem Behav.69 (3–4):643–652.doi:10.1016/s0091-3057(01)00552-4.PMID11509227.
