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Chemical Compound Review

Tocris-0941     2-chloro-6-piperazin-1-yl- pyrazine

Synonyms: CHEMBL269521, MK-212, CHEBI:105969, NSC-317326, BPBio1_000111, ...
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Disease relevance of MK-212

  • Forty-eight hours after a single injection of mianserin, there was a shift to the right in the dose-response relationship for MK-212-induced hyperthermia [1].
  • In contrast, pindolol (0.03-0.1 mg/kg) and methiothepin (10 mg/kg) selectively antagonized hypothermia induced by 8-OH-DPAT but did not alter hyperthermia induced by MK-212 [2].
  • DOI (5-HT1C/2 agonist, 0-5 mg/kg i.p.) and 6-chloro-2-[1-piperazinyl]-pyrazine (MK-212) (less selective, but predominantly a 5-HT1C agonist, 0-20 mg/kg i.p.) were administered 18 hr after the final antidepressant injection and 30 min before decapitation [3].
  • Our present study indicated the possible value of MK-212 and (-)-baclofen in the management of clinical myoclonus [4].
  • Besides, MK 212 failed to influence catalepsy following administration of haloperidol [5].

Psychiatry related information on MK-212


High impact information on MK-212


Chemical compound and disease context of MK-212


Biological context of MK-212


Anatomical context of MK-212


Associations of MK-212 with other chemical compounds


Gene context of MK-212

  • Chronic treatment with mianserin (10 mg/kg/day), a tetracyclic antidepressant with 5-HT1C and 5-HT2 receptor antagonistic properties, did not change PE induced by MK 212, but caused an increase of PE induced by DOI and a decrease of DOI-induced HS [28].
  • METHODS: In the first experiment, male Wistar rats were exposed for 5 min to the EPM 27 min following intraperitoneal (i.p.) (1.0 ml/kg) injections of the preferential 5-HT2C receptor agonist 6-chloro-2[1-piperazinyl]pyrazine (MK-212) at doses of 1.0, 2.0, or 4.0 mg/kg [7].
  • Clozapine administration to schizophrenic patients was found to produce dopamine2 (D-2) and serotonin2 (5-HT2) receptor blockade, as evidenced by the ability to block the increases in growth hormone and cortisol secretion produced by apomorphine and MK-212, respectively, direct acting dopamine (DA) and 5-HT2 agonists [29].
  • In contrast, the effect of the high dose of MK-212 on plasma prolactin concentration was reduced by both antidepressants [3].
  • The MK-212-induced increase in plasma concentrations of corticosterone and beta-END were not affected by treatment with the 5-HT1A antagonists spiperone and (-)-pindolol [30].

Analytical, diagnostic and therapeutic context of MK-212

  • MK-212 was effective despite bilateral vagotomy [31].
  • MK-212 was not self-administered by rats, while the self-administration of amphetamine and morphine were demonstrated using the same experimental protocol [32].
  • Male Wistar rats implanted with a cannula in the 3rd ventricle were injected with the 5-HT1C/5-HT2 agonist 6-chloro-2-[1-piperazinyl]-pyrazine (MK-212) at doses of 0.5, 5, 25, 50 and 125 nmol/2 microliters [8].


  1. Selective desensitization of serotonin (5-HT) receptor-mediated hyperthermia by mianserin and other 5-HT antagonists. Gudelsky, G.A., Koenig, J.I., Meltzer, H.Y. Neuropharmacology (1987) [Pubmed]
  2. Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors. Gudelsky, G.A., Koenig, J.I., Meltzer, H.Y. Neuropharmacology (1986) [Pubmed]
  3. Long-term treatment with the antidepressants fluoxetine and desipramine potentiates endocrine responses to the serotonin agonists 6-chloro-2-[1-piperazinyl]-pyrazine (MK-212) and (+-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane HCl (DOI). Li, Q., Brownfield, M.S., Battaglia, G., Cabrera, T.M., Levy, A.D., Rittenhouse, P.A., van de Kar, L.D. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  4. Serotonergic drugs, benzodiazepines and baclofen block muscimol-induced myoclonic jerks in a strain of mice. Menon, M.K., Vivonia, C.A. Eur. J. Pharmacol. (1981) [Pubmed]
  5. Effect of serotonergic agents on neuroleptic induced catalepsy in rats. Rao, S.G., Hrishikeshavan, H.J., Guruswami, M.N. Funct. Neurol. (1990) [Pubmed]
  6. Prolactin and cortisol responses to MK-212, a serotonin agonist, in obsessive-compulsive disorder. Bastani, B., Nash, J.F., Meltzer, H.Y. Arch. Gen. Psychiatry (1990) [Pubmed]
  7. Behavioral effects of systemically administered MK-212 are prevented by ritanserin microinfusion into the basolateral amygdala of rats exposed to the elevated plus-maze. de Mello Cruz, A.P., Pinheiro, G., Alves, S.H., Ferreira, G., Mendes, M., Faria, L., Macedo, C.E., Motta, V., Landeira-Fernandez, J. Psychopharmacology (Berl.) (2005) [Pubmed]
  8. Central serotonergic modulation of drinking behavior induced by water deprivation: effect of a serotonergic agonist (MK-212) administered intracerebroventricularly. Reis, L.C., Ramalho, M.J., Antunes-Rodrigues, J. Braz. J. Med. Biol. Res. (1990) [Pubmed]
  9. A single point mutation (Phe340-->Leu340) of a conserved phenylalanine abolishes 4-[125I]iodo-(2,5-dimethoxy)phenylisopropylamine and [3H]mesulergine but not [3H]ketanserin binding to 5-hydroxytryptamine2 receptors. Choudhary, M.S., Craigo, S., Roth, B.L. Mol. Pharmacol. (1993) [Pubmed]
  10. Effect of the serotonin agonist, MK-212, on body temperature in schizophrenia. Lee, H.S., Bastani, B., Friedman, L., Ramirez, L., Meltzer, H.Y. Biol. Psychiatry (1992) [Pubmed]
  11. Differential effects of novel ligands for 5-HT receptor subtypes on nonopioid defensive analgesia in male mice. Rodgers, R.J., Shepherd, J.K., Donát, P. Neuroscience and biobehavioral reviews. (1991) [Pubmed]
  12. Administration of SCH 23390 into the medial prefrontal cortex blocks the expression of MDMA-induced behavioral sensitization in rats: an effect mediated by 5-HT2C receptor stimulation and not by D1 receptor blockade. Ramos, M., Goñi-Allo, B., Aguirre, N. Neuropsychopharmacology (2005) [Pubmed]
  13. Modification of apomorphine hypothermia by drugs affecting brain 5-hydroxytryptamine function. Menon, M.K., Vivonia, C.A. Eur. J. Pharmacol. (1981) [Pubmed]
  14. Selective cross-tolerance to 5-HT1A and 5-HT2 receptor-mediated temperature and corticosterone responses. Nash, J.F., Meltzer, H.Y., Gudelsky, G.A. Pharmacol. Biochem. Behav. (1989) [Pubmed]
  15. The effect of apomorphine, MK-212 (6-chloro-2-[1-piperazinyl]-pyrazine) and placebo on smooth pursuit gain and corrective saccades in normal subjects. Friedman, L., Jesberger, J.A., Meltzer, H.Y. Neuropsychopharmacology (1994) [Pubmed]
  16. Serotonin-stimulated phosphoinositide turnover: mediation by the S2 binding site in rat cerebral cortex but not in subcortical regions. Conn, P.J., Sanders-Bush, E. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  17. Modulation of 5-HT receptor subtype-mediated behaviours by corticosterone. Berendsen, H.H., Kester, R.C., Peeters, B.W., Broekkamp, C.L. Eur. J. Pharmacol. (1996) [Pubmed]
  18. The 5-HT2 receptor agonist MK-212 reduces food intake and increases resting but prevents the behavioural satiety sequence. Halford, J.C., Lawton, C.L., Blundell, J.E. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  19. Pharmacological characterization of serotonin-stimulated phosphoinositide turnover in brain regions of the immature rat. Claustre, Y., Rouquier, L., Scatton, B. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  20. In vivo modulation of vagal-identified dorsal medullary neurones by activation of different 5-Hydroxytryptamine(2) receptors in rats. Sévoz-Couche, C., Spyer, K.M., Jordan, D. Br. J. Pharmacol. (2000) [Pubmed]
  21. Preferential modulation of mesolimbic vs. nigrostriatal dopaminergic function by serotonin(2C/2B) receptor agonists: a combined in vivo electrophysiological and microdialysis study. Di Giovanni, G., Di Matteo, V., Di Mascio, M., Esposito, E. Synapse (2000) [Pubmed]
  22. In vivo effects of serotonergic agents on alpha-melanocyte-stimulating hormone secretion. Carr, J.A., Saland, L.C., Samora, A., Benavidez, S., Krobert, K. Neuroendocrinology (1991) [Pubmed]
  23. 5-HT1C receptors mediate phosphoinositide turnover activation in the immature rat hippocampus. Claustre, Y., Eudeline, B., Benavides, J., Scatton, B. Eur. J. Pharmacol. (1992) [Pubmed]
  24. Neuroendocrine responses to serotonergic agents in alcoholics. Lee, M.A., Meltzer, H.Y. Biol. Psychiatry (1991) [Pubmed]
  25. Stimulus properties of fluvoxamine in a conditioned taste aversion procedure. Gommans, J., Bouwknecht, J.A., Hijzen, T.H., Berendsen, H.H., Broekkamp, C.L., Maes, R.A., Olivier, B. Psychopharmacology (Berl.) (1998) [Pubmed]
  26. Discriminative stimulus properties of the serotonin agonist MK 212. Cunningham, K.A., Callahan, P.M., Appel, J.B. Psychopharmacology (Berl.) (1986) [Pubmed]
  27. Effects of MK-212 (6-chloro-2[1-piperazinyl]pyrazine) on schedule-controlled behavior and their reversal by 5-HT antagonists in the pigeon. Mansbach, R.S., Barrett, J.E. Neuropharmacology (1986) [Pubmed]
  28. Attenuation of 5-HT1A and 5-HT2 but not 5-HT1C receptor mediated behaviour in rats following chronic treatment with 5-HT receptor agonists, antagonists or anti-depressants. Berendsen, H.H., Broekkamp, C.L. Psychopharmacology (Berl.) (1991) [Pubmed]
  29. Clinical studies on the mechanism of action of clozapine: the dopamine-serotonin hypothesis of schizophrenia. Meltzer, H.Y. Psychopharmacology (Berl.) (1989) [Pubmed]
  30. Stimulation of corticosterone and beta-endorphin secretion in the rat by selective 5-HT receptor subtype activation. Koenig, J.I., Gudelsky, G.A., Meltzer, H.Y. Eur. J. Pharmacol. (1987) [Pubmed]
  31. Central serotonergic agents raise the repetitive extrasystole threshold of the vulnerable period of the canine ventricular myocardium. Blatt, C.M., Rabinowitz, S.H., Lown, B. Circ. Res. (1979) [Pubmed]
  32. Anorexigenic and ancillary actions of MK-212 (6-chloro-2-(1-piperazinyl)-pyrazine; CPP). Clineschmidt, B.V., Hanson, H.M., Pflueger, A.B., McGuffin, J.C. Psychopharmacology (Berl.) (1977) [Pubmed]
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