MK-212 HCl
new
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525681

CAS#: 61655-58-1 (HCl)

Description: MK-212 is a 5HT2C-receptor agonist. A dose-dependent the effect of 5HT2C-receptor agonist MK-212 on mouse behavior was demonstrated. Intraperitoneal injection of MK-212 in high doses (0.5 and 1.0 mg/kg) increased blood level of corticosterone in mice and reduced their motor activity. In low doses of 0.1 and 0.2 mg/kg, the agonist reduced anxiety, but had no effect on motor activity. It is hypothesized that low doses of MK-212 exhibited anxiolytic activity in mice.


Chemical Structure

img
MK-212 HCl
CAS# 61655-58-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 525681
Name: MK-212 HCl
CAS#: 61655-58-1 (HCl)
Chemical Formula: C8H12Cl2N4
Exact Mass: 234.04
Molecular Weight: 235.112
Elemental Analysis: C, 40.87; H, 5.14; Cl, 30.16; N, 23.83

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 1950 2 Weeks
1g USD 2950 2 Weeks
2g USD 5150 2 Weeks
5g USD 7950 2 Weeks
Bulk inquiry

Related CAS #: 64022-27-1 (free base)   61655-58-1 (HCl)    

Synonym: MK212; MK 212; MK-212

IUPAC/Chemical Name: 2-chloro-6-(piperazin-1-yl)pyrazine hydrochloride

InChi Key: PFIZGLUIYAZQFU-UHFFFAOYSA-N

InChi Code: InChI=1S/C8H11ClN4.ClH/c9-7-5-11-6-8(12-7)13-3-1-10-2-4-13;/h5-6,10H,1-4H2;1H

SMILES Code: ClC1=CN=CC(N2CCNCC2)=N1.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: MK-212 (CPP) monohydrochloride is a centrally acting 5-HT1C/5-HT2 agonist.
In vitro activity: The inhibitory effects of microiontophoretically-applied serotonin (5-HT) and 6-chloro-2[1-piperazinyl]pyrazine (MK-212) were examined on spontaneously firing somatosensory cerebral cortical neurons and dorsal raphe neurons in rats anesthetized with chloral hydrate. On cortical neurons, MK-212 caused only weak and variable inhibition of extracellularly recorded neuronal activity, compared to the effects of 5-HT. However, on raphe cells, MK-212 exerted potent inhibitory effects, equivalent to those observed with 5-HT. Reference: Neuropharmacology. 1984 Nov;23(11):1271-7. https://pubmed.ncbi.nlm.nih.gov/6527736/
In vivo activity: The results showed that systemic administration of the 5-HT2C receptor agonist MK212 did not affect normal PPI behavior, but reversed the PPI deficits induced by the N-methyl d-aspartate receptor antagonist MK801 in mice. In addition, the 5-HT2C receptor antagonist SB242084 had no effect on PPI behavior despite MK801 treatment. Moreover, local infusion of MK212 into the medial prefrontal cortex and ventral hippocampus, excluding the nucleus accumbens or ventral tegmental area, rescued the PPI deficits induced by MK801. Reference: Prog Neuropsychopharmacol Biol Psychiatry. 2022 Mar 8;113:110441. https://pubmed.ncbi.nlm.nih.gov/34560172/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Water 11.8 50.00

Preparing Stock Solutions

The following data is based on the product molecular weight 235.11 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Yarbrough GG, Singh DK, Pettibone DJ. A comparative electrophysiological and biochemical assessment of serotonin (5-HT) and a novel 5-HT agonist (MK-212) on central serotonergic receptors. Neuropharmacology. 1984 Nov;23(11):1271-7. doi: 10.1016/0028-3908(84)90044-3. PMID: 6527736. 2. Guo G, Tang J, Shi M, Yang C, Ou H, Chen W. MK212, a 5-hydroxytryptamine 2C receptor agonist, reverses prepulse inhibition deficits in the medial prefrontal cortex and ventral hippocampus. Prog Neuropsychopharmacol Biol Psychiatry. 2022 Mar 8;113:110441. doi: 10.1016/j.pnpbp.2021.110441. Epub 2021 Sep 21. PMID: 34560172. 3. Wang X, Sun M, Gan L, Chen W. MK212, a 5-hydroxytryptamine 2C receptor agonist, inhibits conditioned avoidance responses independent of blocking endogenous dopamine release in rats. Prog Neuropsychopharmacol Biol Psychiatry. 2019 Mar 8;89:16-22. doi: 10.1016/j.pnpbp.2018.08.022. Epub 2018 Aug 24. PMID: 30145182.
In vitro protocol: 1. Yarbrough GG, Singh DK, Pettibone DJ. A comparative electrophysiological and biochemical assessment of serotonin (5-HT) and a novel 5-HT agonist (MK-212) on central serotonergic receptors. Neuropharmacology. 1984 Nov;23(11):1271-7. doi: 10.1016/0028-3908(84)90044-3. PMID: 6527736.
In vivo protocol: 1. Guo G, Tang J, Shi M, Yang C, Ou H, Chen W. MK212, a 5-hydroxytryptamine 2C receptor agonist, reverses prepulse inhibition deficits in the medial prefrontal cortex and ventral hippocampus. Prog Neuropsychopharmacol Biol Psychiatry. 2022 Mar 8;113:110441. doi: 10.1016/j.pnpbp.2021.110441. Epub 2021 Sep 21. PMID: 34560172. 2. Wang X, Sun M, Gan L, Chen W. MK212, a 5-hydroxytryptamine 2C receptor agonist, inhibits conditioned avoidance responses independent of blocking endogenous dopamine release in rats. Prog Neuropsychopharmacol Biol Psychiatry. 2019 Mar 8;89:16-22. doi: 10.1016/j.pnpbp.2018.08.022. Epub 2018 Aug 24. PMID: 30145182.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Kozhevnikova LM, Mesitov MV, Moskovtsev AA. [Agonists of 5HT2C-receptors SCH 23390 and MK 212 incresase the force of rat aorta contraction in the presence of vasopressin and angiotensin II]. Patol Fiziol Eksp Ter. 2014 Oct-Dec;(4):17-29. Russian. PubMed PMID: 25980223.
2: Kuznetsova EG, Amstislavskaya TG, Bulygina VV, Tibeikina MA, Popova NK. Effect of 5HT2C-receptor agonist MK-212 on blood corticosterone level and behavior in mice. Bull Exp Biol Med. 2006 Nov;142(5):594-7. PubMed PMID: 17415471.
3: de Mello Cruz AP, Pinheiro G, Alves SH, Ferreira G, Mendes M, Faria L, Macedo CE, Motta V, Landeira-Fernandez J. Behavioral effects of systemically administered MK-212 are prevented by ritanserin microinfusion into the basolateral amygdala of rats exposed to the elevated plus-maze. Psychopharmacology (Berl). 2005 Nov;182(3):345-54. Epub 2005 Oct 19. PubMed PMID: 16133141.
4: Halford JC, Lawton CL, Blundell JE. The 5-HT2 receptor agonist MK-212 reduces food intake and increases resting but prevents the behavioural satiety sequence. Pharmacol Biochem Behav. 1997 Jan;56(1):41-6. PubMed PMID: 8981607.
5: Hemrick-Luecke SK, Fuller RW. Involvement of 5-HT2A receptors in the elevation of rat serum corticosterone concentrations by quipazine and MK-212. Eur J Pharmacol. 1996 Sep 12;311(2-3):207-11. PubMed PMID: 8891601.
6: Meltzer HY, Maes M. Effect of pindolol pretreatment on MK-212-induced plasma cortisol and prolactin responses in normal men. Biol Psychiatry. 1995 Sep 1;38(5):310-8. PubMed PMID: 7495925.
7: Friedman L, Jesberger JA, Meltzer HY. 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. 1994 Aug;11(1):49-62. PubMed PMID: 7945744.
8: Lee MA, Meltzer HY. Blunted oral body temperature response to MK-212 in cocaine addicts. Drug Alcohol Depend. 1994 Jun;35(3):217-22. PubMed PMID: 7956751.
9: Li Q, Brownfield MS, Battaglia G, Cabrera TM, Levy AD, Rittenhouse PA, van de Kar LD. 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). J Pharmacol Exp Ther. 1993 Aug;266(2):836-44. PubMed PMID: 8394920.
10: Cooper SJ, Barber DJ. Effects of d-fenfluramine, MK-212, and ondansetron on saline drinking in two-choice tests in the rehydrating rat. Pharmacol Biochem Behav. 1993 Jul;45(3):593-6. PubMed PMID: 8332621.
11: Van de Kar LD, Rittenhouse PA, O'Connor P, Palionis T, Brownfield MS, Lent SJ, Carnes M, Bethea CL. Effect of cocaine injections on the neuroendocrine response to the serotonin agonist MK-212. Biol Psychiatry. 1992 Aug 1;32(3):258-69. PubMed PMID: 1330009.
12: Lee HS, Bastani B, Friedman L, Ramirez L, Meltzer HY. Effect of the serotonin agonist, MK-212, on body temperature in schizophrenia. Biol Psychiatry. 1992 Mar 1;31(5):460-70. PubMed PMID: 1581424.
13: Bastani B, Nash JF, Meltzer HY. Prolactin and cortisol responses to MK-212, a serotonin agonist, in obsessive-compulsive disorder. Arch Gen Psychiatry. 1990 Sep;47(9):833-9. PubMed PMID: 2203327.
14: McKearney JW. Effects of serotonin agonists on operant behavior in the squirrel monkey: quipazine, MK-212, trifluoromethylphenylpiperazine, and chlorophenylpiperazine. Pharmacol Biochem Behav. 1990 Jan;35(1):181-5. PubMed PMID: 2315357.
15: Reis LC, Ramalho MJ, Antunes-Rodrigues J. Central serotonergic modulation of drinking behavior induced by angiotensin II and carbachol in normally hydrated rats: effect of intracerebroventricular injection of MK-212. Braz J Med Biol Res. 1990;23(12):1339-42. PubMed PMID: 2136567.
16: Reis LC, Ramalho MJ, Antunes-Rodrigues J. Central serotonergic modulation of drinking behavior induced by water deprivation: effect of a serotonergic agonist (MK-212) administered intracerebroventricularly. Braz J Med Biol Res. 1990;23(12):1335-8. PubMed PMID: 2136566.
17: King BH, Brazell C, Dourish CT, Middlemiss DN. MK-212 increases rat plasma ACTH concentration by activation of the 5-HT1C receptor subtype. Neurosci Lett. 1989 Oct 23;105(1-2):174-6. PubMed PMID: 2562060.
18: McKearney JW. Apparent antinociceptive properties of piperazine-type serotonin agonists: trifluoromethylphenylpiperazine, chlorophenylpiperazine, and MK-212. Pharmacol Biochem Behav. 1989 Mar;32(3):657-60. PubMed PMID: 2740421.
19: Lowy MT, Meltzer HY. Stimulation of serum cortisol and prolactin secretion in humans by MK-212, a centrally active serotonin agonist. Biol Psychiatry. 1988 Apr 15;23(8):818-28. PubMed PMID: 3365458.
20: Cunningham KA, Callahan PM, Appel JB. Discriminative stimulus properties of the serotonin agonist MK 212. Psychopharmacology (Berl). 1986;90(2):193-7. PubMed PMID: 3097699.