MK212 - CAS 64022-27-1
Catalog number: 64022-27-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C8H11ClN4
Molecular Weight:
198.65
COA:
Inquire
Targets:
5-HT Receptor
Description:
MK212 is a 5HT2C-receptor agonist. It exhibited anxiolytic activity in mice at low doses. It is a serotonin agonist. It could promote the secretion of serum prolactin and cortisol in humans.
Purity:
98%
Appearance:
Solid powder
Synonyms:
2-Chloro-6-(1-piperazinyl)pyrazine;MK-212;2-Chloro-6-(piperazin-1-yl)pyrazine
Solubility:
Soluble in DMSO, not in water
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
MK212 exhibites anxiolytic activity and could promote the secretion of serum prolactin and cortisol in humans.
Quality Standard:
In-house standard
Quantity:
Grams to Kilograms
Boiling Point:
364.1±42.0 °C | Condition: Press: 760 Torr
Density:
1.272±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
CJAWPFJGFFNXQI-UHFFFAOYSA-N
InChI:
InChI=1S/C8H11ClN4/c9-7-5-11-6-8(12-7)13-3-1-10-2-4-13/h5-6,10H,1-4H2
Canonical SMILES:
C1CN(CCN1)C2=CN=CC(=N2)Cl
1.5-HT2 receptor-mediated reversal of the inhibition of hippocampal long-term potentiation by acute inescapable stress.
Ryan BK;Anwyl R;Rowan MJ Neuropharmacology. 2008 Aug;55(2):175-82. doi: 10.1016/j.neuropharm.2008.05.006. Epub 2008 May 16.
The serotonergic system is known to modulate and mediate many of the central nervous system effects of stress. Here we investigated the ability of serotonergic agents to reverse the inhibition of the induction of hippocampal long-term potentiation (LTP) caused by prior exposure to inescapable stress. Elevated platform stress prevented the induction of LTP in the CA1 area of anaesthetized rats. An agent that increases extracellular 5-HT concentration, fenfluramine (5 mg/kg, i.p.) enabled the induction of LTP in previously stressed animals. Consistent with a role for enhanced activation of 5-HT(2) receptors, the facilitatory effect of fenfluramine was prevented by the 5-HT(2) receptor antagonist cinanserin (30 mg/kg). Agents that directly activate 5-HT(2) receptors, including the 5-HT(2B) receptor agonist BW 723C86 (30 mg/kg) and the 5-HT(2C) receptor agonist MK-212 (3 mg/kg), mimicked the restorative effect of fenfluramine. Fenfluramine also opposed inhibition of LTP caused by the NMDA-receptor antagonist D-AP5 (100 nmol, i.c.v.) which suggests that the facilitatory action of serotonergic agents is not restricted to stress-mediated inhibition of LTP. These findings support an important role for activation of 5-HT(2) receptors by systemically applied agents to enable recovery from the inhibition of LTP by stress.
2.Further investigations of the serotonergic properties of the ibogaine-induced discriminative stimulus.
Helsley S;Rabin RA;Winter JC Prog Neuropsychopharmacol Biol Psychiatry. 1999 Feb;23(2):317-26.
1. 5-HT3, 5-HT2C, and 5-HT1A receptor ligands were assessed in rats trained to discriminate ibogaine from water. 2. Significant ibogaine-appropriate responding was observed following treatment with the 5-HT2C agonists MK-212 (79.6%) and mCPP (76.4%). This substitution was completely antagonized by metergoline, an agent with 5-HT2C antagonist properties. However, metergoline was ineffective against ibogaine itself. This suggests that although ibogaine may act as an agonist at 5-HT2C receptors, this interaction is not essential to its discriminative cue. 3. Neither the 5-HT3 agonist, mCPBG (44.3%), nor the 5-HT3 antagonist, ondansetron (48.9%) substituted for ibogaine. Likewise, the 5-HT1A agonist 8-OH-DPAT (34.7%) and the 5-HT1A antagonist WAY-100635 (30.1%) failed to substitute. Furthermore, WAY-100635 failed to antagonize the ibogaine cue. 4. Unlike 5-HT2C receptors, 5-HT1A and 5-HT3 receptors do not appear to be involved in the ibogaine stimulus.
3.Anorexigenic and ancillary actions of MK-212 (6-chloro-2-(1-piperazinyl)-pyrazine; CPP).
Clineschmidt BV;Hanson HM;Pflueger AB;McGuffin JC Psychopharmacology (Berl). 1977 Nov 24;55(1):27-33.
In rats allowed to eat for 2 h/day and injected i.p. 30 min before feeding, MK-212, ED50 = 1.5 mg/kg, was two times more potent as an anorexigen than fenfluramine. However, the compounds were equiactive in the rat following p.o. administration 1.5 or 3 h before the test, while fenfluramine was more potent if the interval was extended to 6 h. In cats permitted to eat for 3 h/day, the ED50 dose (mg/kg p.o.) for MK-212 determined at 0.5, 1 and 3 h after feeding was, respectively, 15, 10, and 3 times less than that of fenfluramine. Emesis and diarrhea were frequently observed ancillary effects in cats treated with fenfluramine, whereas apparent sedation and salivation were commonly detected in animals after MK-212. In rats or cats pretreated with methergoline, the decrease in food consumption elicited by MK-212 was markedly inhibited, suggesting that the mechanism of action involves a serotoninlike effect. Compared with the marked stimulant action of amphetamine, MK-212 had only a minor and inconsistent effect on motor activity in rats and mice. Similar results were obtained with fenfluramine. MK-212 was not self-administered by rats, while the self-administration of amphetamine and morphine were demonstrated using the same experimental protocol.
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CAS 64022-27-1 MK212

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