Details
Stereochemistry | ACHIRAL |
Molecular Formula | C8H11ClN4.ClH |
Molecular Weight | 235.114 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.ClC1=CN=CC(=N1)N2CCNCC2
InChI
InChIKey=PFIZGLUIYAZQFU-UHFFFAOYSA-N
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
MK-212 is a 5HT2C-receptor agonist. It displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 uM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). 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.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Serotonergic drugs, benzodiazepines and baclofen block muscimol-induced myoclonic jerks in a strain of mice. | 1981 Jul 17 |
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Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. | 1993 Mar |
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Serotonin(2C) receptors appear to mediate genetic sensitivity to cocaine-induced convulsions. | 1999 Oct |
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Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors. | 2000 Feb |
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Modulation of 5-HT(2A) receptor-mediated head-twitch behaviour in the rat by 5-HT(2C) receptor agonists. | 2001 Jul-Aug |
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Activation of presynaptic 5-hydroxytryptamine 2A receptors facilitates excitatory synaptic transmission via protein kinase C in the dorsolateral septal nucleus. | 2002 Sep 1 |
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Hyperlocomotive and discriminative stimulus effects of cocaine are under the control of serotonin(2C) (5-HT(2C)) receptors in rat prefrontal cortex. | 2003 Aug |
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Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. | 2003 Sep |
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Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. | 2004 Aug |
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Anxiogenic effects in the rat elevated plus-maze of 5-HT(2C) agonists into ventral but not dorsal hippocampus. | 2004 Feb |
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Antiallodynic effects of intrathecally administered 5-HT(2C) receptor agonists in rats with nerve injury. | 2004 Mar |
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Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. | 2004 Sep |
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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. | 2005 Dec |
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Attenuation of nicotine's discriminative stimulus effects in rats and its locomotor activity effects in mice by serotonergic 5-HT2A/2C receptor agonists. | 2005 May |
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Behavioral effects of systemically administered MK-212 are prevented by ritanserin microinfusion into the basolateral amygdala of rats exposed to the elevated plus-maze. | 2005 Nov |
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Updated overview of the putative role of the serotoninergic system in obsessive-compulsive disorder. | 2005 Sep |
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Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities. | 2005 Sep 28 |
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Pharmacological characterization of 5-hydroxytryptamine-induced contraction in the chicken gastrointestinal tract. | 2006 Apr |
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5-HT receptor subtypes involved in the anxiogenic-like action and associated Fos response of acute fluoxetine treatment in rats. | 2006 Apr |
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Serotonin2C receptors (5-HT2C R) control expression of cocaine-induced conditioned hyperactivity. | 2006 Feb 28 |
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Possible involvement of spinal noradrenergic mechanisms in the antiallodynic effect of intrathecally administered 5-HT2C receptor agonists in the rats with peripheral nerve injury. | 2007 Jul 12 |
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Impact of RNA editing on functions of the serotonin 2C receptor in vivo. | 2010 |
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5-HT2C receptor agonists attenuate pain-related behaviour in a rat model of trigeminal neuropathic pain. | 2010 Nov |
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Spontaneous rhythmogenic capabilities of sympathetic neuronal assemblies in the rat spinal cord slice. | 2010 Oct 27 |
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Locomotor response to L-DOPA in reserpine-treated rats following central inhibition of aromatic L-amino acid decarboxylase: further evidence for non-dopaminergic actions of L-DOPA and its metabolites. | 2010 Sep |
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Stimulation of medial prefrontal cortex serotonin 2C (5-HT(2C)) receptors attenuates cocaine-seeking behavior. | 2010 Sep |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3365458
The effects of MK-212 (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 produced a dose-related increase in serum cortisol levels, with the 20- and 40-mg doses producing significant elevations. Serum prolactin levels were significantly elevated only by the 40-mg dose.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6122646
MK-212 (1 x 10(-7)M -- 1 x 10(-5)M) produced dose-dependent contractions of guinea pig ileum, taenia coil and rat fundus strip.
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DBSALT002137
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67250-10-6
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NON-SPECIFIC STOICHIOMETRY | |||
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DTXSID60210668
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8722D514RX
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262-883-0
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198421
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61655-58-1
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ACTIVE MOIETY
SUBSTANCE RECORD