Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C8H11ClN4 |
| Molecular Weight | 198.653 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=NC(=CN=C1)N2CCNCC2
InChI
InChIKey=CJAWPFJGFFNXQI-UHFFFAOYSA-N
InChI=1S/C8H11ClN4/c9-7-5-11-6-8(12-7)13-3-1-10-2-4-13/h5-6,10H,1-4H2
| Molecular Formula | C8H11ClN4 |
| Molecular Weight | 198.653 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|---|---|---|
| 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 |
|
| Hyperlocomotive and discriminative stimulus effects of cocaine are under the control of serotonin(2C) (5-HT(2C)) receptors in rat prefrontal cortex. | 2003 Aug |
|
| Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. | 2003 Sep |
|
| Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. | 2004 Aug |
|
| Anxiogenic effects in the rat elevated plus-maze of 5-HT(2C) agonists into ventral but not dorsal hippocampus. | 2004 Feb |
|
| Antiallodynic effects of intrathecally administered 5-HT(2C) receptor agonists in rats with nerve injury. | 2004 Mar |
|
| Contribution of serotonin (5-hydroxytryptamine; 5-HT) 5-HT2 receptor subtypes to the hyperlocomotor effects of cocaine: acute and chronic pharmacological analyses. | 2004 Sep |
|
| 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 |
|
| 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 |
|
| 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 |
|
| Updated overview of the putative role of the serotoninergic system in obsessive-compulsive disorder. | 2005 Sep |
|
| Inhibition of serotonin transporters by cocaine and meprylcaine through 5-TH2C receptor stimulation facilitates their seizure activities. | 2005 Sep 28 |
|
| Pharmacological characterization of 5-hydroxytryptamine-induced contraction in the chicken gastrointestinal tract. | 2006 Apr |
|
| 5-HT receptor subtypes involved in the anxiogenic-like action and associated Fos response of acute fluoxetine treatment in rats. | 2006 Apr |
|
| Serotonin2C receptors (5-HT2C R) control expression of cocaine-induced conditioned hyperactivity. | 2006 Feb 28 |
|
| 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 |
|
| Impact of RNA editing on functions of the serotonin 2C receptor in vivo. | 2010 |
|
| 5-HT2C receptor agonists attenuate pain-related behaviour in a rat model of trigeminal neuropathic pain. | 2010 Nov |
|
| Spontaneous rhythmogenic capabilities of sympathetic neuronal assemblies in the rat spinal cord slice. | 2010 Oct 27 |
|
| 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 |
|
| Stimulation of medial prefrontal cortex serotonin 2C (5-HT(2C)) receptors attenuates cocaine-seeking behavior. | 2010 Sep |
Sample Use Guides
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 19:42:14 GMT 2023
by
admin
on
Fri Dec 15 19:42:14 GMT 2023
|
| Record UNII |
62C3N7238U
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| Record Status |
Validated (UNII)
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| Record Version |
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64022-27-1
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DB12111
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62C3N7238U
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DTXSID80214007
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317326
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107992
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MK-212
Created by
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