MK-212
MK-212 (CPP) is an orally active, blood-brain barrier permeable agonist of 5-HT1C, 5-HT2 and 5-HT1A receptors. MK-212 induces hyperthermia, nausea, arousal, irritability and restlessness, inhibits the elevation of plasma cortisol and prolactin, and reduces feelings of calmness and overall positive affect. MK-212 mediates anxiety-like behaviors and motor inhibition. MK-212 is applicable to research related to schizophrenia and anxiety disorders.
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- CAS No.: 64022-27-1
- Formule: C8H11ClN4
- Masse moléculaire:198.65
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT1C Receptor |
5-HT2 Receptor |
5-HT1A Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.028 μM
Compound: MK-212
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Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
|
[PMID: 23301527] |
| HEK293 | EC50 |
0.16 μM
Compound: MK-212
|
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
|
[PMID: 23301527] |
| HEK293 | EC50 |
0.42 μM
Compound: MK-212
|
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
|
[PMID: 23301527] |
| HEK293 | EC50 |
1.2 μM
Compound: MK-212
|
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
|
[PMID: 23301527] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 200-290 g)[2]
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Dosage:1.0 mg/kg; 2.0 mg/kg; 4.0 mg/kg
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Administration:i.p.; single injection
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Result:Decreased the percentage of open-arm entries and the percentage of time spent in open arms at 2.0 mg/kg and 4.0 mg/kg doses compared to saline controls.
Decreased the absolute number of closed-arm entries at 4.0 mg/kg dose compared to saline controls.
Showed no significant effect on any measured parameter at 1.0 mg/kg dose.
Confirmed anxiogenic effects of 2.0 mg/kg and 4.0 mg/kg doses remained significant when controlling for closed-arm entries via ANCOVA.
Decreased the number of floor crossings from 78 in saline controls to 17 at 4.0 mg/kg dose compared to saline controls.
Decreased rearings from 18 in saline controls to 9 at 4.0 mg/kg dose compared to saline controls.
Showed no significant effect on either locomotor measure at 1.0 mg/kg and 2.0 mg/kg doses.
Decreased the percentage of open-arm entries and the percentage of time spent in open arms compared to saline-pretreated controls when paired with vehicle or 0.5 μg ritanserin microinfusions into the basolateral amygdala.
Had anxiogenic effect dose-dependently prevented by ritanserin microinfusions at doses of 1.25 μg, 2.5 μg, and 5.0 μg into the basolateral amygdala, with no significant differences between MK-212-pretreated and saline-pretreated groups at these higher ritanserin doses.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 64022-27-1
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Appearance Solid
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Masse moléculaire 198.65
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Formule C8H11ClN4
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SMILES
ClC1=NC(N2CCNCC2)=CN=C1
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Synonyms
CPP
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
Références
[1]. Lee HS, et al. Effect of the serotonin agonist, MK-212, on body temperature in schizophrenia. Biol Psychiatry. 1992 Mar 1;31(5):460-70. [Content Brief]
[2]. de Mello Cruz AP, et al. 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. 2005 Nov;182(3):345-54. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-212 Related Classifications
HY-101324 Related Classifications
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