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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
Structure of MK-212

SMILES

ClC1=CN=CC(=N1)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

HIDE SMILES / InChI

Description

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.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
28.0 nM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
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
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.