PeptideDB

MPEP Hydrochloride

CAS: 219911-35-0 F: C14H12ClN W: 229.70

MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagoni
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects[1][2].
Invitro MPEP does not show agonist or antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μM on the human mGlu6 receptor[1].
In Vivo MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice[2].MPEP (1-20 mg/kg) does shorten the immobility time in a tail suspension test in mice, however it is inactive in the behavioural despair test in rats[2].MPEP (30 mg/kg i.p.) slightly but significantly increases (by 39%) the number of punished crossings in the four-plate test, lower doses of the compound (3 and 10 mg/kg) does not affect the number of punished crossings in that test (F (3,36)=3.240, P<0.05)[2]. MPEP (1, 10 and 20 mg/kg) significantly (by 55% after the highest dose), (F(3,28)=15.47, P<0.001) decreases the immobility time of mice in the tail suspension test. Its efficacy is similar to that of imipramine (20 mg/kg), used as the positive standard[2]. Animal Model:
Name MPEP Hydrochloride
CAS 219911-35-0
Formula C14H12ClN
Molar Mass 229.70
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [1]. F Gasparini, et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a Potent, Selective and Systemically Active mGlu5 Receptor Antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503. [2]. E Tatarczyńska, et al. Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. Br J Pharmacol. 2001 Apr;132(7):1423-30.