MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
MPEP 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 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[3]. MPEP at 10 mg/kg significantly attenuated ethanol withdrawal induced anxiety without any compromising effects on locomotor activities. Despite reversing several indices of ethanol withdrawal induced anxiety in both the elevated plus maze and the open field, low doses of MPEP (2.5, 5 mg/kg) significantly compromised the locomotor activities of ethanol withdrawn rats. High doses of MPEP (20 and 30 mg/kg) significantly attenuated withdrawal anxiety when tested in the elevated plus maze but not in the open field. Administration of MPEP (2.5, 5, 10, 20, 30 mg/kg) has no significant compromising effect on the locomotor activities of ethanol naïve rats[4]. MPEP (10 and 30 mg/kg) significantly enhanced both the sedative and hypnotic effects of ethanol[5].
Mexico
... 展开 >> Asociacion Mexicana para la Salud Sexual, A.C.
Mexico City, Mexico D.F., Mexico, 14000
Centro Especializado en Urología y Andrología del Hospital Star Médica
Mexico City, Mexico D.F, Mexico, 06700 收起 <<
Mexico
... 展开 >> Asociacion Mexicana para la Salud Sexual, A.C.
Mexico City, Mexico D.F., Mexico, 14000
Centro Especializado en Urología y Andrología del Hospital Star Médica
Mexico City, Mexico D.F, Mexico, 06700 收起 <<
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