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Description: JNJ16259685 is a novel, potent, selective and non-competitive antagonist of mGlu1 receptor with IC50 of 19 nM. It inhibits the synaptic activation of mGlu1 in a concentration-dependent manner. JNJ16259685 produced very minimal effects on locomotor activity and posture up to a dose of 30 mg/kg. Motor skill was unaffected for well-learned tasks (up to 30 mg/kg) in rats, but impaired in mice. Both rats and mice rats were profoundly impaired (0.3 mg/kg) in the acquisition of a novel motor skill (rotarod).
References: Eur J Pharmacol. 2008 May 31; 586(1-3):217-20; Pharmacol Biochem Behav. 2011 Apr; 98(2):181-7; Neuropharmacology. 2004 Dec; 47(7):961-72..
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