TASP0433864 is a novel positive allosteric modulator of metabotropic glutamate 2 receptor. TASP0433864 exhibited PAM activity at human and rat mGlu2 receptors with EC50 of 199 and 206 nM, respectively, without exerting agonist activity at rat mGlu2 receptor. TASP0433864 produced a leftward and upward shift in the concentration-response curve of glutamate-increased guanosine 5'-O-(3-[(35)S]thio)triphosphate binding to mGlu2 receptor. The inhibitory effect of TASP0433864 on cortical activation was also observed in the mouse 2-deoxy-glucose uptake study. TASP0433864 is a selective mGlu2 receptor PAM with antipsychotic activity, and the attenuation of excess glutamatergic neurotransmission may be involved in the action of TASP0433864. References: Hiyoshi T, Marumo T, Hikichi H, Tomishima Y, Urabe H, Tamita T, Iida I, Yasuhara A, Karasawa J, Chaki S. Neurophysiologic and antipsychotic profiles of TASP0433864, a novel positive allosteric modulator of metabotropic glutamate 2 receptor. J Pharmacol Exp Ther. 2014 Dec;351(3):642-53. doi: 10.1124/jpet.114.218651. PubMed PMID: 25277141.

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CAS：1431980-60-7