TASP 0433864 |
カタログ番号GC50150 |
TASP 0433864 は、代謝型グルタミン酸 2 (mGlu2) 受容体の選択的ポジティブ アロステリック モジュレーター (PAM) であり、EC50 値は、ヒトおよびラットの mGlu2 受容体に対してそれぞれ 199 nM および 206 nM です。
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Cas No.: 1431980-60-7
Sample solution is provided at 25 µL, 10mM.
Selective mGlu2 receptor positive allosteric modulator (EC50 values are 199 and 206 nM for human and rat receptors, respectively). Exhibits negligible activity against a range of neurotransmitter targets, except 5-HT2B and MAO-B (72 and 92% inhibition at 10 μM, respectively). Potentiates inhibitory effect of DCG IV on excitatory postsynaptic potentials in hippocampal slices and ketamine- and methamphetamine-induced increases in locomotor activity in rats and mice.
Hiyoshi et al (2014) Neurophysiologic and antipsychotic profiles of TASP0433864, a novel positive allosteric modulator of metabotropic glutamate 2 receptor. J.Pharmacol.Exp.Ther. 351 642 PMID:25277141
Average Rating: 5
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