TASP 0433864 是一种代谢型谷氨酸 2 (mGlu2) 受体的选择性正变构调节剂 (PAM)，对人和大鼠 mGlu2 受体的 EC50 值分别为 199 nM 和 206 nM。
| Cas No. | 1431980-60-7 |
| Canonical SMILES | CC(C)(C)C1=CC=C(OC[C@@H]2CN3C(O2)=NC(C(N)=O)=C3C)C=C1 |
| 分子式 | C18H23N3O3 |
| 分子量 | 329.39 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 |
