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CAS No. : 825658-63-7
MCE 国际站:RTI-7470-44
产品活性:RTI-7470-44 是一种有效且具有选择性和血脑屏障透过性的人微量胺相关受体 1 (hTAAR1) 拮抗剂,IC50 为 8.4 nM。RTI-7470-44 具有中等的代谢稳定性和良好的初步脱靶谱。RTI-7470-44 可增加小鼠中脑腹侧被盖区 (VTA) 多巴胺能神经元的自发放电率。RTI-7470-44 可用于精神分裂症、活性分子成瘾和帕金森病 (PD) 的研究。
研究领域:Others
作用靶点:Others
In Vitro: RTI-7470-44 (10 μM) shows little to no off-target activity with the exception of the benzylpiperazine (BZP) rat brain site and human sigma 2 with inhibition of 75 and 90%, respectively; has a moderate affinity for the BZP rat brain site (Ki=1 μM) and a very weak affinity for human sigma 2 (Ki=8.4 μM).
In Vivo: RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist).
RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes.
Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes.
species | half-life (min) | clearance, CLINT (mL/min/mg) |
Human | 83.9 | 14.9 |
Rat | 9.11 | 274 |
Mouse | 65.8 | 63.5 |
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