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2244884-08-8

中文名稱(chēng) RTI-13951-33
英文名稱(chēng) RTI-13951-33
CAS 2244884-08-8
分子式 C28H33N3O3
分子量 459.58
MOL 文件 2244884-08-8.mol
2244884-08-8 結(jié)構(gòu)式 2244884-08-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12778L
英文別名
RTI-13951-33
RTI1395133,RTI 13951 33

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜

常見(jiàn)問(wèn)題列表

生物活性
RTI-13951-33 是一種有效、選擇性、可透過(guò)血腦屏障的 GPR88 激動(dòng)劑,在 GPR88 cAMP 功能性實(shí)驗(yàn)中,EC50 值為 25 nM。RTI-13951-33 可以減少大鼠酒精強(qiáng)化和攝取行為。
靶點(diǎn)

EC50: 25 nM (GPR88)

體外研究

RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC 50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [ 35 S]-GTPγS binding (EC 50 , 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice.
RTI-13951-33 has weak affinities at kappa opioid receptor (KOR; K i , 2.29 μM), vesicular monoamine transporter (VMAT; K i , 4.23 μM), and moderate affinity at serotonin transporter (SERT; K i , 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC 50 , 25.1 ± 2.7 μM).

體內(nèi)研究

RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t 1/2 of 48 min and 87 min in rat plasma and brain.
RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration.

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