RTI-13951-33
RTI-13951-33 性质
| 沸点 | 637.3±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.181±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 6.99±0.13(Predicted) |
RTI-13951-33 用途与合成方法
EC50: 25 nM (GPR88)
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).
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.
