RTI-13951-33 hydrochloride 是一种有效、选择性、可透过血脑屏障的 GPR88 激动剂，在 GPR88 cAMP 功能性实验中，EC₅₀ 值为 25 nM。RTI-13951-33 hydrochloride 可以减少大鼠酒精强化和摄取行为。

RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC 50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.

Solid

EC50: 25 nM (GPR88)

RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 elevates [S]-GTPγS binding (EC50, 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; Ki, 2.29 μM), vesicular monoamine transporter (VMAT; Ki, 4.23 μM), and moderate affinity at serotonin transporter (SERT; Ki, 0.75 μM), however, RTI-13951-33 poorly inhibits SERT (IC50, 25.1±2.7 μM). has not independently confirmed the accuracy of these methods. They are for reference only.

RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Jin C, et al. Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake. J Med Chem. 2018 Aug 9;61(15):6748-6758.

In Vitro: DMSO : 50 mg/mL (93.90 mM; Need ultrasonic)H₂O : 50 mg/mL (93.90 mM; Need ultrasonic)配制储备液