RTI-13951-33 

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 reduces alcohol reinforcement and intake behaviors in rats^[1].

EC50: 25 nM (GPR88)^[1]

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 [³⁵S]-GTPγS binding (EC₅₀， 535 nM) in mouse striatal membranes but not in membranes from GPR88 KO mice^[1].
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 (IC₅₀, 25.1 ± 2.7 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently decreases alcohol lever responses in a rat model of alcohol self-administration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

459.58

C₂₈H₃₃N₃O₃

2244884-08-8

COCC1=CC=C(C2=CC=C(N(C[C@@H](N)[C@@H](C)OC)C([C@H]3[C@H](C4=CC=CC=N4)C3)=O)C=C2)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]