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RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,820 | 8-10 weeks | |
50 mg | $2,380 | 8-10 weeks | |
100 mg | $3,100 | 8-10 weeks |
Description | RTI-13951-33 is an effective and brain-penetrant GPR88 agonist (EC50: 25 nM, in GPR88 cAMP functional assay). |
Targets&IC50 | GPR88:(EC50)25 nM |
In vitro | RTI-13951-33 poorly inhibits SERT (IC50: 25.1 ± 2.7 μM). RTI-13951-33 elevates [35S]-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) [1]. |
In vivo | RTI-13951-33 (10 and 20 mg/kg, i.p.) dose-dependently reduces alcohol lever responses in a rat model of alcohol self-administration. RTI-13951-33 (10 mg/kg, i.p.) has sufficient brain penetration, with t1/2 of 48 min and 87 min in rat plasma and brain [1]. |
Molecular Weight | 459.58 |
Formula | C28H33N3O3 |
Cas No. | 2244884-08-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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