2244884-08-8
2244884-08-8 structure
- Name: RTI-13951-33
- Chemical Name: RTI-13951-33
- CAS Number: 2244884-08-8
- Molecular Formula: C28H33N3O3
- Molecular Weight: 459.58
- Catalog: Research Areas Neurological Disease
- Create Date: 2019-02-13 06:21:16
- Modify Date: 2024-01-03 18:50:17
-
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].
| Name | RTI-13951-33 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
EC50: 25 nM (GPR88)[1] |
| In Vitro | 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; 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)[1]. |
| In Vivo | 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]. 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]. |
| References |
| Molecular Formula | C28H33N3O3 |
|---|---|
| Molecular Weight | 459.58 |