2. GPCR/G Protein
  3. GPR88
  4. RTI-122

RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder.

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RTI-122

RTI-122 Chemical Structure

CAS No. : 3034664-39-3

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Description

RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder[1][2].

In Vitro

RTI-122 potently activates human GPR88 in CHO cells stably expressing PPLS-HA-GPR88, with an EC50 of 10.8 nM for cAMP at 30 min; it also potently activates the G protein signaling pathway of human GPR88 in PPLS-HA-hGPR88-CHO cell membranes, with an EC50 of 11.5 nM for [35S]GTPγS at 60 min[1].
RTI-122 (30 μM; 60 min) shows no activity in striatal membranes from GPR88 knockout mice, but selectively activates endogenous mouse GPR88 in striatal membranes from wild-type mice, with an EC50 of 155 nM for [35S]GTPγS[1].
RTI-122 exhibits favorable metabolic stability in mouse liver microsomes, with a half-life of 24.6 min and a clearance rate of 56.4 μL/min/mg[1].
RTI-122 (10 μM; 90 min) exhibits favorable blood-brain barrier penetration potential, with an apical-to-basolateral Papp of 2.8 × 10-6 cm/s and an efflux ratio of 2.5 in the MDCK-MDR1 assay[1].
RTI-122 (1 μM; 6 h) binds highly to mouse plasma proteins, with a binding rate of 99.5%[1].

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

RTI-122 Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration Tmax (Plasma) CLplasma T1/2 (Plasma) AUC0-∞ (Plasma) Brain Concentration Tmax (Brain) CLbrain T1/2 (Brain) AUC0-∞ (Brain)
Mice[1] 10 mg/kg i.p. 662 ng/mL 2.0 h 23 mL/min/kg 5.8 h 7292 ng·h/mL 630 ng/mL 4.0 h 20 mL/min/kg 5.5 h 8530 ng·h/mL
In Vivo

RTI-122 (10 mg/kg; i.p.; single administration) significantly attenuates binge-like drinking behavior in male C57BL/6J mice, with an efficacy comparable to that of 30 mg/kg RTI-13951-33 (HY-112612)[1].
RTI-122 (10-20 mg/kg; i.p.; single administration) reduces spontaneous locomotor activity in male C57BL/6J mice in a dose-dependent manner. Within the first 20 min post-injection, both the 10 mg/kg and 20 mg/kg groups exhibit efficacy, while only the 20 mg/kg group shows efficacy during the 20-40 min period[2].
RTI-122 (10-20 mg/kg; i.p.; single administration) induces GPR88-specific reduction of alcohol intake in wild-type mice. Both 10 mg/kg and 20 mg/kg doses are effective in male mice, while only the 20 mg/kg dose is effective in female mice[2].
RTI-122 (5-10 mg/kg; i.p.; single administration) dose-dependently reduces operant alcohol self-administration in alcohol-preferring male and female rats, with no effect on sucrose self-administration, indicating its regulatory role in alcohol-specific reward[2].
RTI-122 (2.5-10 mg/kg; i.p.; single administration) reduces the motivation of alcohol-preferring male and female rats to self-administer unadulterated alcohol and quinine (HY-D0143)-adulterated alcohol[2].
RTI-122 (20 mg/kg; i.p.; single administration) reduces yohimbine (HY-N0127)-induced alcohol-seeking behavior in both male and female alcohol-preferring rats, and inhibits relapse of alcohol self-administration in both sexes at doses of 10 mg/kg and 20 mg/kg[2].

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

Animal Model: C57BL/6J mice with Alcohol use disorder (male)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Produced significant attenuation of binge-like alcohol consumption, with effects equivalent to those of RTI-13951-33 at 30 mg/kg.
Showed no effect on water intake.
Confirmed significant effect compared to saline-treated mice via Newman-Keuls post hoc testing.
Animal Model: Alcohol-preferring Rat (male and female, progressive ratio operant self-administration for unadulterated and quinine-adulterated 15% alcohol)[2]
Dosage: 2.5 mg/kg (unadulterated and quinine-adulterated alcohol); 5 mg/kg (unadulterated and quinine-adulterated alcohol); 10 mg/kg (unadulterated alcohol)
Administration: i.p.; single dose per test session
Result: Reduced break point and alcohol intake for unadulterated alcohol at 5 mg/kg and 10 mg/kg.
Reduced locomotor rate for unadulterated alcohol at all tested doses.
Reduced break point for quinine-adulterated alcohol at 5 mg/kg.
Reduced alcohol intake in females for quinine-adulterated alcohol at 2.5 mg/kg and 5 mg/kg.
Reduced locomotor rate in females for quinine-adulterated alcohol at both 2.5 mg/kg and 5 mg/kg, and in males at 2.5 mg/kg.
Animal Model: Alcohol-preferring Rat (male and female, yohimbine-induced reinstatement of alcohol-seeking and self-administration following 16 extinction sessions)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose per test session
Result: Reduced alcohol-seeking lever responses in the seeking phase at 20 mg/kg.
Reduced alcohol self-administration lever responses in the reinitiation phase at 10 mg/kg and 20 mg/kg.
Reduced locomotor rate during the seeking phase at both 10 mg/kg and 20 mg/kg.
Showed no effect on locomotor rate during the reinitiation phase.
Molecular Weight

491.60

Formula

C29H34FN3O3
CAS No.
SMILES

CO[C@H](C)[C@H](N)CN(C1=CC=C(C2=CC=C(C=C2)OC(C)C)C=C1)C([C@H]3[C@H](C4=CC=C(C=N4)F)C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RTI-122 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RTI-1223034664-39-3RTI122RTI 122GPR88G Protein-Coupled Receptor 88G protein activityPPLS-HA-GPR88 CHO cellsMDCK-MDR1 assayC57BL/6J micealcohol use disorderwild-type mouse striatal membranesmouse liver microsomescAMP signalingGPR88 knockout mouse striatal membranesInhibitorinhibitorinhibit

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