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

RTI-122 dihydrochloride 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 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride 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 dihydrochloride

RTI-122 dihydrochloride Chemical Structure

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Based on 1 publication(s) in Google Scholar

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RTI-122 dihydrochloride Related Antibodies

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Description

RTI-122 dihydrochloride 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 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride 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 dihydrochloride 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 dihydrochloride (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 dihydrochloride 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 dihydrochloride (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 dihydrochloride (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 dihydrochloride Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax (Plasma) CL T1/2 AUC0-inf Tmax (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 4.0 h
In Vivo

RTI-122 (10 mg/kg; i.p.; single administration) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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 (male, 8−9 weeks of age)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced binge-like alcohol intake compared to saline controls, with magnitude matching that of reference compound RTI-13951-33 at 30 mg/kg dose.
Showed no effect on water intake.
Animal Model: C57BL/6J (male, 3-5 months old, 25-35 g)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose
Result: Reduced spontaneous locomotion dose-dependently during the first 20 min post-injection, with significant effects at 10 mg/kg and 20 mg/kg.
Reduced locomotion only at 20 mg/kg during the 20-40 min period.
Showed no effects on locomotion during the 40-60 min period.
Animal Model: alcohol-preferring (P) (male and female)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Reduced alcohol lever responses with significant reductions at 5 mg/kg and 10 mg/kg.
Reduced alcohol intake with significant reductions at 5 mg/kg and 10 mg/kg.
Reduced locomotor rate at 10 mg/kg during alcohol self-administration testing.
Showed no effect on sucrose lever responses or sucrose intake.
Reduced locomotor rate at 10 mg/kg during sucrose self-administration testing.
Reduced lever responding in the seeking phase at 20 mg/kg.
Reduced lever responding in the reinitiation phase at both 10 mg/kg and 20 mg/kg.
Reduced locomotor rate during the seeking phase at both doses.
Molecular Weight

564.52

Formula

C29H36Cl2FN3O3
Appearance

Solid

Color

White to light yellow

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.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (177.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7714 mL 8.8571 mL 17.7142 mL
5 mM 0.3543 mL 1.7714 mL 3.5428 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.7714 mL 8.8571 mL 17.7142 mL 44.2854 mL
5 mM 0.3543 mL 1.7714 mL 3.5428 mL 8.8571 mL
10 mM 0.1771 mL 0.8857 mL 1.7714 mL 4.4285 mL
15 mM 0.1181 mL 0.5905 mL 1.1809 mL 2.9524 mL
20 mM 0.0886 mL 0.4429 mL 0.8857 mL 2.2143 mL
25 mM 0.0709 mL 0.3543 mL 0.7086 mL 1.7714 mL
30 mM 0.0590 mL 0.2952 mL 0.5905 mL 1.4762 mL
40 mM 0.0443 mL 0.2214 mL 0.4429 mL 1.1071 mL
50 mM 0.0354 mL 0.1771 mL 0.3543 mL 0.8857 mL
60 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7381 mL
80 mM 0.0221 mL 0.1107 mL 0.2214 mL 0.5536 mL
100 mM 0.0177 mL 0.0886 mL 0.1771 mL 0.4429 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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RTI-122 dihydrochloride Related Classifications

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  • 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-122RTI122RTI 122GPR88G Protein-Coupled Receptor 88GPR88 agonistalcohol use disorderC57BL/6Jmicealcohol-preferring ratInhibitorinhibitorinhibit

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