2. GPCR/G Protein
  3. GPR52
  4. R-185

R-185 is an orally active and brain-penetrant GPR52 agonist. R-185 activates GPR52 to increase intracellular cAMP levels. R-185 can be used for the research of schizophrenia.

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R-185

R-185 Chemical Structure

CAS No. : 3066783-67-0

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R-185 Related Antibodies

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Description

R-185 is an orally active and brain-penetrant GPR52 agonist. R-185 activates GPR52 to increase intracellular cAMP levels. R-185 can be used for the research of schizophrenia[1].

In Vitro

R-185 (Compound 14h) potently activates human GPR52 in HEK293 cells transiently expressing the receptor, with an EC50 of 26 nM and an Emax of 87%[1].

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

R-185 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-∞ T1/2 Cmax CL Vd F
Mice[1] 5 mg/kg p.o. 3232 ng·h/mL 1.76 h 1173 ng/mL / / 130 %
Mice[1] 1 mg/kg i.v. 496 ng·h/mL 1.40 h 1283 ng/mL 33.8 mL/min/kg 1.74 L/kg /
Rat[1] 5 mg/kg p.o. 2284 ng·h/mL 3.53 h 318 ng/mL / 4.40 L/kg 67 %
Rat[1] 1 mg/kg i.v. 680 ng·h/mL 2.05 h 760 ng/mL 24.8 mL/min/kg / /
In Vivo

R-185 (Compound 14h) (1-5 μM) dose-dependently inhibits MK-801 (HY-15084B)-induced hyperlocomotion in zebrafish larvae, with near-complete activity normalization at the 5 μM dose[1].
R-185 (1-5 mg/kg; p.o. or i.v.; single dose) exhibits favorable pharmacokinetic characteristics in mice, crosses the blood-brain barrier, and has an oral bioavailability of 130%[1].
R-185 (1-5 mg/kg; p.o. or i.v.; single dose) exhibits favorable pharmacokinetic characteristics in rats, crosses the blood-brain barrier, and has an oral bioavailability of 67%[1].

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

Animal Model: SD mice (male, 30 g)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: p.o. or i.v.; single dose
Result: Exihibited favorable pharmacokinetic characteristics and could cross the blood-brain barrier.
Showed F of 130%, Cmax of 1173 ng/mL, Tmax of 1.76 h and AUC0-∞ of 3232 ng·h/mL (p.o.).
Showed T1/2 of 1.40 h, CL of 33.8 mL/min/kg, Vd of 1.74 L/kg and AUC0-∞ of 496 ng·h/mL (i.v.).
Animal Model: SD rats (male, 200-250 g)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: p.o. or i.v.; single dose
Result: Exihibited favorable pharmacokinetic characteristics and could cross the blood-brain barrier.
Exhibited F of 67%, Cmax of 318 ng/mL, Tmax of 3.53 h and AUC0-∞ of 2284 ng·h/mL.
Exhibited T1/2 of 2.05 h, CL of 24.8 mL/min/kg, Vd of 4.4 L/kg and AUC0-∞ of 680 ng·h/mL.
Molecular Weight

461.41

Formula

C22H19F4N5O2
CAS No.
SMILES

FC1=CC(OC2CCN(CC2)C3=C(N=CC=N3)C(NC4=CC=NC=C4)=O)=CC(C(F)(F)F)=C1
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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R-185 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:

R-1853066783-67-0R185R 185GPR52G Protein-Coupled Receptor 52schizophreniaHEK293 cellsintracellular cAMPG protein-coupled receptor 52MK-801zebrafish larvaehuman GPR52Inhibitorinhibitorinhibit

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