2. GPCR/G Protein
  3. GPR52
  4. GPR52 agonist-1

GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.

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GPR52 agonist-1 Chemical Structure

GPR52 agonist-1 Chemical Structure

CAS No. : 1207965-40-9

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GPR52 agonist-1 Related Antibodies

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Description

GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity[1].

IC50 & Target

pEC50: 7.53 (GPR52)[1]
In Vivo

GPR52 agonist-1 (compound 7m) (3, 10, and 30 mg/kg; PO; single dosage) attenuates Methamphetamine-induced hyperlocomotion in mice[1].
GPR52 agonist-1 (0.1 mg/kg, IV and 1 mg/kg, PO; single dosage) exhibits good oral pharmacokinetic profile with an Cmax of 108.1 ng/mL, an AUC0-8h of 613.7 ng·h/mL, and an F (bioavailability) of 73% in mouse[1].

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

Animal Model: Male ICR mice (7-8 weeks; subcutaneously injected with 2 mg/kg Methamphetamine after 60 min administration)[1]
Dosage: 3, 10, and 30 mg/kg
Administration: PO; single dosage
Result: Attenuated Methamphetamine-induced hyperlocomotion dose-dependently.
Did not show significant cataleptogenic effects even at a dose of 100 mg/kg and had a low risk of extrapyramidal side effects.
Molecular Weight

453.96

Formula

C25H21ClFNO2S
CAS No.
SMILES

COCCNC(C1=CC(C2=C3SC(CC4=CC(Cl)=CC(F)=C4)=CC3=CC=C2)=CC=C1)=O
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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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GPR52 agonist-1 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:

GPR52 agonist-11207965-40-9GPR52G Protein-Coupled Receptor 52orally activeblood-brain barrierBBBcAMP accumulationhyperactivityantipsychoticICR miceInhibitorinhibitorinhibit

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