TRR469
TRR469 is a positive allosteric modulator of the A1 adenosine receptor (A1AR). TRR469 significantly increases the affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A₁AR, increasing the number of receptors recognized by the agonist radioligand [³H]-CCPA. TRR469 shows significant effects in both anxiety and pain models. TRR469 can be used to study anxiety disorders and pain management.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1394867-58-3
- Fòrmula: C28H25ClFN3OS
- Peso molecular:506.03
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas Adenosine Receptor
More
Actividad biológica
TRR469 (10 μM) inhibits the release of excitatory neurotransmitters by enhancing the activation of A₁AR in the spinal cord of mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TRR469 (0.3-3 mg/kg, i.p., single dose) demonstrates dose-dependent anti-anxiety effects in all four anxiety models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Formalin test, writhing test, and diabetic neuropathic pain model established in CD-1 mice[1]
-
Dosage:0.01, 0.03, 1 and 3 mg/kg
-
Administration:Intraperitoneal injection (i.p.), single dose
-
Result:Showed dose-dependent analgesic effect with ED50s of 0.257 and 0.171 mg/kg in formalin test and writhing test.
Dose-dependent reversaled mechanical abnormal pain.
-
Animal Model:Elevated cross maze test, the light-dark box test, the opening test and the buried pearl test established in CD-1 mice[2]
-
Dosage:0.3, 1 and 3 mg/kg
-
Administration:Intraperitoneal injection (i.p.), single dose
-
Result:Demonstrated dose-dependent anti-anxiety effects in all four anxiety models.
Did not enhance the sedative effect of ethanol, nor does it impair the motor coordination function.
Chemical Information
-
No. CAS 1394867-58-3
-
Peso molecular 506.03
-
Fòrmula C28H25ClFN3OS
-
SMILES
O=C(C1=C(N)SC(C2=CC=C(F)C=C2)=C1CN3CCN(C4=CC=CC=C4)CC3)C5=CC=C(Cl)C=C5
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Vincenzi F, et al. TRR469, a potent A(1) adenosine receptor allosteric modulator, exhibits anti-nociceptive properties in acute and neuropathic pain models in mice. Neuropharmacology. 2014 Jun;81:6-14. [Content Brief]
[2]. Vincenzi F, et al. Positive allosteric modulation of A1 adenosine receptors as a novel and promising therapeutic strategy for anxiety. Neuropharmacology. 2016 Dec;111:283-292. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRR469 Related Classifications
HY-112567 Related Classifications
Powered by Bioz