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.
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- CAS No.: 1394867-58-3
- Formule: C28H25ClFN3OS
- Masse moléculaire:506.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
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Animal Model:Formalin test, writhing test, and diabetic neuropathic pain model established in CD-1 mice[1]
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Dosage:0.01, 0.03, 1 and 3 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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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.
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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]
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Dosage:0.3, 1 and 3 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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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
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CAS No. 1394867-58-3
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Masse moléculaire 506.03
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Formule C28H25ClFN3OS
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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)
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