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.
For research use only. We do not sell to patients.
- CAS No.: 1394867-58-3
- Formula: C28H25ClFN3OS
- Molecular Weight:506.03
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Adenosine Receptor Isoforms
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Biological Activity
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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Molecular Weight 506.03
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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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