A-349821
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists.
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- CAS No.: 556835-30-4
- Formule: C28H35F3N2O5
- Masse moléculaire:536.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Activité biologique
Chemical Information
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CAS No. 556835-30-4
-
Masse moléculaire 536.58
-
Formule C28H35F3N2O5
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SMILES
FC(F)(C(O)=O)F.C[C@H](CC[C@H]1C)N1CCCOC2=CC=C(C3=CC=C(C(N4CCOCC4)=O)C=C3)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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