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.
For research use only. We do not sell to patients.
- CAS No.: 556835-30-4
- Formula: C28H35F3N2O5
- Molecular Weight:536.58
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Histamine Receptor Isoforms
More
Biological Activity
Chemical Information
-
CAS No. 556835-30-4
-
Molecular Weight 536.58
-
Formula C28H35F3N2O5
-
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
-
Shipping
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz