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A-349821

CAT: 0804-HY-12193Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-12193Size:1 Each
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Description
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[1].
CAS Number
556835-30-4
UNSPSC
12352005
Target
Histamine Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling
Field of Research
Others
Assay Protocol
https://www.medchemexpress.com/a-349821.html
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
Molecular Formula
C28H35F3N2O5
Molecular Weight
536.58
References & Citations
[1]Use of the H3 receptor antagonist radioligand [ 3 H]-A-349821 to reveal in vivo receptor occupancy of cognition enhancing H3 receptor antagonist
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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CatalogName
GTR19210828-01A-349821

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