2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 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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A-349821 Chemical Structure

A-349821 Chemical Structure

CAS No. : 556835-30-4

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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].

Molecular Weight

536.58

Formula

C28H35F3N2O5
CAS No.
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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A-349821 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

A-349821556835-30-4A349821A 349821Histamine ReceptorInhibitorinhibitorinhibit

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