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H3R antagonist 6

H3R antagonist 6 (Compounds 3) (H3-2406) is a Histamine receptor 3 (H3R) antagonist with an IC50 of 5.6 nM. H3R antagonist 6 labeled with 18F has high radiochemical yield, molar activity and moderate brain uptake, but with an off-target binding to the Sigma-1 receptor. H3R antagonist 6 can be used as a PET radioligand for positron emission tomography imaging for central nervous system (CNS) disorders research[1].

Product Specifications

CAS Number

[2183338-59-0]

UNSPSC

12352005

Target

Histamine Receptor; Sigma Receptor

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=C(N1CCN(C2CCCC2)CC1)[C@@H]3[C@@H](C4=CC=C(F)C=C4)C3

Molecular Formula

C19H25FN2O

Molecular Weight

316.41

References & Citations

[1]Song Z, et al. Development and Preclinical Characterization of [18F]H3-2406 and [18F]H3-2407 for Positron Emission Tomography Imaging of the Histamine Subtype-3 Receptor. J Med Chem. 2025 Jul 15.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

H3 Receptor; Sigma 1 Receptor

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