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H3-2401
- Development stage
- Preclinical
- Lead developer
- Emory University
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
H3-2401 is a novel piperazine-based dual-targeting small molecule ligand that acts as an antagonist of the histamine H3 receptor (H3R) and a modulator of the sigma-1 receptor (σ1R). Derived from the structure of the selective H3R antagonist AZD5213, H3-2401 was developed by Emory University in collaboration with AstraZeneca and Karolinska Institutet. When radiolabeled with fluorine-18 to form [18F]H3-2401, it serves as a positron emission tomography (PET) imaging tracer with high brain penetration, favorable pharmacokinetics, and excellent specificity. Preclinical studies in mouse models of spared nerve injury (SNI) and in non-human primates have demonstrated its selective accumulation in pain-associated neural tissues, highlighting its potential both as a diagnostic imaging agent and as a therapeutic candidate for the treatment of neuropathic pain.
- Other names
- 18F-H3-2401F-18 H3-2401F18 H3-2401F 18 H3-2401[18F]H3-2401
02
Targets
HRH3 (Histamine Receptor H3)SIGMAR1 (Sigma non-opioid intracellular receptor 1)
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