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PNU-120596
- Development stage
- Preclinical
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Intravenous, Subcutaneous, Intraperitoneal, Oral
01
Overview
PNU-120596 is a potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptor (α7nAChR). It acts by increasing the probability of channel opening and significantly slowing the rate of receptor desensitization, thereby enhancing cholinergic signaling. Originally developed by Pharmacia & Upjohn (now Pfizer), the compound is widely utilized as a research tool to investigate the therapeutic potential of α7nAChR modulation in cognitive disorders, chronic pain, and inflammatory conditions. Recent research presented at the EHA 2026 Congress highlights its potential role in allogeneic hematopoietic stem cell transplantation (allo-HSCT), where it appears to restrain T cell activation and expansion, suggesting a possible application in the prophylaxis or treatment of Graft-versus-Host Disease (GVHD).
- Other names
- 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea
02
Targets
CHRNA7 (α7 nicotinic receptor)LGCC (Ligand-gated chloride-selective channel of Lymnaea stagnalis)RK (Ribokinase)
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