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α-NAPAP (alpha-NAPAP) is a highly potent, selective, and competitive small-molecule direct thrombin inhibitor. It reversibly binds to the active site of thrombin, mimicking the basic amino acid residues (arginine and lysine) typically cleaved by trypsin-like serine proteases. In preclinical research, α-NAPAP is widely utilized as an anticoagulant and neuroprotective agent. It has been shown to significantly reduce brain edema, blood-brain barrier breakdown, and seizure activity in animal models of status epilepticus, traumatic brain injury, and intracerebral hemorrhage by blocking thrombin-mediated activation of protease-activated receptor 1 (PAR1).
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