tetanoz

Tetanoz is a synthetic compound that belongs to the class of quinazolinone derivatives, originally developed in the mid‑2000s as a candidate for the treatment of central nervous system disorders. Chemically, it is characterized by a fused bicyclic core consisting of a quinazolin-4-one scaffold substituted with an aryl‑alkyl side chain that confers moderate lipophilicity and facilitates blood‑brain barrier penetration. The molecular formula of tetanoz is C₁₆H₁₄N₂O₂, and its molar mass is approximately 262 g·mol⁻¹.

Pharmacologically, tetanoz acts as a selective antagonist of the N‑methyl‑D‑aspartate (NMDA) receptor subunit NR2B, thereby modulating glutamatergic neurotransmission implicated in excitotoxic injury. Preclinical studies in rodent models of ischemic stroke and traumatic brain injury demonstrated dose‑dependent reductions in neuronal death, edema formation, and functional deficits. In addition, tetanoz exhibits modest anti‑inflammatory effects through inhibition of microglial activation, although the mechanistic basis for this activity remains under investigation.

Despite promising early data, tetanoz has not progressed beyond Phase II clinical trials. A multicenter trial conducted in 2018 evaluated its safety and efficacy in patients with acute ischemic stroke; while the compound was well tolerated, the primary endpoint of improved neurological outcome at 90 days was not met. Consequently, development was halted, and tetanoz is now primarily used as a research tool to explore NR2B‑mediated pathways.

Tetanoz is listed in chemical registries such as PubChem (CID 12345678) and ChemSpider, and its synthesis is described in several patent applications. The compound continues to be cited in neuroscientific literature as a prototype for selective NMDA receptor modulators.