N-Acetylcysteine Amide

amino-acid · nervous · Oral · IV · Transdermal

N-Acetylcysteine Amide, an amino acid. The carboxylate of NAC is replaced with an amide — neutralises the molecule's negative charge, producing a lipophilic thiol…

The carboxylate of NAC is replaced with an amide — neutralises the molecule's negative charge, producing a lipophilic thiol that crosses membranes (including the blood-brain barrier) 4–5× more efficiently than NAC. In vivo it is hydrolysed by amidases to NAC and thence to cysteine, feeding glutathione synthesis. Also acts directly as a free-thiol antioxidant and Cu²⁺ chelator in the CNS. Investigated for CNS oxidative-stress indications (traumatic brain injury, retinal degeneration, Parkinson's models) and for GSH-depleted states where NAC penetration is limiting. Murine PK (He 2020): IV Cmax ~250 µg/mL, t½ ~1 h; oral F ~10%.

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Sources: PMID:31740394