Des dérivés simples de la glycine aux systèmes lipidiques transporteurs de glycine : essai de vectorisation d'un acide aminé neutre de petite taille vers le système nerveux central
(1994)
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- Abstract
- The design of 1,3-diacylaminopropan-2-ols as CNS-directed carrier groups is based on their resemblance to endogenous lipids and the properties of pseudotriglyceride esters to facilitate the brain penetration of therapeutic agents. É-[S-acethylthiropan-1,3-diacylaminopropan-2-ols, differing from the nature of 1,3-acyl chains, were synthsized anf evaluated in vivo using the hot-plate jump test. The compounds exhibited naloxone reversible analgesic properties. The effects were superior to those of parent compounds thiorpan and S-acetylthiorphan. The palmitoyl derivative showed also activity at 0.8 mmlo/kg after oral administration. Like acetrophan, a thriophan prodrug, these compounds were poor susbtrates for brain enkephalinase, suggesting the release of the pharmacological active inhibitor at the site of action in the brain
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Lambert, D. M. (1994). Des dérivés simples de la glycine aux systèmes lipidiques transporteurs de glycine : essai de vectorisation d’un acide aminé neutre de petite taille vers le système nerveux central. https://hdl.handle.net/2078.5/111272