Tyr¹-ψ[( Z)CF═CH]-Gly² Fluorinated Peptidomimetic Improves Distribution and Metabolism Properties of Leu-Enkephalin.

ABSTRACT: Opioid peptides are key regulators in cellular and intercellular physiological responses, and could be therapeutically useful for modulating several pathological conditions. Unfortunately, the use of peptide-based agonists to target centrally located opioid receptors is limited by poor physicochemical (PC), distribution, metabolic, and pharmacokinetic (DMPK) properties that restrict penetration across the blood-brain barrier via passive diffusion. To address these problems, the present paper exploits fluorinated peptidomimetics to simultaneously modify PC and DMPK properties, thus facilitating entry into the central nervous system. As an initial example, the present paper exploited the Tyr¹-ψ[( Z)CF═CH]-Gly² peptidomimetic to improve PC druglike characteristics (compu

SUBMITTER: Altman RA 

PROVIDER: S-EPMC6051889 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature