A novel PEG–haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer–drug conjugates in a non-prodrug fashion,10.1039/C6PY01418F

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

A novel PEG–haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer–drug conjugates in a non-prodrug fashion

Felicity Heath,Amy Newman,Chiara Clementi,Gianfranco Pasut,Hong Lin,Gary J. Stephens,Benjamin J. Whalley,Helen M. I. Osborn,Francesca Greco

Polymer Chemistry Pub Date : 11/15/2016 00:00:00 , DOI:10.1039/C6PY01418F

Abstract

A PEG–haloperidol conjugate containing a non-biodegradable linker was synthesised. Incubation with rat plasma demonstrated excellent linker stability, and competition radioligand binding assays demonstrated retained binding to the D₂-receptor. In silico studies predicted that the conjugate will not cross the blood–brain barrier (BBB), thus potentially restricting haloperidol action to one side of the BBB.