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.
A novel PEG-haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer-drug conjugates in a non-prodrug fashion
CLEMENTI, CHIARA;PASUT, GIANFRANCO;
2016
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.
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