Method of selecting nonsedating H1-antagonists

Abstract

A method is described in accordance with which one may select a nonsedating histamine H1-antagonist; comprising the step of determining whether a candidate H1-antagonist is a substrate for P-gp, especially P-gp expressed by MDR1 or mdr1a/1b, comprising the step of determining the brain-to-plasma AUC ratio in mdr1a/1b KO mice, and in WT mice, and selecting said candidate where the brain-to-plasma AUC ratio for said KO mice to the brain-to-plasma concentration ratio for said WT mice is 1.5 or greater.

Dependencies are inferred from the claim text.