Discovery of orally bioavailable NK1 receptor antagonists

Abstract Benzyloxyphenethylpiperazines are a new class of high affinity NK 1 receptor antagonists. Oral bioavailability and selectivity can be fine tuned by the nature of the substituents on the basic nitrogen atom. Addition of substituents with a carboxylic acid group led to very selective and orally active NK 1 antagonists free of interaction with l -type calcium channels.