Synthesis of metabolically stable arylpiperazine 5-HT1A receptor agonists

Arthur G. Romero, William H. Darlington, Monford F. Piercey, Robert A. Lahti

Research output: Contribution to journalArticlepeer-review

26 Scopus citations


Although N-alkylarylpiperazines as a class are finding use as anxiolytics and antidepressants, many of these arylpiperazines are highly metabolically labile at the n-alkyl-piperazine bond. We have found that cyclopropanating the n-butyl chain contained in the 5-HT1A receptor agonist ipsapirone (2) instills a resistance to this metabolism as well as providing information about the geometrical requirements of the 5-HT1A receptor.

Original languageEnglish
Pages (from-to)1703-1706
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number12
StatePublished - Dec 1992


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