Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives

J. Warren Beach, M. Imad Damaj, Ramamohana R. Jonnala, Alvin V Terry, Jerry J. Buccafusco

Research output: Contribution to journalArticlepeer-review


The synthesis of the N-ethyl and N-phenylethyl derivatives of isoarecolone are described. These compounds were evaluated in vitro for their ability to displace [3H](±)epibatidine and/or [3H](-) nicotine from nicotinic receptors derived from rat cerebral cortex and their ability to inhibit acetylcholinesterase. The N-ethyl derivative and isoarecolone were evaluated in vivo for their antinociceptive, hypothermia and hypomotility activity in mice. The in vivo activity of isoareeolone was found to the reversible by mecamylamine, however the N-ethyl derivative was found to be insensitive to blockade by mecamylamine.

Original languageEnglish (US)
Pages (from-to)510-522
Number of pages13
JournalMedicinal Chemistry Research
Issue number9
StatePublished - Dec 1 1998

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry


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