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 journalArticle

3 Citations (Scopus)

Abstract

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
Volume8
Issue number9
StatePublished - Dec 1 1998

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Mecamylamine
epibatidine
Derivatives
Nicotinic Receptors
Acetylcholinesterase
Hypothermia
Nicotine
Cerebral Cortex
Rats
In Vitro Techniques
isoarecolone

ASJC Scopus subject areas

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

Cite this

Beach, J. W., Damaj, M. I., Jonnala, R. R., Terry, A. V., & Buccafusco, J. J. (1998). Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives. Medicinal Chemistry Research, 8(9), 510-522.

Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives. / Beach, J. Warren; Damaj, M. Imad; Jonnala, Ramamohana R.; Terry, Alvin V; Buccafusco, Jerry J.

In: Medicinal Chemistry Research, Vol. 8, No. 9, 01.12.1998, p. 510-522.

Research output: Contribution to journalArticle

Beach, JW, Damaj, MI, Jonnala, RR, Terry, AV & Buccafusco, JJ 1998, 'Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives', Medicinal Chemistry Research, vol. 8, no. 9, pp. 510-522.
Beach, J. Warren ; Damaj, M. Imad ; Jonnala, Ramamohana R. ; Terry, Alvin V ; Buccafusco, Jerry J. / Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives. In: Medicinal Chemistry Research. 1998 ; Vol. 8, No. 9. pp. 510-522.
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