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

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

Pharmacology and Toxicology

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	510-522
Number of pages	13
Journal	Medicinal Chemistry Research
Volume	8
Issue number	9
State	Published - Dec 1 1998

ASJC Scopus subject areas

Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

Cite this

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title = "Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives",

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.",

author = "Beach, {J. Warren} and Damaj, {M. Imad} and Jonnala, {Ramamohana R.} and Terry, {Alvin V} and Buccafusco, {Jerry J.}",

year = "1998",

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T1 - Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives

AU - Beach, J. Warren

AU - Damaj, M. Imad

AU - Jonnala, Ramamohana R.

AU - Terry, Alvin V

AU - Buccafusco, Jerry J.

PY - 1998/12/1

Y1 - 1998/12/1

N2 - 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.

AB - 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.

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AN - SCOPUS:0032430161

SN - 1054-2523

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JO - Medicinal Chemistry Research

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IS - 9

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

Abstract

ASJC Scopus subject areas

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