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

3 Scopus citations

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 - 1998

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
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",

language = "English (US)",

volume = "8",

pages = "510--522",

journal = "Medicinal Chemistry Research",

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TY - JOUR

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

Y1 - 1998

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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M3 - Article

AN - SCOPUS:0032430161

SN - 1054-2523

VL - 8

SP - 510

EP - 522

JO - Medicinal Chemistry Research

JF - Medicinal Chemistry Research

IS - 9

ER -

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

Abstract

ASJC Scopus subject areas

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