221057-89-2Relevant articles and documents
Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives
Beach, J. Warren,Damaj, M. Imad,Jonnala, Ramamohana R.,Terry Jr., Alvin V.,Buccafusco, Jerry J.
, p. 510 - 522 (2007/10/03)
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.