(±)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents
摘要:
Several amine-substituted 8-amino-5,6,7,8-tetrahydroisoquinolines were examined as conformationally-constrained analogs of the nicotinic cholinergic (nACh) 3-(aminomethyl)pyridines. Although these ligands failed to bind at nACh receptors, the N-ethyl-N-methyl analog 3d was found to be at least equipotent with nicotine in rodent tests of antinociception. The mechanism of action of 3d is currently unknown. (C) 2004 Elsevier Ltd. All rights reserved.
(±)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents
摘要:
Several amine-substituted 8-amino-5,6,7,8-tetrahydroisoquinolines were examined as conformationally-constrained analogs of the nicotinic cholinergic (nACh) 3-(aminomethyl)pyridines. Although these ligands failed to bind at nACh receptors, the N-ethyl-N-methyl analog 3d was found to be at least equipotent with nicotine in rodent tests of antinociception. The mechanism of action of 3d is currently unknown. (C) 2004 Elsevier Ltd. All rights reserved.
(±)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents
作者:Małgorzata Dukat、Mohamed Taroua、Abdelaziz Dahdouh、Umamaheswar Siripurapu、M Imad Damaj、Billy R Martin、Richard A Glennon
DOI:10.1016/j.bmcl.2004.05.020
日期:2004.7
Several amine-substituted 8-amino-5,6,7,8-tetrahydroisoquinolines were examined as conformationally-constrained analogs of the nicotinic cholinergic (nACh) 3-(aminomethyl)pyridines. Although these ligands failed to bind at nACh receptors, the N-ethyl-N-methyl analog 3d was found to be at least equipotent with nicotine in rodent tests of antinociception. The mechanism of action of 3d is currently unknown. (C) 2004 Elsevier Ltd. All rights reserved.