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(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.

作者信息

Dukat Małgorzata, Taroua Mohamed, Dahdouh Abdelaziz, Siripurapu Umamaheswar, Damaj M Imad, Martin Billy R, Glennon Richard A

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA.

出版信息

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3651-4. doi: 10.1016/j.bmcl.2004.05.020.

Abstract

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.

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