(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
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.
Dukat
Małgorzata
M
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA.
Taroua
Mohamed
M
Dahdouh
Abdelaziz
A
Siripurapu
Umamaheswar
U
Damaj
M Imad
MI
Martin
Billy R
BR
Glennon
Richard A
RA
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D002478:Cells, Cultured; D004195:Disease Models, Animal; D008024:Ligands; D051379:Mice; D010146:Pain / Q000188:drug therapy; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use
D000700:Analgesics; D008024:Ligands; D011978:Receptors, Nicotinic; D044005:Tetrahydroisoquinolines