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.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Analgesics / chemical synthesis*
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Analgesics / pharmacology
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Analgesics / therapeutic use
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Animals
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Cells, Cultured
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Disease Models, Animal
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Ligands
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Mice
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Pain / drug therapy
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Receptors, Nicotinic / drug effects
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Receptors, Nicotinic / metabolism
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Tetrahydroisoquinolines / chemical synthesis*
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Tetrahydroisoquinolines / pharmacology
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Tetrahydroisoquinolines / therapeutic use
Substances
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Analgesics
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Ligands
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Receptors, Nicotinic
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Tetrahydroisoquinolines