Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts

We describe the synthesis of tetrahydroisoquinolines and tetrahydroisoquinolinium salts together with their pharmacological properties at various nicotinic acetylcholine receptors. In general, the compounds were α4β2 nAChR antagonists, with the tetrahydroisoquinolinium salts being more potent than t...

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Veröffentlicht in:	Journal of medicinal chemistry 2018-02, Vol.61 (4), p.1719-1729
Hauptverfasser:	Crestey, François, Jensen, Anders A, Soerensen, Christian, Magnus, Charlotte Busk, Andreasen, Jesper T, Peters, Günther H. J, Kristensen, Jesper L
Format:	Artikel
Sprache:	eng
Schlagworte:	alpha7 Nicotinic Acetylcholine Receptor - agonists Animals Antidepressive Agents - chemistry Humans Mice Molecular Docking Simulation Nicotinic Antagonists Receptors, Nicotinic - drug effects Salts - pharmacology Stereoisomerism Swimming Tetrahydroisoquinolines - chemical synthesis Tetrahydroisoquinolines - pharmacology
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