A-366833: a novel nicotinonitrile-substituted 3,6-diazabicyclo[3.2.0]-heptane alpha4beta2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in animal models

5-[(1R,5S)-3,6-Diazabicyclo[3.2.0]heptan-6-yl]nicotinonitrile (A-366833) is a novel nicotinic acetylcholine receptor (nAChR) ligand that binds to the agonist-binding site ([3H]-cytisine) with Ki value of 3.1 nM and exhibits agonist selectivity at alpha4beta2 nAChR relative to the alpha3beta4 nAChR s...

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Veröffentlicht in:	Biochemical pharmacology 2007-10, Vol.74 (8), p.1253
Hauptverfasser:	Ji, Jianguo, Bunnelle, William H, Anderson, David J, Faltynek, Connie, Dyhring, Tino, Ahring, Philip K, Rueter, Lynne E, Curzon, Peter, Buckley, Michael J, Marsh, Kennan C, Kempf-Grote, Anita, Meyer, Michael D
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics - pharmacology Animals Cystine - metabolism Ferrets Male Mice Models, Animal Nausea - chemically induced Nicotinic Agonists - chemical synthesis Nicotinic Agonists - pharmacokinetics Nicotinic Agonists - pharmacology Nicotinic Agonists - toxicity Rats Rats, Sprague-Dawley Receptors, Nicotinic - drug effects
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