Synthesis of Tropeines and Allosteric Modulation of Ionotropic Glycine Receptors

Twenty esters of 3α- and 3β-hydroxy(nor)tropanes and two amides of 3α-aminotropane were prepared with substituted benzoic acids. These (nor)tropeines inhibited [3H]strychnine binding to glycine receptors in synaptosomal membranes of rat spinal cord. A ternary allosteric model was applied to determin...

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Veröffentlicht in:	Journal of medicinal chemistry 2004-12, Vol.47 (25), p.6384-6391
Hauptverfasser:	Maksay, Gábor, Nemes, Péter, Bíró, Tímea
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals Benzoates - chemistry Binding, Competitive Biological and medical sciences Glutamatergic system (aspartate and other excitatory aminoacids) Glycine - metabolism In Vitro Techniques Male Medical sciences Models, Molecular Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Rats Rats, Wistar Receptors, Glycine - metabolism Receptors, Serotonin, 5-HT3 - metabolism Spinal Cord - drug effects Spinal Cord - metabolism Structure-Activity Relationship Strychnine - metabolism Tropanes - chemical synthesis Tropanes - chemistry Tropanes - pharmacology
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