A Series of N4-Imidoethyl Derivatives of 1-(2,3-Dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A Receptor Ligands: Synthesis and Structure-Affinity Relationships

A series of unsubstituted and substituted succinimido, maleimido, and glutarimidoethyl derivatives of eltoprazine (3) was synthesized and tested for affinity for the 5-HT1A receptor in rat brain homogenates. The unsubstituted compounds have a moderate affinity for the receptor, while the affinity co...

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Veröffentlicht in:	Journal of medicinal chemistry 1995-10, Vol.38 (21), p.4303-4308
Hauptverfasser:	van Steen, B. J, van Wijngaarden, I, Tulp, M. Th. M, Soudijn, W
Format:	Artikel
Sprache:	eng
Schlagworte:	8-Hydroxy-2-(di-n-propylamino)tetralin - metabolism Animals Binding Sites Biological and medical sciences Brain - metabolism Cyclization Frontal Lobe - metabolism Hydrogen-Ion Concentration Lipid Metabolism Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperazines - chemistry Rats Receptors, Serotonin - metabolism Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - metabolism Serotoninergic system Stereoisomerism Structure-Activity Relationship
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