6-hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs : new centrally acting 5-HT1A receptor agonists

6-hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs : new centrally acting 5-HT1A receptor agonists

The ring-closed phenylethylamine analogue 6-hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine (1) is a 5-HT1A receptor agonist of moderate potency, according to both in vivo biochemical data and in vitro binding data. The active compounds of this series also induce the 5-HT behavioral syndrome....

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Veröffentlicht in:Journal of medicinal chemistry 1992-10, Vol.35 (22), p.3984-3990
Hauptverfasser: WIKSTRÖM, H, ANDERSSON, B, ELEBRING, T, LAGERKVIST, S, HALLNEMO, G, PETTERSSON, I, JOVAL, P.-Å, SVENSSON, K, EKMAN, A, CARLSSON, A
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Benzazepines - chemistry
Benzazepines - pharmacology
Binding, Competitive
Biological and medical sciences
Brain - drug effects
Brain - metabolism
Dopamine - biosynthesis
Feedback
In Vitro Techniques
Male
Medical sciences
Models, Molecular
Molecular Conformation
Motor Activity - drug effects
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Norepinephrine - biosynthesis
Pharmacology. Drug treatments
Radioligand Assay
Rats
Rats, Sprague-Dawley
Receptors, Serotonin - drug effects
Receptors, Serotonin - metabolism
Serotonin - biosynthesis
Serotonin Receptor Agonists - chemistry
Serotonin Receptor Agonists - pharmacology
Serotoninergic system
Structure-Activity Relationship
Thermodynamics
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Zusammenfassung:The ring-closed phenylethylamine analogue 6-hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine (1) is a 5-HT1A receptor agonist of moderate potency, according to both in vivo biochemical data and in vitro binding data. The active compounds of this series also induce the 5-HT behavioral syndrome. Molecular modeling studies were performed with molecular mechanics calculations, and a tentative explanation for the relatively low potency of these serotonergic benzazepines is provided.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00100a002