Binding of isotryptamines and indenes at h5-HT6 serotonin receptors

To determine if the indolic nitrogen atom is required for the binding of N(1)-benzyltryptamines at h5-HT(6) serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (8), p.1987-1991
Hauptverfasser:	KOLANOS, Renata, SIRIPURAPU, Uma, PULLAGURLA, Manik, RIAZ, Mohamed, SETOLA, Vince, ROTH, Bryan L, DUKAT, Małgorzata, GLENNON, Richard A
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Biological and medical sciences Humans Indenes - chemistry Indenes - metabolism Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Protein Binding Receptors, Serotonin - chemistry Receptors, Serotonin - metabolism Serotoninergic system Tryptamines - chemistry Tryptamines - metabolism
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	To determine if the indolic nitrogen atom is required for the binding of N(1)-benzyltryptamines at h5-HT(6) serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl)indene (11, K(i)=3nM) indicates that the indolic nitrogen atom is not essential for binding.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.02.070