3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1h-indoles as bioavailable h5-HT2A antagonists

A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT2A receptor. 3-(8-Phenethyl-8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indole is a high-affinity (1.2nM), selective (>800 fold over h5-HT2C and hD2 recep...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 10; no. 24; pp. 2701 - 2703
Main Authors:	CRAWFORTH, James, GOODACRE, Simon, MAXEY, Robert, BOURRAIN, Sylvie, PATEL, Smita, MARWOOD, Rosemarie, O'CONNOR, Desmond, HERBERT, Richard, HUTSON, Peter, ROWLEY, Michael
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier 18-12-2000
Subjects:	Administration, Oral Animals Binding, Competitive Biological and medical sciences Biological Availability Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis Bridged Bicyclo Compounds, Heterocyclic - pharmacokinetics Bridged Bicyclo Compounds, Heterocyclic - pharmacology Humans Indoles - chemical synthesis Indoles - pharmacokinetics Indoles - pharmacology Ligands Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacokinetics Piperidines - pharmacology Rats Receptors, Dopamine D2 - metabolism Receptors, Serotonin - metabolism Serotonin Antagonists - chemical synthesis Serotonin Antagonists - pharmacokinetics Serotonin Antagonists - pharmacology Serotoninergic system Structure-Activity Relationship Rat Nitrogen heterocycle Rodentia Oral administration Selectivity Bioavailability In vitro 5-HT2 Serotonine receptor Vertebrata Mammalia Structure activity relation Animal Piperidine derivatives Bicyclic compound Aromatic compound Antagonist Indole derivatives Pharmacokinetics Chemical synthesis
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