100561-24-8Relevant articles and documents
The synthesis of carbon-14 labeled (R)-4-(dipropylamino)-1,3,4,5- tetrahydrobenz[cd]indole-6-carboxamide hippurate. A partial ergoline with 5-HT1A agonist activity and an 125I-labeled analog
Wheeler, William J.,Swanson, Steven P.,Varie, David L.,O'Bannon, Douglas D.
, p. 139 - 148 (2005)
Partial ergoline agonists such as (R)-4-(dipropylamino)-1,3,4,5- tetrahydrobenz[cd]-indole-6-carboxamide (LY228729, 1a) mimic a locked conformational analog of serotonin and in fact possess potent in vitro activity as agonists of the 5-HT1A receptor. In the course of pre-clinical investigation of la for potential use as an anxiolytic agent, 1b was prepared in a five step synthesis from K14CN. In addition, an 125I-analog of 1a was prepared for aid in the development of a radioimmunoassay (RIA). Copyright
Synthetic studies toward the partial ergot alkaloid LY228729, a potent 5HT(1A) receptor agonist
Carr,Creviston,Hutchison,Kennedy,Khau,Kress,Leanna,Marshall,Martinelli,Peterson,Varie,Wepsiec
, p. 8640 - 8653 (2007/10/03)
Synthetic studies on LY228729 (3) afforded two innovative approaches for the construction of this class of partial ergoline 5HT(1a) receptor agonists. The first synthesis is based upon a diastereoselective epoxidation of racemic olefin 5, followed by ring
THE SYNTHESIS OF (+)- AND (-)-1-BENZOYL-1,2,2a,3,4,5-HEXAHYDROBENZINDOL-4-AMINE, and PREPARATION OF LY228729
Martinelli, Michael J.,Leanna, M. Robert,Varie, David L.,Peterson, Barry C.,Kress, Thomas J.,et al.
, p. 7579 - 7582 (2007/10/02)
Racemic epoxide 5 was reacted with S-Phenylethylamine to afford diastereomers 6 and 7, from which amino alcohol 6 could be isolated directly.Aziridine formation and tandem-hydrogenolysis provided optically pure primary amine 2 (31percent from racemic 4),
6-Substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: Potent serotonin agonists
Flaugh,Mullen,Fuller,Mason
, p. 1746 - 1753 (2007/10/02)
A series of 6-substituted tricyclic ergoline partial structures has been synthesized and found to possess very strong serotonin agonist activity. A methoxy group at the 6-position greatly enhances activity, but at the expense of compound stability. Substi
Method of treating anxiety with tetrahydrobenz[c,d]indole-6-carboxamides
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, (2008/06/13)
The present invention provides a method of treating anxiety in humans employing a 4-substituted-1,3,4,5-tetrahydrobenz[c,d]indole-6-carboxamide derivative.
6-Substituted-4-dialkylaminotetrahydrobenz[c,d]indoles
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, (2008/06/13)
(±)-4-substitutedamino-6-substituted-1,3,4,5-tetrahydrobenz[c,d]indoles and pharmaceutically acceptable salts thereof, useful as anti depressants.