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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Evaluation of 2,3,4,8,13a Hexahydro-1H-Benzo[5,6]Cyclohepta-6,7- Dihydroxy[1,2,3-ef][3]Benzazepine Derivatives as Dopamine Receptor Ligands

Author(s): P. Sozio, F. Pinnen, A. Cocco, I. Cacciatore, G. Giorgioni, B. Costa, M. Montali, G. Spoto, F. Santoleri and ">Antonio Di Stefano

Volume 3 , Issue 1 , 2006

Page: [55 - 60] Pages: 6

DOI: 10.2174/157018006775240971

Price: $65


This paper reports the synthesis of 2,3,4,8,13a-hexahydro-1H-benzo[5,6]cyclohepta[1,2,3- ef][3]benzazepine derivatives (2a-d) as an extension of our studies about rigid congeners of 1- benzyltetrahydroisoquinoline. The new compounds were evaluated for affinities at D1 and D2 dopamine receptors. Compounds 2b-d showed similar D1 and D2 affinities to dopamine. 2,3,4,8,13a-hexahydro-1Hbenzo[ 5,6]cyclohepta-6,7-dihydroxy-[1,2,3-ef][3]benzazepine 2b and the N-methyl analogue 2d showed weak D1-like agonistic activity. This was demonstrated by their effect on the cyclic guanosine monophosphate (cGMP) content in rat neostriatal membranes.

Keywords: Cyclohepta[1,2,3-ef][3]benzazepine derivatives, Dopamine receptor ligands, Binding affinity, Rat striatal membranes, Guanylate cyclase, cGMP

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