Gmeiner P (1995)
Publication Type: Journal article
Publication year: 1995
Publisher: Wiley-VCH Verlag
Book Volume: 328
Pages Range: 329-332
The 3-phenylazepino[5,4,3-c,d]indole derivatives 5 and 9-11, representing heterocyclic analogs of the selective dopamine D-1 receptor ligands of the 3-phenylbenzazepine class, were synthesized starting from the indole-4-carboxylate 7. Receptor binding studies employing bovine striatal membranes demonstrated that the test compounds 5, 10, and 11 are able to displace the D-1 selective radioligand [3H]-SCH 23390 as well as the D-2 antagonist [3H]-spiperone. Compound 5b turned out to be the most potent and selective ligand (k(i) = 1.8 μM for D-1 and k(i) = 8.9 μM for D-2). It is assumed that the moderate selectivity of 5b is due to the conformational inequality of the 7-membered rings when compared to the benzazepines. This results in a spatial arrangement of the phenyl substituent which is not able to interact with a 'subtype selectivity-inducing site'.
APA:
Gmeiner, P. (1995). Synthesis and Dopamine Receptor Binding of 3-Phenylazepino[5,4,3-c,d]indole Derivatives. Archiv Der Pharmazie, 328, 329-332.
MLA:
Gmeiner, Peter. "Synthesis and Dopamine Receptor Binding of 3-Phenylazepino[5,4,3-c,d]indole Derivatives." Archiv Der Pharmazie 328 (1995): 329-332.
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