Journal of Medicinal Chemistry p. 1850 - 1854 (1991)
Update date:2022-08-04
Topics:
Russo, Filippo
Romeo, Giuseppe
Guccione, Salvatore
Blasi, Antonio De
A number of 3-substituted pyrimido<5,4-b>indole-2,4-diones (7-23) were evaluated for their in vitro α1 adrenoceptor affinity by radioligand receptor binding assays.Some compounds bearing a (phenylpiperazinyl(alkyl side chain were potent α1 adrenoceptor ligands.The most active derivative in displacement of <3H>prazosin from rat cortical membranes was 3-<2-<4-(2-methoxyphenyl)piperazin-1-yl>ethyl>pyrimido<5,4-b>indole-2,4-dione (10) (Ki = 0.21 nM).Discrete modifications in the structure resulted in higher selectivity (> 10000 times) for α1 than α2, β2, and 5HT1A receptors.Some compounds also had affinity for the 5HT1A receptor.The most selective α1 ligand was 3-<2-<4-(2-chlorophenyl)piperazin-1-yl>ethyl>pyrimido<5,4-b>indole-2,4-dione (13).
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