133399-65-2Relevant academic research and scientific papers
Heterocyclic systems containing the pyrimido-2,4-dione ring as selective ligands for the α1-adrenoceptors
Romeo,Russo,Guccione,Barbarulo,De Blasi
, p. 471 - 477 (2007/10/02)
In the present paper recent results obtained in the field of the α1-adrenoceptor (α1AR) ligands are reported. Syntheses, α1AR binding properties and structure-affinity relationships of tricyclic compounds containing the pyrimido-2,4-dione ring are described. Moreover, preliminary results on the binding properties of some derivatives for the recently cloned α1AR subtypes expressed in COS-7 cells (α(1B), α(1C), α(1D)) are discussed. Obtained data clearly indicate that some of the synthesized compounds are able to discriminate between the α(1B) and the α(1C)/α(1D) adrenoceptor subclasses.
Pyrimidoindole Derivatives. 1. A New Class of Potent and Selective α1 Adrenoceptor Ligands
Russo, Filippo,Romeo, Giuseppe,Guccione, Salvatore,Blasi, Antonio De
, p. 1850 - 1854 (2007/10/02)
A number of 3-substituted pyrimidoindole-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 prazosin from rat cortical membranes was 3-ethyl>pyrimidoindole-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-ethyl>pyrimidoindole-2,4-dione (13).
