Author/Authors :
Ricardo Menegatti، نويسنده , , Anna C. Cunha، نويسنده , , V??tor F Ferreira، نويسنده , , Edna F.R Perreira، نويسنده , , Ahmed El-Nabawi، نويسنده , , Amira T. Eldefrawi، نويسنده , , Edson X. Albuquerque، نويسنده , , Gilda Neves، نويسنده , , Stela M.K Rates، نويسنده , , Carlos A.M. Fraga، نويسنده , , Eliezer J. Barreiro، نويسنده ,
Abstract :
The present study describes the synthesis and pharmacological profile of three novel heterocyclic compounds originally designed, on the basis of bioisosterism, as dopamine D2 receptor ligands: 1-[1-(4-chlorophenyl)-1H-pyrazol-4-ylmethyl]-4-phenyl-piperazine (LASSBio-579), 1-phenyl-4-(1-phenyl-1H-[1,2,3]triazol-4-ylmethyl)-piperazine (LASSBio-580) and 1-[1-(4-chlorophenyl)-1H-[1,2,3]triazol-4-ylmethyl]-4-phenyl-piperazine (LASSBio-581). Binding studies performed on brain homogenate indicated that all three compounds bind selectively to D2 receptors. In addition, electrophysiological studies carried out in cultured hippocampal neurons suggested that LASSBio-579 and 581 act as D2 agonists, whereas LASSBio-580 acts as a D2 antagonist.
