| 14556797 |
Menegatti R, Cunha AC, Ferreira VF, Perreira EF, El-Nabawi A, Eldefrawi AT, Albuquerque EX, Neves G, Rates SM, Fraga CA, Barreiro EJ: Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands. Bioorg Med Chem. 2003 Nov 3;11(22):4807-13.
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. |
82(1,1,1,2) |