| Title : Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands - Menegatti_2003_Bioorg.Med.Chem_11_4807 |
| Author(s) : Menegatti R , Cunha AC , Ferreira VF , Pereira EF , El-Nabawi A , Eldefrawi AT , Albuquerque EX , Neves G , Rates SM , Fraga CA , Barreiro EJ |
| Ref : Bioorganic & Medicinal Chemistry , 11 :4807 , 2003 |
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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. |
| PubMedSearch : Menegatti_2003_Bioorg.Med.Chem_11_4807 |
| PubMedID: 14556797 |
Menegatti R, Cunha AC, Ferreira VF, Pereira EF, El-Nabawi A, Eldefrawi AT, Albuquerque EX, Neves G, Rates SM, Fraga CA, Barreiro EJ (2003)
Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands
Bioorganic & Medicinal Chemistry
11 :4807
Menegatti R, Cunha AC, Ferreira VF, Pereira EF, El-Nabawi A, Eldefrawi AT, Albuquerque EX, Neves G, Rates SM, Fraga CA, Barreiro EJ (2003)
Bioorganic & Medicinal Chemistry
11 :4807