lassbio-581 and Schizophrenia

lassbio-581 has been researched along with Schizophrenia* in 1 studies

Other Studies

1 other study(ies) available for lassbio-581 and Schizophrenia

Article	Year
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. Bioorganic & medicinal chemistry, 2010, Mar-01, Volume: 18, Issue:5 We described herein the design, synthesis, and pharmacological evaluation of N-phenylpiperazine heterocyclic derivatives as multi-target compounds potentially useful for the treatment of schizophrenia. The isosteric replacement of the heterocyclic ring at the biaryl motif generating pyrazole, 1,2,3-triazole, and 2-methylimidazole[1,2-a]pyridine derivatives resulted in 21 analogues with different substitutions at the para-biaryl and para-phenylpiperazine positions. Among the compounds prepared, 4 (LASSBio-579) and 10 (LASSBio-664) exhibited an adequate binding profile and a potential for schizophrenia positive symptoms treatment without cataleptogenic effects. Structural features of this molecular scaffold are discussed regarding binding affinity and selectivity for D(2)-like, 5-HT(1A), and 5-HT(2A) receptors. Topics: Administration, Oral; Animals; Antipsychotic Agents; Cell Line; Humans; Ligands; Male; Mice; Piperazines; Pyrazoles; Rats; Receptor, Serotonin, 5-HT1A; Receptors, Dopamine D2; Schizophrenia	2010

Article

Year

Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.

Bioorganic & medicinal chemistry, 2010, Mar-01, Volume: 18, Issue:5

We described herein the design, synthesis, and pharmacological evaluation of N-phenylpiperazine heterocyclic derivatives as multi-target compounds potentially useful for the treatment of schizophrenia. The isosteric replacement of the heterocyclic ring at the biaryl motif generating pyrazole, 1,2,3-triazole, and 2-methylimidazole[1,2-a]pyridine derivatives resulted in 21 analogues with different substitutions at the para-biaryl and para-phenylpiperazine positions. Among the compounds prepared, 4 (LASSBio-579) and 10 (LASSBio-664) exhibited an adequate binding profile and a potential for schizophrenia positive symptoms treatment without cataleptogenic effects. Structural features of this molecular scaffold are discussed regarding binding affinity and selectivity for D(2)-like, 5-HT(1A), and 5-HT(2A) receptors.

Topics: Administration, Oral; Animals; Antipsychotic Agents; Cell Line; Humans; Ligands; Male; Mice; Piperazines; Pyrazoles; Rats; Receptor, Serotonin, 5-HT1A; Receptors, Dopamine D2; Schizophrenia

2010