New 3-benzisothiazolyl and 3-benzisoxazolylpiperazine derivatives with atypical antipsychotic binding profile.
New 3-benzisothiazolyl and 3-benzisoxazolylpiperazine derivatives were synthesised and their 5-HT(1A), 5-HT(2A) and D(2) receptor binding affinities evaluated. The compounds displayed high affinity for the 5-HT(2A) receptor combined with moderate to low 5-HT(1A) and D(2) affinities. Two of them, 18 and 25, have been selected for further pharmacological studies to be evaluated as potential atypical antipsychotics.
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000493:pharmacokinetics; D000478:Alkylation; D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D018492:Dopamine Antagonists / Q000494:pharmacology; D007202:Indicators and Reagents; D007700:Kinetics; D008297:Male; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2 / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D044263:Receptors, Serotonin, 5-HT1; D018967:Risperidone / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; D018492:Dopamine Antagonists; D007202:Indicators and Reagents; D010879:Piperazines; D044402:Receptor, Serotonin, 5-HT2A; D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D018967:Risperidone