Literature DB >> 8568801

3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.

H R Howard1, J A Lowe, T F Seeger, P A Seymour, S H Zorn, P R Maloney, F E Ewing, M E Newman, A W Schmidt, J S Furman, G L Robinson, E Jackson, C Johnson, J Morrone.   

Abstract

A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an approach to a novel atypical antipsychotic agent. The in vitro profile of 8e from this series is a combination of D2 receptor affinity comparable to the typical antipsychotic agent haloperidol and a 5-HT2A/D2 ratio comparable to the atypical agent clozapine. In vivo 8e possesses activity consistent with an efficacious antipsychotic agent with less tendency to induce extrapyramidal side effects in man.

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Year:  1996        PMID: 8568801     DOI: 10.1021/jm950625l

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Single- and multiple-dose pharmacokinetics of ziprasidone in healthy young and elderly volunteers.

Authors:  K D Wilner; T G Tensfeldt; B Baris; T A Smolarek; R Z Turncliff; W A Colburn; R A Hansen
Journal:  Br J Clin Pharmacol       Date:  2000       Impact factor: 4.335

Review 2.  Biotransformation of post-clozapine antipsychotics: pharmacological implications.

Authors:  S Caccia
Journal:  Clin Pharmacokinet       Date:  2000-05       Impact factor: 6.447

Review 3.  Functionalized congener approach to the design of ligands for G protein-coupled receptors (GPCRs).

Authors:  Kenneth A Jacobson
Journal:  Bioconjug Chem       Date:  2009-04-30       Impact factor: 4.774

  3 in total

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