Literature DB >> 15686911

Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent.

Takeshi Ochi1, Masato Sakamoto, Akira Minamida, Kenji Suzuki, Tomohiko Ueda, Teruaki Une, Hiroshi Toda, Kazuya Matsumoto, Yoshiaki Terauchi.   

Abstract

Two major metabolites in humans of blonanserin, 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta-[b]pyridine (code name AD-5423), were synthesized. The first, 7-hydroxylated AD-5423, was synthesized through a four-step process starting from 4-fluorobenzoylacetonitrile (1), and the second, 8-hydroxylated AD-5423, a nine-step process also from 1. The optical resolution, structures, and receptor binding properties of the metabolites were documented.

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Year:  2005        PMID: 15686911     DOI: 10.1016/j.bmcl.2004.12.028

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Blonanserin - A Novel Antianxiety and Antidepressant Drug? An Experimental Study.

Authors:  Ramchandra Prabhakar Limaye; Aditi Nitin Patil
Journal:  J Clin Diagn Res       Date:  2016-09-01

Review 2.  Dopamine and Dopamine-Related Ligands Can Bind Not Only to Dopamine Receptors.

Authors:  Jaromir Myslivecek
Journal:  Life (Basel)       Date:  2022-04-19

3.  Simple and sensitive analysis of blonanserin and blonanserin C in human plasma by liquid chromatography tandem mass spectrometry and its application.

Authors:  Yunliang Zheng; Xingjiang Hu; Jian Liu; Guolan Wu; Huili Zhou; Meixiang Zhu; You Zhai; Lihua Wu; Jianzhong Shentu
Journal:  J Anal Methods Chem       Date:  2014-02-11       Impact factor: 2.193

4.  Effect of the piperazine unit and metal-binding site position on the solubility and anti-proliferative activity of ruthenium(II)- and osmium(II)- arene complexes of isomeric indolo[3,2-c]quinoline-piperazine hybrids.

Authors:  Lukas K Filak; Danuta S Kalinowski; Theresa J Bauer; Des R Richardson; Vladimir B Arion
Journal:  Inorg Chem       Date:  2014-06-13       Impact factor: 5.165

5.  Piperazinyl fragment improves anticancer activity of Triapine.

Authors:  Marta Rejmund; Anna Mrozek-Wilczkiewicz; Katarzyna Malarz; Monika Pyrkosz-Bulska; Kamila Gajcy; Mieczyslaw Sajewicz; Robert Musiol; Jaroslaw Polanski
Journal:  PLoS One       Date:  2018-04-13       Impact factor: 3.240

Review 6.  The Role of Descending Pain Modulation in Chronic Primary Pain: Potential Application of Drugs Targeting Serotonergic System.

Authors:  Zhuo-Ying Tao; Pei-Xing Wang; Si-Qi Wei; Richard J Traub; Jin-Feng Li; Dong-Yuan Cao
Journal:  Neural Plast       Date:  2019-12-17       Impact factor: 3.599

  6 in total

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