Pharmacological evaluation of a diarylmethylene-piperidine derivative: A new potent atypical antipsychotic?

被引：7
|
作者：
Talaga, P [1 ]
Matagne, A [1 ]
Klitgaard, H [1 ]
机构：
[1] UCB SA, Pharma Sector, B-1420 Braine Lalleud, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 10期
关键词：
D O I：
10.1016/S0960-894X(01)00200-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new diaryl-methylene piperidine derivative, 2, displayed an atypical antipsychotic profile both in vitro and in vivo. The main pharmacological characteristics of this compound appears to reside in a more potent antagonism of the 5-HT2 serotonergic receptor than of the D2 dopaminergic receptor. This confirms that molecules displaying a D2/5-HT2 binding ratio <1 possess clozapine-like antipsychotic activity. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1313 / 1316
页数：4
相关论文
共 50 条
  • [41] Design, Synthesis, Molecular Docking, and Preliminary Pharmacological Screening of some New Benzo[d]thiazol-2-ylamino Containing Chromen-2-one Derivatives with Atypical Antipsychotic Profile
    Gawai, Ashish A.
    Biyani, Kailash R.
    Das, Sanjib
    Tapadiya, Ganesh G.
    Mokale, Santosh N.
    Dhawale, Sachin A.
    CURRENT COMPUTER-AIDED DRUG DESIGN, 2023, 19 (06) : 465 - 475
  • [42] Preparation and Cytotoxic Evaluation of PGV-1 Derivative, CCA-1.1, as a New Curcumin Analog with Improved-Physicochemical and Pharmacological Properties
    Utomo, Rohmad Yudi
    Wulandari, Febri
    Novitasari, Dhania
    Lestari, Beni
    Susidarti, Ratna Asmah
    Jenie, Riris Istighfari
    Kato, Jun-ya
    Sardjiman, Sardjiman
    Meiyanto, Edy
    ADVANCED PHARMACEUTICAL BULLETIN, 2022, 12 (03) : 603 - 612
  • [43] New selective and potent 5-HT1B/1D antagonists:: Chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides
    Liao, Y
    Böttcher, H
    Harting, J
    Greiner, H
    van Amsterdam, C
    Cremers, T
    Sundell, S
    März, J
    Rautenberg, W
    Wikström, H
    JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (03) : 517 - 525
  • [44] Design, synthesis, and preliminary pharmacological evaluation of 1,4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents
    Manetti, D
    Ghelardini, C
    Bartolini, A
    Bellucci, C
    Dei, S
    Galeotti, N
    Gualtieri, F
    Romanelli, MN
    Scapecchi, S
    Teodori, E
    JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (10) : 1969 - 1974
  • [45] Synthesis, characterization, biological evaluation and molecular docking of a new quinazolinone-based derivative as a potent dual inhibitor for VEGFR-2 and EGFR tyrosine kinases
    Riadi, Yassine
    Alamri, Mubarak A.
    Geesi, Mohammed H.
    Anouar, El Hassane
    Ouerghi, Oussama
    Alabbas, Alhumaidi B.
    Alossaimi, Manal A.
    Altharawi, Ali
    Dehbi, Oussama
    Alqahtani, Safar M.
    JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2022, 40 (15): : 6810 - 6816
  • [46] Synthesis and preliminary pharmacological evaluation of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides as novel atypical antipsychotic agents
    Sekhar, K. V. G. Chandra
    Rao, V. S.
    Vyas, D. Ravi Kumar
    Kumar, M. Murali Krishna
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (23) : 6054 - 6057
  • [47] Pharmacological evaluation of 5-{2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-1,3-dihydro-benz-imidazole-2-thione as a potential atypical antipsychotic agent
    Tomic, M
    Kundakovic, M
    Butorovic, B
    Vasilev, V
    Dragovic, D
    Roglic, G
    Ignjatovic, DJ
    Soskic, V
    Kostic-Rajacic, S
    PHARMAZIE, 2003, 58 (09): : 677 - 678
  • [48] Design, synthesis and pharmacological evaluation of 2-arylurea-1,3,5-tria-zine derivative (XIN-9): A novel potent dual PI3K/mTOR inhibitor for cancer therapy
    Sun, Xin
    Zhang, Binliang
    Luo, Leixuan
    Yang, Yang
    He, Bin
    Zhang, Qian
    Wang, Linxiao
    Xu, Shan
    Zheng, Pengwu
    Zhu, Wufu
    BIOORGANIC CHEMISTRY, 2022, 129
  • [49] Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 4-{4-[2-(4-(2-substitutedquinoxalin-3-yl)piperazin-1-yl)ethyl]phenyl}thiazoles as atypical antipsychotic agents
    Kondapalli Venkata Gowri Chandra Sekhar
    Vajja Sambasiva Rao
    Winnie Deuther-Conrad
    Divya Sridhar
    Hunsur Nagendra Nagesh
    Vellas Sreedhar Kumar
    Peter Brust
    Muthyala Murali Krishna Kumar
    Medicinal Chemistry Research, 2013, 22 : 1660 - 1673
  • [50] Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 4-{4-[2-(4-(2-substitutedquinoxalin-3-yl)piperazin-1-yl)ethyl]phenyl}thiazoles as atypical antipsychotic agents
    Sekhar, Kondapalli Venkata Gowri Chandra
    Rao, Vajja Sambasiva
    Deuther-Conrad, Winnie
    Sridhar, Divya
    Nagesh, Hunsur Nagendra
    Kumar, Vellas Sreedhar
    Brust, Peter
    Kumar, Muthyala Murali Krishna
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (04) : 1660 - 1673
12345