5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like properties

被引：17
|
作者：
Diouf, O
Carato, P
Depreux, P
Bonte, JP
Caignard, DH
GuardiolaLemaitre, B
Rettori, MC
Belzung, C
Lesieur, D
机构：
[1] INST CHIM PHARMACEUT, F-59006 LILLE, FRANCE
[2] ADIR, F-92415 COURBEVOIE, FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(97)10023-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of new benzothiazolin-2-one, benzoxazolin-2-one and benzoxazin-3-one derivatives were synthesized and their binding profile at 5-HT1A, 5-HT2A, 5-HT2C as well as D-2 and alpha(1) receptors was determined. All studied compounds displayed high to moderate affinity for both 5-HT1A and 5-HT2A receptor subtypes. Among these, one compound (29) emerged since it exhibited potent antagonist activities at 5-HT1A, 5-HT2A, D-2 and alpha(1) central receptors and showed anxiolytic and antipanic-like effects in mice. 29 is currently undergoing preclinical evaluation. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码：2579 / 2584
页数：6
相关论文
共 50 条
  • [1] Activation of 5-HT1A receptors in the rat basolateral amygdala induces both anxiolytic and antipanic-like effects
    de Andrade Strauss, Christiana Villela
    Vicente, Maria Adrielle
    Zarrossi, Helio, Jr.
    BEHAVIOURAL BRAIN RESEARCH, 2013, 246 (01) : 103 - 110
  • [2] 5-HT1A and 5-HT2A receptors in the rat dorsal periaqueductal gray mediate the antipanic-like effect induced by the stimulation of serotonergic neurons in the dorsal raphe nucleus
    Roger L. H. Pobbe
    Hélio Zangrossi
    Psychopharmacology, 2005, 183 : 314 - 321
  • [3] 5-HT1A and 5-HT2A receptors in the rat dorsal periaqueductal gray mediate the antipanic-like effect induced by the stimulation of serotonergic neurons in the dorsal raphe nucleus
    Pobbe, RLH
    Zangrossi, H
    PSYCHOPHARMACOLOGY, 2005, 183 (03) : 314 - 321
  • [4] Synthesis of ligands with mixed 5-HT1A and 5-HT2A receptor profile
    Cybulski, Marcin
    PRZEMYSL CHEMICZNY, 2007, 86 (08): : 764 - 767
  • [5] Anxiolytic-like effect of a serotonergic ligand with high affinity for 5-HT1A, 5-HT2A and 5-HT3 receptors
    Delgado, M
    Caicoya, AG
    Greciano, V
    Benhamú, B
    López-Rodríguez, ML
    Fernández-Alfonso, MS
    Pozo, MA
    Manzanares, J
    Fuentes, JA
    EUROPEAN JOURNAL OF PHARMACOLOGY, 2005, 511 (01) : 9 - 19
  • [6] The role of 5-HT2A receptor and 5-HT2A/5-HT1A receptor interaction in the suppression of catalepsy
    Naumenko, V. S.
    Bazovkina, D. V.
    Kondaurova, E. M.
    Zubkov, E. A.
    Kulikov, A. V.
    GENES BRAIN AND BEHAVIOR, 2010, 9 (05) : 519 - 524
  • [7] Calmodulin interacts with and modulates 5-HT1a and 5-HT2a receptors
    Raymond, J. R.
    Gelasco, A. K.
    Turner, J. H.
    JOURNAL OF PHARMACOLOGICAL SCIENCES, 2006, 101 : 58 - 58
  • [8] The therapeutic role of 5-HT1A and 5-HT2A receptors in depression
    Celada, P
    Puig, MV
    Amargós-Bosch, M
    Adell, A
    Artigas, F
    JOURNAL OF PSYCHIATRY & NEUROSCIENCE, 2004, 29 (04): : 252 - 265
  • [9] Buspirone analogues as ligands of the 5-HT1A receptor II: Capacity factors as chromatographic parameter of lipophilicity evaluation in a series of 5-HT1A and 5-HT2A receptor ligands
    Chilmonczyk, Z
    Ksycinska, H
    Cybulski, J
    WozniakowskaSzelejewska, A
    PHARMAZIE, 1996, 51 (12): : 924 - 927
  • [10] SSRI exerts anxiolytic effect via 5-HT1A and 5-HT2A receptors in the basolateral nucleus of amygdala (BLA)
    Izumi, Takeshi
    Wan, Ce
    Yoshioka, Mitsuhiro
    JOURNAL OF PHARMACOLOGICAL SCIENCES, 2017, 133 (03) : S129 - S129
12345