Allosteric drugs acting at muscarinic acetylcholine receptors

被引:8
|
作者
Waelbroeck, M [1 ]
机构
[1] Free Univ Brussels, Sch Med, Dept Biochem & Nutr, B-1070 Brussels, Belgium
关键词
muscarinic receptors; allosteric drugs; facilitator effects; subtype selectivity; gallamine; alcuronium;
D O I
10.1023/A:1022888332221
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The binding properties of muscarinic acetylcholine receptors are affected by various drugs acting at a second (allosteric) binding site, usually (but not always) at supratherapeutic concentrations. Allosteric drugs acting at GABA receptors present advantages over competitive drugs; this explains the interest raised by allosteric effects on muscarinic receptors. A theoretical and practicable definition of allosteric drugs acting at muscarinic receptors will be given in this work, together with a summary of recent data concerning, the number, position, and structural requirements of their binding sites.
引用
收藏
页码:419 / 422
页数:4
相关论文
共 50 条
  • [1] Allosteric Drugs Acting at Muscarinic Acetylcholine Receptors
    Magali Waelbroeck
    [J]. Neurochemical Research, 2003, 28 : 419 - 422
  • [2] Allosteric modulation of muscarinic acetylcholine receptors
    Tucek, S
    Dolezal, V
    Jakubík, J
    Krejcíi, A
    Lysíková, M
    [J]. 5TH CONGRESS OF THE EUROPEAN SOCIETY FOR CLINICAL NEUROPHARMACOLOGY, 2000, : 117 - 123
  • [3] Allosteric modulation of muscarinic acetylcholine receptors
    Gregory, Karen J.
    Sexton, Patrick M.
    Christopoulos, Arthur
    [J]. CURRENT NEUROPHARMACOLOGY, 2007, 5 (03) : 157 - 167
  • [4] Allosteric regulation of muscarinic acetylcholine receptors
    Tucek, S
    Jakubik, J
    ElFakahany, EE
    Bacakova, L
    [J]. JOURNAL OF NEUROCHEMISTRY, 1996, 66 : S73 - S73
  • [5] Allosteric Modulation of Muscarinic Acetylcholine Receptors
    Jakubik, Jan
    El-Fakahany, Esam E.
    [J]. PHARMACEUTICALS, 2010, 3 (09): : 2838 - 2860
  • [6] Allosteric binding sites on muscarinic acetylcholine receptors
    Wess, J
    [J]. MOLECULAR PHARMACOLOGY, 2005, 68 (06) : 1506 - 1509
  • [7] ALLOSTERIC MODULATION OF MUSCARINIC ACETYLCHOLINE-RECEPTORS
    TUCEK, S
    PROSKA, J
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1995, 16 (06) : 205 - 212
  • [8] Muscarinic acetylcholine receptors: basic properties and allosteric regulation
    Tucek, S
    Dolezal, V
    [J]. JOURNAL OF PHYSIOLOGY-LONDON, 1998, 511P : 2S - 2S
  • [9] Allosteric modulators of ligand binding to muscarinic acetylcholine receptors
    Holzgrabe, U
    Mohr, K
    [J]. DRUG DISCOVERY TODAY, 1998, 3 (05) : 214 - 222
  • [10] Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    Jakubik, J
    Bacakova, L
    ElFakahany, EE
    Tucek, S
    [J]. MOLECULAR PHARMACOLOGY, 1997, 52 (01) : 172 - 179