Positive effects of allosteric modulators on the binding properties and the function of muscarinic acetylcholine receptors

被引:10
|
作者
Tucek, S
Jakubik, J
Dolezal, V
El-Fakahany, EE
机构
[1] Inst Physiol AV CR, Prague 14220, Czech Republic
[2] Univ Minnesota, Sch Med, Minneapolis, MN 55455 USA
关键词
muscarinic receptors; presynaptic receptors; allosteric regulation; alcuronium; acetylcholine;
D O I
10.1016/S0928-4257(98)80026-0
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
Data are reviewed indicating that allosteric modulators can enhance the affinities of muscarinic receptors for their antagonists and agonists, that the enhancement of the affinity for agonists is relevant functionally, and that the allosterically induced conformational change also affects the interaction between the receptors and the G proteins. ((C)Elsevier, Paris).
引用
收藏
页码:241 / 243
页数:3
相关论文
共 50 条
  • [21] Allosteric Drugs Acting at Muscarinic Acetylcholine Receptors
    Magali Waelbroeck
    Neurochemical Research, 2003, 28 : 419 - 422
  • [22] ALLOSTERIC MODULATION OF MUSCARINIC ACETYLCHOLINE-RECEPTORS
    TUCEK, S
    PROSKA, J
    TRENDS IN PHARMACOLOGICAL SCIENCES, 1995, 16 (06) : 205 - 212
  • [24] Elevation of ligand binding to muscarinic M2 acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators
    Raasch, A
    Scharfenstein, O
    Tränkle, C
    Holzgrabe, U
    Mohr, K
    JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (17) : 3809 - 3812
  • [25] Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors
    Shang, Yi
    Yeatman, Holly R.
    Provasi, Davide
    Alt, Andrew
    Christopoulos, Arthur
    Canals, Meritxell
    Filizola, Marta
    ACS CHEMICAL BIOLOGY, 2016, 11 (05) : 1220 - 1229
  • [26] Allosteric binding sites on muscarinic receptors
    Ellis, J
    DRUG DEVELOPMENT RESEARCH, 1997, 40 (02) : 193 - 204
  • [27] Evidence for a multiple binding mode of bispyridinium-type allosteric modulators of muscarinic receptors
    Kostenis, E
    Cid, HMB
    Holzgrabe, U
    Mohr, K
    EUROPEAN JOURNAL OF PHARMACOLOGY, 1996, 314 (03) : 385 - 392
  • [28] Neurosteroids and steroid hormones are allosteric modulators of muscarinic receptors
    Dolejsi, Eva
    Szanti-Pinter, Eszter
    Chetverikov, Nikolai
    Nelic, Dominik
    Randakova, Alena
    Dolezal, Vladimir
    Kudova, Eva
    Jakubik, Jan
    NEUROPHARMACOLOGY, 2021, 199
  • [29] Pharmacophore improvement of allosteric modulators of muscarinic receptors.
    Holzgrabe, U
    Cid, HMB
    Kostenis, E
    MiesKlomfass, E
    Mohr, K
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1997, 213 : 47 - MEDI
  • [30] The involvement of GABAB receptors in antipsychotic-like effects of positive allosteric modulator of muscarinic acetylcholine M4 receptors
    Cieslik, P.
    Wozniak, M.
    Pilc, A.
    Wieronska, J.
    EUROPEAN NEUROPSYCHOPHARMACOLOGY, 2017, 27 : S965 - S966