BINDING OF TROPANE ALKALOIDS TO NICOTINIC AND MUSCARINIC ACETYLCHOLINE RECEPTORS

被引:0
|
作者
SCHMELLER, T [1 ]
SPORER, F [1 ]
SAUERWEIN, M [1 ]
WINK, M [1 ]
机构
[1] UNIV HEIDELBERG,INST PHARMAZEUT BIOL,D-69120 HEIDELBERG,GERMANY
来源
PHARMAZIE | 1995年 / 50卷 / 07期
关键词
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Fourteen tropane and related alkaloids were analyzed for their affinity for nicotinic and/or muscarinic acetylcholine receptors. The biogenetic intermediates littorine, 6 beta-hydroxyhyoscyamine, 7 beta-hydroxyhyoscyamine exhibit similar affinities at the muscarinic receptor as scopolamine and atropine. The quarternary derivatives N-methylatropine and N-methylscopolamine show the highest binding with IC50 values of less than 100 pM and 300 pM, respectively. The tropane alkaloids (including cocaine) also bind to the nicotinic acetylcholine receptor, albeit with much lower affinities.
引用
收藏
页码:493 / 495
页数:3
相关论文
共 50 条
  • [21] COMPARISON OF ACTION OF ACETYLCHOLINE AND ACETYLCHOLINE MUSTARD (CHLOROETHYL-METHYLAMINOETHYL ACETATE) ON MUSCARINIC AND NICOTINIC RECEPTORS
    HUDGINS, PM
    STUBBINS, JF
    JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 1972, 182 (02): : 303 - &
  • [22] Molecular Recognition of the Neurotransmitter Acetylcholine by an Acetylcholine Binding Protein Reveals Determinants of Binding to Nicotinic Acetylcholine Receptors
    Olsen, Jeppe A.
    Balle, Thomas
    Gajhede, Michael
    Ahring, Philip K.
    Kastrup, Jette S.
    PLOS ONE, 2014, 9 (03):
  • [23] MUSCARINIC ACETYLCHOLINE RECEPTORS
    UCHIDA, S
    TAKEYASU, K
    YONEHARA, N
    YOSHIDA, H
    JAPANESE JOURNAL OF PHARMACOLOGY, 1978, 28 : P22 - P22
  • [24] RC-4BC cells express nicotinic and muscarinic acetylcholine receptors
    Zhubanova, Gulsamal
    Filchakova, Olena
    PLOS ONE, 2022, 17 (12):
  • [25] CONTRIBUTION OF NICOTINIC AND MUSCARINIC RECEPTORS IN THE SECRETION OF CATECHOLAMINES EVOKED BY ENDOGENOUS AND EXOGENOUS ACETYLCHOLINE
    WAKADE, AR
    WAKADE, TD
    NEUROSCIENCE, 1983, 10 (03) : 973 - 978
  • [26] Muscarinic acetylcholine receptors
    Ishii, Masaru
    Kurachi, Yoshihisa
    CURRENT PHARMACEUTICAL DESIGN, 2006, 12 (28) : 3573 - 3581
  • [27] IDENTIFICATION OF NICOTINIC AND MUSCARINIC ACETYLCHOLINE RECEPTORS IN SUBCELLULAR-FRACTIONS OF MOUSE BRAIN
    SCHLEIFER, LS
    ELDEFRAWI, ME
    NEUROPHARMACOLOGY, 1974, 13 (01) : 53 - 63
  • [28] Acetylcholine Promotes Binding of α-Conotoxin MII at α3β2 Nicotinic Acetylcholine Receptors
    Sambasivarao, Somisetti V.
    Roberts, Jessica
    Bharadwaj, Vivek S.
    Slingsby, Jason G.
    Rohleder, Conrad
    Mallory, Chris
    Groome, James R.
    McDougal, Owen M.
    Maupin, C. Mark
    CHEMBIOCHEM, 2014, 15 (03) : 413 - 424
  • [29] Acetylcholine-binding proteins - Functional and structural hornologs of nicotinic acetylcholine receptors
    Smit, August B.
    Celie, Patrick H. N.
    Kasheverov, Igor E.
    Mordvintsev, Dmitry Y.
    van Nierop, Pim
    Bertrand, Daniel
    Tsetlin, Victor
    Sixma, Titia K.
    JOURNAL OF MOLECULAR NEUROSCIENCE, 2006, 30 (1-2) : 9 - 10
  • [30] Nicotinic acetylcholine receptors
    Dmitrieva, N
    Wang, Y
    Lindstrom, JM
    Keyser, KT
    INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE, 1997, 38 (04) : 227 - 227