CONFORMATIONAL-ANALYSIS AND RECEPTOR MODELING OF M1 AND M2 SELECTIVE ANTAGONISTS

被引:0
|
作者
KERCKHOFF, H [1 ]
HOLTJE, HD [1 ]
机构
[1] FREIEN UNIV,INST PHARM,D-14195 BERLIN,GERMANY
来源
PHARMAZIE | 1994年 / 49卷 / 08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
On the basis of an elaborate conformational analysis of m1- and m2-selective antagonists a respective pharmacophore was deduced. This then was introduced into models of the two muscarinic receptor subtypes. These models were constructued starting from bacteriorhodopsin as a template in accordance with alignment data and mutation experiments. The validity of the interaction geometries between ligands and receptor subtypes is supported by a significant correlation between calculated interaction energies and experimentally determined affinity data.
引用
收藏
页码:566 / 573
页数:8
相关论文
共 50 条
  • [1] SELECTIVE AGONISTS AND ANTAGONISTS OF M1 AND M2 MUSCARINE RECEPTORS
    GOYAL, RK
    RATTAN, S
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1984, 188 (AUG): : 47 - MEDI
  • [2] Muscarinic M1 receptor agonists and M2 receptor antagonists as therapeutic targets in Alzheimer's disease
    Sheardown, MJ
    EXPERT OPINION ON THERAPEUTIC PATENTS, 2002, 12 (06) : 863 - 870
  • [3] Identification and characterization of m1 selective muscarinic receptor antagonists
    Augelli-Szafran, CE
    Blankley, CJ
    Jaen, JC
    Moreland, DW
    Nelson, CB
    Penvose-Yi, JR
    Schwarz, RD
    Thomas, AJ
    JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (03) : 356 - 363
  • [4] MUSCARINIC M1 CONTRARY TO M2 ANTAGONISTS DO NOT INDUCE ANALGESIA
    GHELARDINI, C
    GIOTTI, A
    GUALTIERI, F
    MALCANGIO, M
    MALMBERGAIELLO, P
    SCAPECCHI, S
    BARTOLINI, A
    TRENDS IN PHARMACOLOGICAL SCIENCES, 1989, : 99 - 99
  • [5] Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor
    Kozlowski, JA
    Lowe, DB
    Guzik, HS
    Zhou, GW
    Ruperto, VB
    Duffy, RA
    McQuade, R
    Crosby, G
    Taylor, LA
    Billard, W
    Binch, H
    Lachowicz, JE
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (20) : 2255 - 2257
  • [6] Analysis of M1, M2/M1, M2/N Retrial Queue System with Non-preemptive Priority
    Zhou, Zonghao
    PROCEEDINGS OF 2018 IEEE 9TH INTERNATIONAL CONFERENCE ON SOFTWARE ENGINEERING AND SERVICE SCIENCE (ICSESS), 2018, : 301 - 304
  • [8] Differential effects of m1 and m2 receptor antagonists in perirhinal cortex on visual recognition memory in monkeys
    Wu, Wei
    Saunders, Richard C.
    Mishkin, Mortimer
    Turchi, Janita
    NEUROBIOLOGY OF LEARNING AND MEMORY, 2012, 98 (01) : 41 - 46
  • [9] PHARMACOLOGIC IDENTIFICATION OF MUSCARINIC M1 AND M2 RECEPTOR SUBTYPES
    GILBERT, R
    RATTAN, S
    GOYAL, RK
    GASTROENTEROLOGIE CLINIQUE ET BIOLOGIQUE, 1983, 7 (8-9): : 704 - 705
  • [10] PHARMACOLOGIC IDENTIFICATION OF MUSCARINIC M1 AND M2 RECEPTOR SUBTYPES
    GILBERT, R
    RATTAN, S
    GOYAL, RK
    GASTROENTEROLOGY, 1983, 84 (05) : 1166 - 1166