Allosterism at muscarinic receptors: Ligands and mechanisms

被引:88
作者
Birdsall, NJM
Lazareno, S
机构
[1] Natl Inst Med Res, Div Phys Biochem, London NW7 1AA, England
[2] MRC Technol, London NW7 1AA, England
基金
英国医学研究理事会;
关键词
muscarinic receptors; allosterism; cooperativity; enhancers; receptor models; structure-activity relationships; interaction studies; receptor subtype selectivity;
D O I
10.2174/1389557054023251
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The evaluation of allosteric ligands at muscarinic receptors is discussed in terms of the ability of the experimental data to be interpreted by the allosteric ternary complex model. The compilation of useful SAR information of allosteric ligands is not simple, especially for muscarinic receptors, where there are multiple allosteric sites and complex interactions.
引用
收藏
页码:523 / 543
页数:21
相关论文
共 190 条
[1]  
[Anonymous], ARCH GES PHYSL
[2]   COMPARISON OF AFFINITY CONSTANTS FOR MUSCARINE-SENSITIVE ACETYLCHOLINE RECEPTORS IN GUINEA-PIG ATRIAL PACEMAKER CELLS AT 29 DEGREESC AND IN ILEUM AT 29 DEGREESC AND 37 DEGREESC [J].
BARLOW, RB ;
BERRY, KJ ;
GLENTON, PAM ;
NIKOLAOU, NM ;
SOH, KS .
BRITISH JOURNAL OF PHARMACOLOGY, 1976, 58 (04) :613-620
[4]   A STABLE AND HIGHLY POTENT HEXAMETHONIUM DERIVATIVE WHICH MODULATES MUSCARINIC RECEPTORS ALLOSTERICALLY IN GUINEA-PIG HEARTS [J].
BEJEUHR, G ;
BLASCHKE, G ;
HOLZGRABE, U ;
MOHR, K ;
SURIG, U ;
TERFLOTH, G .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1994, 46 (02) :108-112
[5]  
BEJEUHR G, 1992, PHARM PHARM LETT, V2, P100
[6]  
BENBARUCH G, 1982, MOL PHARMACOL, V21, P287
[7]   Probing the size of a hydrophobic binding pocket within the allosteric site of muscarinic acetylcholine M2-receptors [J].
Bender, W ;
Staudt, M ;
Tränkle, C ;
Mohr, K ;
Holzgrabe, U .
LIFE SCIENCES, 2000, 66 (18) :1675-1682
[8]  
Bernard C., 1878, Lecons sur les phenomenes de la vie communs aux animaux et aux vegetaux
[9]  
BIRDSALL NJM, 1978, MOL PHARMACOL, V14, P723
[10]   THE EFFECT OF MCN-A-343 ON MUSCARINIC RECEPTORS IN THE CEREBRAL-CORTEX AND HEART [J].
BIRDSALL, NJM ;
BURGEN, ASV ;
HULME, EC ;
STOCKTON, JM ;
ZIGMOND, MJ .
BRITISH JOURNAL OF PHARMACOLOGY, 1983, 78 (02) :257-259