GANGLION-BLOCKING ACTIVITY OF DEQUALINIUM IN FROG AND RAT SYMPATHETIC-GANGLIA INVITRO

被引:7
作者
DUNN, PM
机构
[1] Department of Pharmacology, University College London, London, WC1E 6BT, Gower Street
基金
英国惠康基金;
关键词
DEQUALINIUM; SYMPATHETIC GANGLIA; GANGLION BLOCKERS; MUSCARINIC RECEPTOR ANTAGONISTS; NICOTINIC RECEPTOR ANTAGONISTS;
D O I
10.1016/0014-2999(93)90570-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of dequalinium on ganglionic transmission and responses to exogenous acetylcholine receptor agonists were studied in frog and rat sympathetic ganglia. In frog ganglia, dequalinium reduced ganglionic transmission (measured using gross extracellular recording) with an EC50 of 2 muM. At 1 muM, dequalinium produced non-surmountable antagonism of the ganglion depolarization evoked by nicotinic receptor activation. Dequalinium reduced the amplitude of evoked and spontaneous excitatory postsynaptic potentials recorded intracellularly from frog neurones, but had no effect on the action potential elicited by injection of a depolarizing current pulse. Hyperpolarizing and depolarizing responses to muscarine recorded extracellularly from frog ganglia were antagonized by 3 muM dequalinium. In rat ganglia, synaptic transmission and depolarization by an exogenous nicotinic agonist were only slightly inhibited by dequalinium at a concentration of 100 muM. At 30 muM, dequalinium produced a 17% reduction in the depolarization of this tissue by muscarine (I muM). These results add to the evidence of the diversity of nicotinic and muscarinic acetylcholine receptors, and indicate that dequalinium may be a valuable tool for the study of these receptors. However its usefulness as a probe for calcium-activated potassium channels may be limited by its actions at acetylcholine receptors.
引用
收藏
页码:335 / 339
页数:5
相关论文
共 19 条
[1]  
ARCAVA Y, 1984, FEBS LETT, V174, P267
[2]   STUDIES ON THE MECHANISM OF ACTION OF ACETYLCHOLINE ANTAGONISTS ON RAT PARASYMPATHETIC GANGLION-CELLS [J].
ASCHER, P ;
LARGE, WA ;
RANG, HP .
JOURNAL OF PHYSIOLOGY-LONDON, 1979, 295 (OCT) :139-170
[3]   DEPOLARIZATION OF RAT ISOLATED SUPERIOR CERVICAL-GANGLIA MEDIATED BY BETA-2-ADRENOCEPTORS [J].
BROWN, DA ;
DUNN, PM .
BRITISH JOURNAL OF PHARMACOLOGY, 1983, 79 (02) :429-439
[4]   DISSOCIATION OF ALPHA-BUNGAROTOXIN BINDING AND RECEPTOR BLOCK IN RAT SUPERIOR CERVICAL GANGLION [J].
BROWN, DA ;
FUMAGALLI, L .
BRAIN RESEARCH, 1977, 129 (01) :165-168
[5]  
CASTLE NA, 1987, THESIS U LONDON
[6]   ACTION OF AGONISTS AND ANTAGONISTS AT MUSCARINIC RECEPTORS PRESENT ON ILEUM AND ATRIA INVITRO [J].
CLAGUE, RU ;
EGLEN, RM ;
STRACHAN, AC ;
WHITING, RL .
BRITISH JOURNAL OF PHARMACOLOGY, 1985, 86 (01) :163-170
[7]   PARALYSING ACTIVITY OF SOME HETEROCYCLIC DECAMETHYLENE-ALPHA-OMEGA-BIS QUATERNARY AMMONIUM SALTS [J].
COLLIER, HOJ ;
TAYLOR, EP .
NATURE, 1949, 164 (4168) :491-492
[8]   FURTHER OBSERVATIONS ON THE BIOLOGICAL PROPERTIES OF DEQUALINIUM (DEQUADIN) AND HEDAQUINIUM (TEOQUIL) [J].
COLLIER, HOJ ;
COX, WA ;
HUSKINSON, PL ;
ROBINSON, FA .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1959, 11 (11) :671-680
[9]   ANTIBACTERIAL ACTIVITIES OF SOME BISISOQUINOLINIUM SALTS [J].
COLLIER, HOJ ;
POTTER, MD ;
TAYLOR, EP .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1953, 8 (01) :34-37
[10]   PHARMACOLOGICAL AND FUNCTIONAL DIVERSITY OF NEURONAL NICOTINIC ACETYLCHOLINE-RECEPTORS [J].
DENERIS, ES ;
CONNOLLY, J ;
ROGERS, SW ;
DUVOISIN, R .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1991, 12 (01) :34-40