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PMID: 10742306 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Effects of inhibitors of small- and intermediate-conductance calcium-activated potassium channels, inwardly-rectifying potassium channels and Na(+)/K(+) ATPase on EDHF relaxations in the rat hepatic artery.

British journal of pharmacology ·Vol. 129 ·No. 7 ·2000-04-00 ·Pages 1490-6

Andersson DA, Zygmunt PM, Movahed P, Andersson TL, Högestätt ED

Abstract

1. In the rat hepatic artery, the SK(Ca) inhibitors UCL 1684 (300 nM) completely blocked, and scyllatoxin (1 microM) and d-tubocurarine (100 microM) partially inhibited EDHF relaxations when each of them was combined with charybdotoxin (300 nM). 2. The IK(Ca) inhibitors clotrimazole (3 microM) and 2-chlorophenyl-bisphenyl-methanol (3 microM) strongly depressed EDHF relaxations when each of them was combined with apamin (300 nM). The cytochrome P450 mono-oxygenase inhibitor ketoconazole (10 microM) had no effect in the presence of apamin. 3. Ciclazindol (10 microM), which abolishes EDHF relaxations in the presence of apamin, almost completely prevented the calcium ionophore (A23187) stimulated (86)Rb(+) influx via the Gardos channel (IK(Ca)) in human erythrocytes. 4. The Na(+)/K(+) ATPase inhibitor ouabain (500 microM) and the K(IR) blocker Ba(2+) (30 microM) neither alone nor in combination inhibited EDHF relaxations. Ba(2+) was also without effect in the presence of either apamin or charybdotoxin. 5. In contrast to EDHF, an increase in extracellular [K(+)] from 4.6 mM to 9.6, 14.6 and 19.6 mM inconsistently relaxed arteries. In K(+)-free physiological salt solution, re-admission of K(+) always caused complete and sustained relaxations which were abolished by ouabain but unaffected by Ba(2+). 6. The present study provides pharmacological evidence for the involvement of SK(Ca) and IK(Ca) in the action of EDHF in the rat hepatic artery. Our results are not consistent with the idea that EDHF is K(+) activating Na(+)/K(+) ATPase and K(IR) in this blood vessel.

MeSH Terms
Acetylcholine/pharmacology Alkanes/pharmacology Animals Barium/pharmacology Biological Factors/pharmacology Calcium/physiology Clotrimazole/metabolism,pharmacology Dose-Response Relationship, Drug Electric Conductivity Enzyme Inhibitors/pharmacology Erythrocytes/drug effects,metabolism Female Hepatic Artery/drug effects,physiology Humans In Vitro Techniques Indoles/pharmacology Ketoconazole/pharmacology Ouabain/pharmacology Potassium/pharmacology Potassium Channel Blockers Potassium Channels/physiology Quinolinium Compounds/pharmacology Rats Rats, Sprague-Dawley Rubidium Radioisotopes/metabolism Scorpion Venoms/pharmacology Sodium-Potassium-Exchanging ATPase/antagonists & inhibitors,metabolism Tubocurarine/pharmacology Vasodilation/drug effects
Chemicals
6,10-diaza-3(1,3),8(1,4)dibenzena-1,5(1,4)diquinolinacyclodecaphane Alkanes Biological Factors Enzyme Inhibitors Indoles Potassium Channel Blockers Potassium Channels Quinolinium Compounds Rubidium Radioisotopes Scorpion Venoms endothelium-dependent hyperpolarization factor leiurotoxin I Barium Ouabain Sodium-Potassium-Exchanging ATPase Clotrimazole Acetylcholine Ketoconazole Potassium Calcium Tubocurarine ciclazindol
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Andersson D A
Department of Clinical Pharmacology, Institute of Laboratory Medicine, Lund University, SE-221 85 Lund, Sweden.
Zygmunt P M
Movahed P
Andersson T L
Högestätt E D
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Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
Published
2000-04-00
Pages
1490-6
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1571979
Subset
IM
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