Document Detail


Effects of midazolam on intracellular Ca2+ and tension in airway smooth muscles.
MedLine Citation:
PMID:  7486152     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND: It has been demonstrated that a group of minor tranquilizers, benzodiazepines, are able to relax airway smooth muscles. To determine the underlying mechanisms of this phenomenon, the effects of midazolam on the intracellular Ca2+ concentration ([Ca2+]i) and tension in airway smooth muscles were investigated. METHODS: Using front-surface fluorometry and fura-2-loaded porcine tracheal smooth muscle strips, both [Ca2+]i and isometric tension developments were simultaneously recorded. RESULTS: When the tracheal strips were exposed to a high external K(+)-solution (40 mM) or 10(-7) M carbachol containing 1.25 mM Ca2+, both [Ca2+]i and tension increased rapidly until they reached a plateau (the steady state). During steady-state contraction induced by K(+)-depolarization or carbachol, the cumulative application of midazolam (10(-7) approximately 10(-4) M) caused decreases in both [Ca2+]i and tension, in a concentration-dependent manner. During 40 mM K(+)-induced depolarization, the stepwise increases in the extracellular Ca2+ concentration induced the stepwise increases in [Ca2+]i and tension. Midazolam (3 x 10(-5) M) inhibited these increases in [Ca2+]i and tension, but had no effect on the [Ca2+]i-tension relationship. In the presence of 3 x 10(-3) M NiCl2 (a nonselective cation channel blocker), midazolam (3 x 10(-5) M) did not cause any additional reduction of [Ca2+]i or tension during the contraction induced by carbachol (10(-7) M). In the absence of extracellular Ca2+, midazolam (3 x 10(-5) M) had no effect on the transient increases in either [Ca2+]i or the tension induced by carbachol (10(-7) M) or caffeine (20 mM). Pretreatment with both 10(-5) M flumazenil (a specific central antagonist of benzodiazepines) and 10(-5) M PK11195 (a specific peripheral antagonist of benzodiazepines) did not influence the effect of 10(-5) M midazolam on [Ca2+]i or tension during the contractions induced by carbachol. CONCLUSIONS: Midazolam directly relaxes airway smooth muscles by decreasing [Ca2+]i; this can be attributed to the inhibition of the influx of extracellular Ca2+. Midazolam has no effect on the release of stored Ca2+. In addition, midazolam has no effect on Ca2+ sensitivity of the contractile apparatus. Finally, benzodiazepine antagonists, flumazenil and PK11195, have no effect on this mechanism of direct action of midazolam on airway smooth muscles.
Authors:
H Yoshimura; T Kai; J Nishimura; S Kobayashi; S Takahashi; H Kanaide
Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anesthesiology     Volume:  83     ISSN:  0003-3022     ISO Abbreviation:  Anesthesiology     Publication Date:  1995 Nov 
Date Detail:
Created Date:  1995-12-21     Completed Date:  1995-12-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1300217     Medline TA:  Anesthesiology     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1009-20     Citation Subset:  AIM; IM    
Affiliation:
Department of Anesthesiology and Critical Care Medicine, Faculty of Medicine, Kyushu University, Fukuoka, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Anxiety Agents / pharmacology*
Calcium / metabolism*,  pharmacology
Drug Interactions
Flumazenil / pharmacology
Fluorometry
GABA Modulators / pharmacology
Intracellular Fluid / metabolism
Ion Transport
Isoquinolines / pharmacology
Midazolam / pharmacology*
Muscle Contraction / drug effects
Muscle, Smooth / drug effects*,  metabolism*
Potassium / pharmacology
Swine
Trachea / drug effects
Chemical
Reg. No./Substance:
0/Anti-Anxiety Agents; 0/GABA Modulators; 0/Isoquinolines; 59467-70-8/Midazolam; 7440-09-7/Potassium; 7440-70-2/Calcium; 78755-81-4/Flumazenil; 85340-56-3/PK 11195

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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