Abstract
To determine the mechanisms of receptor-dependent Ca2+ sensitization in airway smooth muscle, canine tracheal smooth muscle (CTSM) was permeabilized with alpha-toxin or beta-escin. Although the effects of 5-hydroxytryptamine (100 microM), histamine (100 microM), and the thromboxane A2 analogue U-46619 (100 microM) were negligible, carbachol (100 microM) and endothelin-1 (ET-1, 1 microM) evoked additional contractions of 47.0 +/- 5.90% and 25.0 +/- 5.37% (n = 6) at pCa 6.7 with GTP (3 microM) (normalized to the maximum contraction at pCa 4.5) in alpha-toxin-permeabilized CTSM. GDP-beta-S (1 mM) reversed the carbachol and ET-1 responses completely. GTP-gamma-S (30 microM) and 4 beta-phorbol 12,13-dibutyrate (PDBu, 3 microM) increased the Ca2+ sensitivity (median effective pCa) of contraction by 1.8- and 4.4-fold, respectively (n = 4-11, P < 0.05). The effects of saturating concentrations of GTP-gamma-S and PDBu were additive. A synthetic peptide (T2) corresponding to the actin-binding site of calponin caused a dose-dependent contraction of beta-escin permeabilized CTSM, with the peak effect (25 +/- 4%, n = 4) at 1200 microM, PDBu (3 microM) caused contraction of the T2 peptide-treated CTSM. In conclusion, Ca2+ sensitization of CTSM depends on receptor type and is mediated by G proteins and protein kinase C whose effects are additive, with a partial contribution by calponin.
MeSH terms
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15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
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Aluminum / pharmacology
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Animals
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Bacterial Toxins / pharmacology
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Calcium / metabolism*
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Calcium-Binding Proteins / metabolism
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Calponins
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Carbachol / pharmacology
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Cell Membrane Permeability / drug effects
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Dogs
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Endothelin-1 / pharmacology
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Escin / pharmacology
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Female
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Fluorine / pharmacology
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GTP-Binding Proteins / metabolism*
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Guanosine 5'-O-(3-Thiotriphosphate) / pharmacology
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Hemolysin Proteins / pharmacology
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Histamine / pharmacology
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Isometric Contraction
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Male
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Microfilament Proteins
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Muscle, Smooth / drug effects
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Muscle, Smooth / metabolism*
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Peptide Fragments / chemical synthesis
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Peptide Fragments / pharmacology
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Phorbol 12,13-Dibutyrate / pharmacology
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Prostaglandin Endoperoxides, Synthetic / pharmacology
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Protein Kinase C / drug effects
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Protein Kinase C / metabolism
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Receptors, Muscarinic / drug effects
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Receptors, Muscarinic / metabolism*
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Serotonin / pharmacology
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Thromboxane A2 / analogs & derivatives
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Thromboxane A2 / pharmacology
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Trachea / anatomy & histology
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Trachea / metabolism*
Substances
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Bacterial Toxins
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Calcium-Binding Proteins
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Endothelin-1
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Hemolysin Proteins
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Microfilament Proteins
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Peptide Fragments
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Prostaglandin Endoperoxides, Synthetic
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Receptors, Muscarinic
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staphylococcal alpha-toxin
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fluoroaluminum
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Fluorine
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Serotonin
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Phorbol 12,13-Dibutyrate
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Guanosine 5'-O-(3-Thiotriphosphate)
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Thromboxane A2
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Escin
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15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
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Histamine
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Carbachol
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Aluminum
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Protein Kinase C
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GTP-Binding Proteins
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Calcium