[Effect of a new selective alpha 2 adrenergic blocker, midaglizole, on isolated airway smooth muscle]. 1990

M Mizobe
Second Department of Medicine, Teikyo University School of Medicine.

The role of alpha-adrenoceptors in asthma is still unclear. However, several studies have shown bronchodilatation after single doses of different alpha-adrenoceptor antagonists in patient's with asthma. The clinical efficacy of midaglizole, a new selective alpha 2 blocker was demonstrated by a more recent investigation. The present investigation was carried out to examine the effects of midaglizole on isolated airway smooth muscle obtained from humans and guinea pigs. Human bronchial smooth muscle was relaxed in a dose-dependent manner by midaglizole. EC50, molar concentration of midaglizole required to produce 50% reversal of carbachol-induced pre-contraction was (6.0 +/- 0.19) X 10(-5) M. Isoproterenol (5 X 10(-10) M) and midaglizole (3 X 10(-5) M) produced 30.0 +/- 9.5% and 40.8 +/- 7.0% of maximal relaxation, respectively. However, they produced almost 100% of maximal relaxation when used together. Isoproterenol, in combination with midaglizole, was associated with a significant increase of human bronchial relaxation as compared to either of the drugs singly. The same findings were obtained when the drugs were used on the guinea pig trachea. Midaglizole had no effect on the binding of the radiolabeled beta adrenergic antagonist [3H] dihydroalprenolol to particulates prepared from the lung. Propranolol did not inhibit the relaxant effect of midaglizole on airway smooth muscle. These results suggest that midaglizole may be effective for the treatment of asthma.

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D007545 Isoproterenol Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant. Isoprenaline,Isopropylarterenol,4-(1-Hydroxy-2-((1-methylethyl)amino)ethyl)-1,2-benzenediol,Euspiran,Isadrin,Isadrine,Isopropyl Noradrenaline,Isopropylnoradrenaline,Isopropylnorepinephrine,Isoproterenol Hydrochloride,Isoproterenol Sulfate,Isuprel,Izadrin,Norisodrine,Novodrin,Hydrochloride, Isoproterenol,Noradrenaline, Isopropyl,Sulfate, Isoproterenol
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D009126 Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position. Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D009130 Muscle, Smooth Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed) Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D001980 Bronchi The larger air passages of the lungs arising from the terminal bifurcation of the TRACHEA. They include the largest two primary bronchi which branch out into secondary bronchi, and tertiary bronchi which extend into BRONCHIOLES and PULMONARY ALVEOLI. Primary Bronchi,Primary Bronchus,Secondary Bronchi,Secondary Bronchus,Tertiary Bronchi,Tertiary Bronchus,Bronchi, Primary,Bronchi, Secondary,Bronchi, Tertiary,Bronchus,Bronchus, Primary,Bronchus, Secondary,Bronchus, Tertiary
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004357 Drug Synergism The action of a drug in promoting or enhancing the effectiveness of another drug. Drug Potentiation,Drug Augmentation,Augmentation, Drug,Augmentations, Drug,Drug Augmentations,Drug Potentiations,Drug Synergisms,Potentiation, Drug,Potentiations, Drug,Synergism, Drug,Synergisms, Drug
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea

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