Oral bronchodilator effect of 16(S)-methyl-20-methoxy-PGE2 (YPG-209) in guinea-pigs. 1977

K Tomioka, and M Terai, and H Maeno

The bronchodilator activity of synthetic 16(S)-methyl-20-methoxy-PGE2 (YPG-209) was investigated in guinea-pigs. The potency of YPG-209 in relaxing the isolated trachea contracted by histamine was 10 times smaller than that of PGE2, and was not reduced by propranolol, while in the anesthetized animals YPG-209 given by an intravenous route was 230 times as potent in inhibiting an increase in the airway resistance induced by histamine as PGE2. When administered either intraduodenally to the anesthetized animals or orally to the conscious ones, YPG-209 showed a pronounced protection against histamine-induced bronchoconstriction, in contrast to PGE2 which had no significant protecting effect. Neither hypotension nor diarrhea could be observed at the doses of YPG-209 exhibiting a considerable bronchodilator effect. The hydroxyl group at carbon-15 of YPG-209 was little oxidized by 15-hydroxy prostaglandin dehydrogenase which was purified from the lung of guinea-pigs, consistent with the comparably long lasting bronchodilator activity of YPG-209 in vivo.

UI MeSH Term Description Entries
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
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D011458 Prostaglandins E (11 alpha,13E,15S)-11,15-Dihydroxy-9-oxoprost-13-en-1-oic acid (PGE(1)); (5Z,11 alpha,13E,15S)-11,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid (PGE(2)); and (5Z,11 alpha,13E,15S,17Z)-11,15-dihydroxy-9-oxoprosta-5,13,17-trien-1-oic acid (PGE(3)). Three of the six naturally occurring prostaglandins. They are considered primary in that no one is derived from another in living organisms. Originally isolated from sheep seminal fluid and vesicles, they are found in many organs and tissues and play a major role in mediating various physiological activities. PGE
D011465 Prostaglandins, Synthetic Compounds obtained by chemical synthesis that are analogs or derivatives of naturally occurring prostaglandins and that have similar activity. PG Analog,PG Analogs,Prostaglandin Analog,Prostaglandin Analogs,Prostaglandin Analogue,Synthetic Prostaglandin,Prostaglandin Analogues,Synthetic Prostaglandins,Analog, PG,Analog, Prostaglandin,Analogs, PG,Analogs, Prostaglandin,Analogue, Prostaglandin,Analogues, Prostaglandin,Prostaglandin, Synthetic
D001993 Bronchodilator Agents Agents that cause an increase in the expansion of a bronchus or bronchial tubes. Bronchial-Dilating Agents,Bronchodilator,Bronchodilator Agent,Broncholytic Agent,Bronchodilator Effect,Bronchodilator Effects,Bronchodilators,Broncholytic Agents,Broncholytic Effect,Broncholytic Effects,Agent, Bronchodilator,Agent, Broncholytic,Agents, Bronchial-Dilating,Agents, Bronchodilator,Agents, Broncholytic,Bronchial Dilating Agents,Effect, Bronchodilator,Effect, Broncholytic,Effects, Bronchodilator,Effects, Broncholytic
D003967 Diarrhea An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight. Diarrheas
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
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
D000403 Airway Resistance Physiologically, the opposition to flow of air caused by the forces of friction. As a part of pulmonary function testing, it is the ratio of driving pressure to the rate of air flow. Airway Resistances,Resistance, Airway,Resistances, Airway
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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