RESUMEN
The paper reports a method for studying mucosecretolytic drugs in the mouse. After i.p. application of phenol red, part of the dye is secreted in the tracheobronchial tract and collected by lung washings with saline. The concentration of secreted phenol red is measured photometrically at 546 nm. All the most important expectorant drugs increase the tracheobronchial secretion of phenol red in the mouse. The ED50 values, calculated as mg/kg, show practically the same activity for N-acetylcysteine, Tiopronine, SF-1284 and S-carboxymethylcysteine, and a lower activity for Ambroxol and Sobrerol. The method was validated for reproducibility utilizing Tiopronine in many experiments performed over twelve months.
Asunto(s)
Bronquios/metabolismo , Expectorantes/farmacología , Fenolsulfonftaleína , Tráquea/metabolismo , Animales , Bronquios/efectos de los fármacos , Femenino , Ratones , Moco/efectos de los fármacos , Moco/metabolismo , Fenolftaleínas , Factores de Tiempo , Tráquea/efectos de los fármacosRESUMEN
Synthesis and pharmacological properties of the 5-fluoro-nicotinic ester with isosorbide-5-mononitrate 3 are reported. The new compound shows an in vitro activity on rabbit aortic helical strips five times higher than isosorbide-5-mononitrate. The hypotensive activity in guinea-pigs of 3 is markedly superior to that of 5-ISMN. In the rat 3 shows a bioavailability and an acute toxicity inferior to those of 5-ISMN after oral administration.
Asunto(s)
Antihipertensivos/síntesis química , Dinitrato de Isosorbide/análogos & derivados , Animales , Antihipertensivos/toxicidad , Presión Sanguínea/efectos de los fármacos , Fenómenos Químicos , Química , Femenino , Cobayas , Técnicas In Vitro , Dinitrato de Isosorbide/síntesis química , Dinitrato de Isosorbide/farmacología , Dinitrato de Isosorbide/toxicidad , Masculino , Ratones , Conejos , Ratas , Ratas EndogámicasRESUMEN
The synthesis of triethylphosphine gold complex with the alpha-mercaptopropionylglycine ethyl ester (compound 3) is reported. The new compound shows an antiinflammatory and antiarthritic activity superior to auranofin.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Artritis Experimental/tratamiento farmacológico , Artritis/tratamiento farmacológico , Oro/farmacología , Tiopronina/síntesis química , Animales , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/uso terapéutico , Oro/uso terapéutico , Masculino , Ratones , Ratas , Ratas Endogámicas , Tiopronina/farmacología , Tiopronina/uso terapéuticoRESUMEN
The effects of 3 alpha, 7 beta-dihydroxy-12-cheto-cholan-24-oic acid (SF-482) were compared with those of ursodeoxycholic acid on bile flow and composition, on gallstones formation and on experimental hyperlipemias. SF-482, like ursodeoxycholic acid, increases the bile flow and residue in normal and ethynylestradiol-treated rats. The two compounds increase the biliary excretion of bile acids and phospholipids with a desaturation of bile cholesterol. SF-482 and ursodeoxycholic acid decrease the incidence of gallstones in mice; both compounds are active in Triton WR-1339, in olive oil and margarine hyperlipemias in rats and in ethanol intoxication in mice. In general, SF-482 is more active than ursodeoxycholic acid.
Asunto(s)
Bilis/efectos de los fármacos , Ácido Quenodesoxicólico/análogos & derivados , Colelitiasis/prevención & control , Ácido Desoxicólico/análogos & derivados , Hiperlipidemias/prevención & control , Hipolipemiantes/farmacología , Ácido Ursodesoxicólico/farmacología , Intoxicación Alcohólica , Animales , Ácido Quenodesoxicólico/farmacología , Colesterol/metabolismo , Femenino , Masculino , Ratones , Fosfolípidos/metabolismo , Ratas , Ratas Endogámicas , Factores de TiempoAsunto(s)
Expectorantes/síntesis química , Pirrolidinonas/síntesis química , Compuestos de Sulfhidrilo/síntesis química , Tiofenos/síntesis química , Animales , Fenómenos Químicos , Química , Femenino , Cobayas , Técnicas In Vitro , Masculino , Ratones , Pirrolidinonas/farmacología , Pirrolidinonas/toxicidad , Ratas , Ratas Endogámicas , Compuestos de Sulfhidrilo/farmacología , Compuestos de Sulfhidrilo/toxicidad , Porcinos , Tiofenos/farmacología , Tiofenos/toxicidadRESUMEN
Diacetylrhein (DAR) is a new anti-inflammatory and anti-osteoarthritic drug. Studies with isolated lung preparation showed that DAR does not exert its action by inhibiting the arachidonic acid metabolism. Furthermore, the in vivo experiments showed that DAR, contrary to most anti-inflammatory drugs, induced an increase of prostaglandin-like substances in the rat exudates. The above results are substantiated by experimental evidence that in the rat this compound displays a dose-dependent protecting activity against indomethacin-induced gastric damage.