RESUMEN
A series of disulfonamidobenzo[a]quinolizines were synthesized and evaluated for their alpha 2- and alpha 1-adrenoceptor antagonist activity on the rat vas deferens and anococcygeus muscle, respectively. N-((2 beta,11b alpha)-1,3,4,6,7,11b-Hexahydro-2H-benzo[a]quinolizin-2-yl)-N- [2-[(methylsulfonyl)amino]ethyl]methanesulfonamide (4) and its N-[2-[(methylsulfonyl)amino]ethyl]ethanesulfonamide (22), N-[2-[(ethylsulfonyl)amino]ethyl]ethanesulfonamide (27), and N-[2-[(methylsulfonyl)amino]ethyl]-4-methylbenzenesulfonamide (30) analogues showed 400-fold or greater selectivity in favor of alpha 2- over alpha 1-adrenoceptor blockade.
Asunto(s)
Antagonistas Adrenérgicos alfa/síntesis química , Quinolizinas/síntesis química , Sulfonamidas/síntesis química , Animales , Fenómenos Químicos , Química , Masculino , Quinolizinas/farmacología , Ratas , Relación Estructura-Actividad , Sulfonamidas/farmacologíaAsunto(s)
Antibacterianos , Péptidos , Fenómenos Químicos , Química Física , Coloides , Computadores , Etanol , Concentración de Iones de Hidrógeno , Sustancias Macromoleculares , Matemática , Metanol , Modelos Estructurales , Peso Molecular , Péptidos Cíclicos , Tensión Superficial , Ultracentrifugación , UreaRESUMEN
Cross-sectional areas of bronchi and bronchial glands of pigs aged from 1 day to 10 months were measured using image analysis. Growth of the bronchial glands was slow for the first month of life, reached a maximum between 1 and 3 months, and slowed again after 5 months. Mucous gland sizes fell into two groups, one included the apical, cardiac and accessory lobes, the other the diaphragmatic lobes. From birth to maturity the percentage increase in mucous gland area of all lobes was very similar. For the anterior lobes, mucous glands and bronchial lumina grew in direct proportion to each other. Up to 1 month of age the bronchial lumina of the diaphragmatic lobes grew but the glands did not. Later, glands and lumina grew in direct proportion. From birth to maturity the percentage increase in bronchial cross-sectional area was similar for all lobes.
Asunto(s)
Bronquios/crecimiento & desarrollo , Glándulas Exocrinas/crecimiento & desarrollo , Porcinos/crecimiento & desarrollo , Factores de Edad , Animales , Animales Recién Nacidos , Femenino , Masculino , Moco , Reacción del Ácido Peryódico de SchiffRESUMEN
Pigs were given 6 daily injections of isoprenaline or pilocarpine. At necropsy the parotid, submaxillary and sublingual salivary glands were removed and weighed. Histological sections were prepared from several regions of each gland and the cross-sectional area of their acini was measured in treated and control animals by means of a Quantimet Image Analysis System. Both isoprenaline and pilocarpine produced a significant increase in the weight of the parotid and submaxillary glands, which was accompanied by an increase in acinar area. There was no change in the weight of the sublingual gland with either drug, but isoprenaline did induce an increase in the area of sublingual acini. A comparison is made of the changes in weight and structure of the salivary glands as shown by these methods.