ABSTRACT
Four new ST-1435 derivatives 4-7 were synthesized. Both 4 and 5 are mixture of Z- and E-isomers. 4 was separated into Z- and E-isomers by spinning TLC. Their binding ability to progesterone receptor was examined and found to be less than ST-1435.
Subject(s)
Contraceptive Agents, Female/chemical synthesis , Norprogesterones/chemical synthesis , Animals , Breast Feeding , Female , Lactation , Norprogesterones/metabolism , Rats , Receptors, Progesterone/metabolismABSTRACT
In an effort to study the structure-activity relationship of analogs of baclofen and to search for more potent and less toxic muscle relaxants and analgesics, fifteen 3-substituted pheny-4-aminobutyric acids and their derivatives were synthesized. Preliminary pharmacological tests in albino mice showed that some of the target compounds exhibited muscle relaxant and analgesic effects. Compounds Ib, IIb, IIIa, IIIc and compounds Ib, IIb, IIIa, IIIb were, respectively, more potent in hot plate tests and morphine-induced straub tail reaction tests than other analogs, but they were still less potent than baclofen. The structure-activity relationship showed that the effects of baclofen were strongly structure specific, and the results also suggested that at least three groups in baclofen-phenyl, amino and carboxy--take important parts in the combination of baclofen with GABAB receptor.
Subject(s)
Baclofen/chemical synthesis , Animals , Baclofen/analogs & derivatives , Baclofen/pharmacology , Female , Male , Mice , Muscle Relaxation/drug effects , Pain/physiopathology , Receptors, GABA-A/drug effects , Sensory Thresholds/drug effects , Structure-Activity RelationshipABSTRACT
This paper describes that the absorption spectrum of bilirubin solution was changed obviously by photo-oxidation. The absorbance was measured at 453 nm before and after light irradiation. The contents of bilirubin of ox gallstone in Liuying pills, Liushen pills and Niuhuang Xiaoyan pills were determined by differential absorbance (delta A). Calibration graph was linear in the range of 1.6-8.0 micrograms/ml for delta A. The average recoveries for three Chinese patent medicines were over 93%. Determinations of bilirubin in Chinese patent medicines were not affected by other components.
Subject(s)
Bilirubin/analysis , Cholelithiasis/chemistry , Materia Medica/chemistry , Animals , Cattle , Cholelithiasis/veterinary , Drug Combinations , Male , Spectrophotometry/methodsSubject(s)
Anti-Arrhythmia Agents , Arrhythmias, Cardiac/drug therapy , Morpholines/therapeutic use , Animals , Cats , Female , Guinea Pigs , Hemodynamics , Lidocaine/therapeutic use , Male , Mice , Morpholines/toxicity , Rats , Rats, Inbred StrainsABSTRACT
Numerous organic silver salts have been tested against a virulent strain of Pseudomonas aeruginosa which had been deliberately applied to the scalded tails of mice and deeper scald wounds on the backs of rabbits. Silver pipemidate was found to be more effective than silver sulphadiazine in treating these infected wounds.
