ABSTRACT
Using the computer system SARD-21 (Structure Activity Relationship & Design) structural features of high- and low-effective anti-arrhythmic agents have been recognized and the influence of these features on the anti-arrhythmic properties has been evaluated. This information has been used for generation of the model for prediction of anti-arrhythmic effectiveness of pharmaceutical preparations with the 82%-level of recognition by two methods. The recognized structural parameters may be successfully used for design of new highly effective anti-arrhythmic drugs, and also for modification of structures of known anti-arrhythmic drugs for the increase of effectiveness of their anti-arrhythmic action.
Subject(s)
Amides/chemistry , Anti-Arrhythmia Agents/chemistry , Models, Theoretical , Quantitative Structure-Activity RelationshipABSTRACT
Ethyl ether of 11-deoxy-16-hydroxy-16-metylprostaglandin E1 (11-deoxymisoprostol) increases the contractile activity of uterine horn segments isolated from nonpregnant rats and produces abortive effect when given in a period of time within 1 - 16 days of pregnancy. The drug action is related to a decrease of the progesterone level in ovarian incubates of pregnant rats.
Subject(s)
Abortifacient Agents/pharmacology , Misoprostol/analogs & derivatives , Uterine Contraction/drug effects , Abortion, Induced , Animals , Female , In Vitro Techniques , Misoprostol/pharmacology , Ovary/drug effects , Ovary/metabolism , Pregnancy , Progesterone/metabolism , RatsABSTRACT
Unique stereochemistry of the third-generation beta-adrenoblockers is a basis of advantages of the new drugs such as carvedilol. Data on the stereochemistry beta-adrenoblockers and the influence of their optical activity on the pharmacological effects of related drugs are presented. Main steps in the practical invest gation of carvedilol stereoisomers are reviewed. Clinical aspects of the use of carvedilol, representing a racemic mixture of two enantiomers, in the treatment chronic heart failure, arterial hypertension, and coronary heart disease are considered.
Subject(s)
Adrenergic beta-Antagonists , Carbazoles , Propanolamines , Adrenergic beta-Antagonists/chemistry , Adrenergic beta-Antagonists/pharmacokinetics , Adrenergic beta-Antagonists/therapeutic use , Carbazoles/chemistry , Carbazoles/pharmacokinetics , Carbazoles/therapeutic use , Carvedilol , Humans , Propanolamines/chemistry , Propanolamines/pharmacokinetics , Propanolamines/therapeutic use , Stereoisomerism , Structure-Activity RelationshipABSTRACT
The experiments on mice showed that 2-methyl-4-amino-hydroxypyrimidine (MAHP) exhibits a pronounced immunostimulant action upon the animal organism under extremal conditions. The effect of MAHP is related to the preferential activation of immunocompetent cells responsible for the immunity.
