About the Book

This book assembles most of the methods for screening substances for pharmacological activity and includes discussions of the organization of screening programs. While screening is widely practiced in pharmacology laboratories, a definition of its meaning is perhaps worthy of attention. The term screening indicates the use of a combination of tests for the purpose of making a decision. The results of the tests provide information on the presence of certain pharmacological properties. A decision whether the tested substance should be studies further may be founded on that information. Incidentally, the direction of further study may also be determined by this information. The operation of retaining from a group of substances those possessing a certain property is fundamental. Screening is the most efficient method of detection and of decision-making in any empirical operation. The finding of substances with a pharmacological property is empirical because no general theory correlating such a property with molecular structure exists. The author tried to collect the simplest and most widely used methods. Absolute completeness has not been attempted, but for the determination of some of the activities (e.g., analgesics), several methods have been described where necessary. Most of the common methods are included and are of such a diversity that new methods will occur to the reader for use in his own studies. Acquaintance with the methods described to aid adaptation of new methods to the problem at hand. Wherever possible, methods have been chosen which could become quantitative if small changes were made in the procedure, such as the use of larger groups of animals. Guiding principles determining the presentation of the methods are described as follows: • A complete and carefully described procedure is given, which includes particularly modifications of the original method, so that unnecessary manipulations are eliminated while the accuracy is sustained. • The application of the method is described for both well-known drugs and new substances; an active, new substance is detected through the use of the method; a discussion is provided of other methods of screening for the activity and of the reasons for preferring the method given. • The reliability of the method and its limitations are stated. Features • The present work is obviously directed to those whose occupation is to search for new pharmaceuticals. • A variety of investigators in the fields of pharmacology, physiology, toxicology, and therapeutics may also find useful methods for their research. • Chemists in the pharmaceutical industry who read this book will be aided in their understanding of the basis for testing the compounds that they synthesize and in their understanding of the programs of testing that the pharmacologist has devised.

Contents:

Volume - I:

1.     Introduction 

2.     A Brief Review of the Biochemistry of the Nervous System 

3.     The Organization of Screening 

4.     General Methods 

5.     Quantal Responses, Calculation of the ED50 

6.     Depressants of the Central Nervous System 

7.     Ataractic (Tranquilizing, Newroleptic) Agents 

8.     Analgesics 

9.     Oxytocic Agents 

10. Antiserotonin Agents 

11. Parasympatholytic Agents 

12. Sympatholytic Agents 

13. Anti-Inflammatory Agents 

14. Anticonvulsants 

15. Sympathomimetic Agents 

16. Central Stimulants 

17. Muscaring Agents 

18. Ganglion-Blocking Agents 

19. Antifibrillatory Agents 

20. Cardiotonic Agents 

21. Histamine-Like Agents 

22. Antihistamine Agents 

23. Antitussive Agents 

24. Antacid Agents 

25. Thyromimetic Agents 

26. Hypoglycemic Agents 

27. Choleretic Agents 

28. Antiparkinson Agents 

29. Anti-Inflammatory and Glucocorticoidal Agents 

30. Antiemetic Agents 

31. Bronchodilatant Agents 

32. Curariform Agents 

33. Anabolic, Androgenic, and Antiandrogenic Agents 

34. Potentiators and Antagonists of Tryptamine 

35. Vasopressive Peptides 

36. Diuretic and Natriuretic Agents 

37. Anticholinesterase Agents 

38. Anticholestrerol Agents 

39. Uricosuric Agents 

40. Antishock Agents 

41. Hemostatic Agents 

42. Local and Spinal Anesthetics 

43. Abortifacient Agents 

44. Thymoleptic Agents 

45. Dermal Irritants 

46. Teratogenic Agents

Volume - II: 

1.     α-Adrenergic Blocking Agents 

2.     β-Adrenergic Blocking Agents

3.     Agents Acting on Coronary Blood Vessels 

4.     Agents with Kininlike Activity 

5.     Androgenic and Anabolic Agents 

6.     Estrogenic and Antiestrogenic Agents 

7.     Anovulatory Agents 

8.     Progestational Agents 

9.     Antihyperlipidemic Agents 

10. Immunosuppressive Agents 

11. Agents Affecting Mucociliary Activity 

12. Antiperspirant Agents 

13. Antidepression Agents 

14. Agents with Analgesic Activity and Dependence Liability 

15. Natriuretic and Antihypertensive Agents Screened by Sequential Methods