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Past civilizations, especially the cultures of ancient Greece and China, compiled the earliest written pharmacological knowledge, identifying certain diseases and the recommended "prescriptions" for these ailments. It was not until thousands of years later that organized experiments in pharmacology began. Many credit Francois Magendie, an early 19th-century French physiologist, with the birth of experimental pharmacology. The research of Magendie and his student, Claude Bernard, on poisons such as strychnine and carbon monoxide, and on the use of curare as a muscle relaxant, helped to establish many of the principles of modern pharmacology. In 1847, a German, Rudolf Bucheim, started the first institute of pharmacology at the University of Dorpat, establishing the study of pharmacology as a singular discipline. A student of Bucheim, Oswald Schmiedeberg, became a professor of pharmacology and further passed on his knowledge to students from all over the world. One of these students, John Jacob Abel, is credited with bringing experimental pharmacology to the United States.

The medical achievements and discoveries of pharmacologists are numerous. Their work has helped in the development of antibiotics, anesthetics, vaccines, tranquilizers, vitamins, and many other substances in wide medical use today. Pharmacologists have been instrumental, for example, in the use of ether and other anesthetics that have modernized surgical procedures. Their research was used in the development of lifesaving drugs such as penicillin, tetanus, and polio vaccines, antimalaria drugs, and countless other compounds. In addition, pharmacologists have helped to develop drugs to treat heart disease, cancer, and psychiatric illnesses.

With the scientific advances of the early 20th century, especially the introduction of antibacterial drugs into medicine, pharmacology gained recognition as a distinct discipline. Spurred by pharmacological research, the Food, Drug, and Cosmetic Act of 1938 was introduced, requiring rigorous studies of drugs before they could be marketed. Regulations continue today through the Food and Drug Administration.

Unlike early pharmacologists who were strictly devoted to developing new drugs, modern pharmacologists perform a much broader range of activities. They test pesticides for harmful reactions, identify poisons and their effects, analyze industrial pollutants, study food preservatives and colorings, and check other substances for their effects on the environment as well as on humans. Their research includes all aspects of modern molecular and cellular biology as well as effects of drugs in animals and humans.

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