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This presentation surveys modern concepts for drug screening as they have emerged from current neurochemical research. Among others, the concept of multiple forms of MAO and phosphodiesterase has revolutionized the approach to drug screening of compounds that change neuronal function through inhibition of these enzymes. Neurochemical progress has opened new vistas and has given indications on how to screen MAO inhibitors for maximum efficacy while avoiding potential side effects. The finding that drugs acting on postsynaptic receptors can now be screened in preparations with receptors made supersensitive by denervation provides another new model, made possible by the discovery that 6-OH-dopamine and 6-hydroxyserotonin can lesion neurons selectively. The use of turnover rate measurements in association with other tests can contribute valuable information on the anatomical site of action of drugs. These tests have a great predictive value if conducted with quantitative criticism of dose-response relations.

Principles of neurochemistry and drug screening procedures in neuropsychopharmacology