In Vitro Screening of Psychoactive Drugs

Abstract

Prior to the designation of illegal drugs (psychoactive drugs) by prefectural regulations, the Tokyo Metropolitan Government conducts surveys on the risk of drugs, reports the results to the governor through the Tokyo Metropolitan Government Advisory Committee on Illegal Drugs, an affiliated organization, and provides the central government with information. The Tokyo Metropolitan Institute of Public Health conducts identification of the constituents of drugs and biological effect tests to help the committee analyze and assess information on the risks of drugs. Narcotics and stimulants increase the concentrations of dopamine, serotonin, and norepinephrine, i.e., neurotransmitters, in the presynaptic clefts, exerting an excitatory effect. In the postsynaptic region, these neurotransmitters are considered to directly combine with the receptors and activate guanine nucleotide-binding proteins, causing activation. We have developed nine types (categorized into three groups) of simple, high-throughput measurement systems and examined their measurement methods. The systems are designed to assess the following properties of drugs: effects of: 1) inhibiting reuptake; 2) stimulating the release of neurotransmitters in the presynaptic region; and 3) activating G proteins in the postsynaptic region. The systems provide useful information in that they allow searches for the effects of a variety of psychoactive substances that are expected to become widespread, e.g., designer drugs, hallucinogenic plants and synthetic cannabinoids; they also allow you to conduct a test using micrograms of a drug, facilitating testing even when it is not available in a large quantity.