Diagnostic reagent for evaluation of pharmacological effect of medicine, and method and reagent for screening pharmaceutical agents comprising enzyme, enzyme inhibitor or receptor ligand and/or prodrugs thereof for one having high medicative efficacy and/or small side effect

摘要

A diagnostic reagent for use in the evaluation of a pharmacological effect of a medicine containing a pharmaceutical agent including an enzyme, an enzyme inhibitor or a receptor ligand or a prodrug of the pharmaceutical agent; and a method of screening pharmaceutical agents each comprising an enzyme, an enzyme inhibitor or a receptor ligand and/or prodrugs of the pharmaceutical agents for one or ones having high medicative efficacy and/or a small side effect are provided. The diagnostic reagent and the reagent used in the method comprise: (a) a compound which serves as a substrate for the enzyme contained in the medicine or the pharmaceutical agent to be evaluated or for an enzyme generated from the prodrug contained in the medicine or the pharmaceutical agent to be evaluated, or a pharmaceutically acceptable salt thereof; (b) a compound which serves as a substrate for a different enzyme capable of exhibiting an alteration in activity by coupling to the effect of the enzyme in (a), or a pharmaceutically acceptable salt thereof; (c) a compound which serves as a substrate for an enzyme which is directly inhibited by the enzyme inhibitor contained in the medicine or the pharmaceutical agent to be evaluated or by an enzyme inhibitor generated from the prodrug contained in the medicine or the pharmaceutical agent to be evaluated, or a pharmaceutically acceptable salt thereof; (d) a compound which serves as a substrate for an enzyme capable of exhibiting an alteration in activity by coupling to the effect of the enzyme inhibitor in (c), or a pharmaceutically acceptable salt thereof; (e) a compound which serves as a substrate for an enzyme capable of exhibiting an alteration in activity by the binding between a receptor and the receptor ligand contained in the medicine or the pharmaceutical agent to be evaluated or a receptor ligand generated from the prodrug contained in the medicine or the pharmaceutical agent to be evaluated, or a pharmaceutically acceptable salt thereof; or (f) a labeled form of any one of the substances (a) to (e). IMAGE