Diagnostic reagent for evalulation of pharmacological effect...

C - Chemistry – Metallurgy – 12 – Q

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Details

C12Q 1/34 (2006.01) C12Q 1/00 (2006.01) C12Q 1/37 (2006.01) G01N 33/15 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2474993

It is intended to provide test agents for evaluating the pharmacological effect of a drug such as a drug comprising an enzyme, an enzyme inhibitor or a receptor ligand or its prodrug; and a method of screening a drug having an excellent administration effect and/or little side effect from among drugs comprising enzymes, enzyme inhibitors or receptor ligands and/or prodrugs thereof. The above test agents and reagents to be used in the above method contain: (a) a compound serving as the substrate of an enzyme contained in a sample; (b) a compound serving as the substrate of another enzyme which couples with the effect of the enzyme (a) and shows a change in the activity; (c) a compound serving as the substrate of an enzyme which is directly inhibited by an enzyme inhibitor contained in a sample; (d) a compound serving as the substrate of another enzyme which couples with the effect of the enzyme inhibitor (c) and shows a change in the activity; (e) a compound serving as the substrate of an enzyme which shows a change in the activity when a receptor ligand in a sample binds to the receptor; or (f) a label for any of the substances (a) to (e).

Cette invention a pour but de produire des agents de tests permettant d'évaluer l'effet pharmacologique d'un médicament, par exemple un médicament comprenant une enzyme, un inhibiteur d'enzyme ou un ligand récepteur ou son promédicament; ainsi qu'à un procédé servant au criblage d'un médicament ayant un excellent effet d'administration et/ou peu d'effets secondaires parmi des médicaments comprenant des enzymes, des inhibiteurs d'enzymes ou des ligands de récepteurs et/ou des promédicaments de ceux-ci. Ces agents de tests et les réactifs à utiliser dans le procédé mentionné ci-dessus contiennent: (a) un composé faisant office de substrat d'une enzyme contenue dans un échantillon; (b) un composé faisant office de substrat d'une autre enzyme qui se couple à l'effet de l'enzyme (a) et présente un changement d'activité; (c) un composé faisant office de substrat d'une enzyme qui est directement inhibée par un inhibiteur d'enzyme contenu dans un échantillon; (d) un composé faisant office de substrat d'une autre enzyme qui se couple à l'effet de l'inhibiteur d'enzyme (c) et présente un changement d'activité; (e) un composé faisant office de substrat d'une enzyme qui présente un changement d'activité, lorsqu'un ligand de récepteur dans un échantillon se fixe au récepteur; ou (f) un marqueur pour l'une et/ou l'autre des substances (a) à (e).

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