FUNCTIONAL ASSAY FOR AGONIST ACTIVATION OF RECEPTORS

The invention provides a novel high throughput functional assay for certain agonist-activated receptors, including Alpha 1A , Alpha 2A, H1, 5HT1A, SHT2A, D2 and D3 receptors. The assay method of the invention uses an elevated temperature and a cell line that stably expresses both the receptor and th...

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Hauptverfasser: WONG, STEPHEN, KWOK-FUNG, SHRIKHANDE, ALKA, VINAY
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creator WONG, STEPHEN, KWOK-FUNG
SHRIKHANDE, ALKA, VINAY
description The invention provides a novel high throughput functional assay for certain agonist-activated receptors, including Alpha 1A , Alpha 2A, H1, 5HT1A, SHT2A, D2 and D3 receptors. The assay method of the invention uses an elevated temperature and a cell line that stably expresses both the receptor and the promiscuous G protein G(1S wherein agonist-induced intracellular Ca
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The assay method of the invention uses an elevated temperature and a cell line that stably expresses both the receptor and the promiscuous G protein G(1S wherein agonist-induced intracellular Ca&lt;2+¿ release was monitored by a Fluorometric Imaging Plate Reader (FLIPR). The magnitude of the agonist-induced response was dramatically enhanced by performing the assay at an elevated temperature, rather than at room temperature. The novel assay of the invention is useful for selecting compounds which are effective in the treatment of disorders related to the activation of certain neuroreceptors. La présente invention concerne une nouvelle analyse fonctionnelle à haut rendement de certains récepteurs activés par des agonistes, y compris les récepteurs Alpha 1A, Alpha 2A, H1, 5HT1A, SHT2A, D2 et D3. Dans le procédé de l'invention, il est fait appel à une température élevée et à une lignée cellulaire qui exprime de façon stable à la fois le récepteur et la protéine G ubiquiste G&lt;15, la libération intracellulaire de Ca&lt;2+&gt; induite par l'agoniste étant contrôlée par lecteur de plaque d'imageuse à fluorescence (FLIPR). Le fait que l'analyse ait été effectuée à une température élevée, plutôt qu'à la température ambiante, a permis d'augmenter dans des proportions énormes l'amplitude de la réponse induite par l'agoniste. 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subjects BEER
BIOCHEMISTRY
CHEMISTRY
COMPOSITIONS OR TEST PAPERS THEREFOR
COMPOSITIONS THEREOF
CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES
CULTURE MEDIA
ENZYMOLOGY
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES
MEASURING
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS
METALLURGY
MICROBIOLOGY
MICROORGANISMS OR ENZYMES
MUTATION OR GENETIC ENGINEERING
PHYSICS
PROCESSES OF PREPARING SUCH COMPOSITIONS
PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS
SPIRITS
TESTING
VINEGAR
WINE
title FUNCTIONAL ASSAY FOR AGONIST ACTIVATION OF RECEPTORS
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