METHOD FOR SELECTION OF ALLOSTERIC MODULATORS OF G-PROTEIN COUPLED RECEPTORS OF THE FAMILY III

摘要

Process for identification and selection of compounds (I) that act as allosteric regulators of a receptor (RCPG-III) coupled to G proteins of class III. Process for identification and selection of compounds (I) that act as allosteric regulators of a receptor (RCPG-III) coupled to G proteins of class III comprises: (i) producing a receptor (RCPG-IIIdelta ) that lacks essentially the extracellular domain of the native receptor; (ii) contacting this with a test compound; (iii) measuring the level (N1) of receptor activity; (iv) comparing N1 with the level, N0, measured in absence of test compound; and (v) selecting a test compound as (I) if N1 and N0 are significantly different. ACTIVITY : Nootropic; Neuroprotective; Neuroleptic; Tranquilizer; Antidepressant; Anticonvulsant; Antiaddictive; Osteopathic; Analgesic; Insecticide; Vermicide. MECHANISM OF ACTION : Regulation of receptors (RCPG-III) coupled to G proteins of class III.