HISTAMINE RECEPTOR H3 ORDINARY ACTIVITY MUTANT AND UTILIZATION THEREOF

摘要

The internal domain (3) of a seven-transmembrane G protein-coupled receptor, which is meaningful in the coupling of the G protein or the activity of the receptor, is well conserved. In the H3 receptor which is one of G protein-coupled receptors, this domain is also well conserved. By transferring a point mutation into a sequence encoding this domain in the H3 receptor cDNA by the PCR method, a mutant H3 receptor having an extremely strong ordinary activity can be successfully constructed. It is further found out that use of the ordinary activity mutant of the H3 receptor makes it possible to easily and efficiently screen a candidate compound for a drug such as an inverse agonist to the H3 receptor.