Efficacy of inverse agonists in cells overexpressing a constitutively active β_2-adrenoceptor and type II adenylyl cyclase

摘要

Maximal stimulant output from the adenylyl cyclase cascade in neuroblastoma X glioma hybrid, NG 108-15, cells is limited by the levels of expression of isoforms of adenylyl cyclase. Stable expression in These cells of a constitutively active mutant (CAM) version of the humanβ_2-adrenoceptor resulted in Higher basal adenylyl cyclase activity activity than following expression of the human wild typeβ_2-adrenoceptor. Isoprenaline acted as a full agonist in membranes from both wild type and CAMβ_2-adrenoceptor Expressing clones.