Can Chronic Inverse Agonist Treatment Enhance GPCR Signaling?
Examples Using Heart Failure and Asthma Richard A. Bond, Ph.D., Associate Professor, College of Pharmacy, University of Houston A paradigm shift that has occurred with regard to the use of beta-adrenoceptor agonists and inverse agonists in the treatment of congestive heart failure. Chronic treatment with certain drugs from the previously contraindicated class known as ‘beta-blockers’ have now been shown to decrease mortality and increase cardiac contractility in heart failure patients. We are attempting to determine whether the unexpected reversal in heart failure upon chronic administration of beta blockers is a one-off event, or indicative of a more general pattern of GPCR regulation by inverse agonists that is applicable to other diseases such as asthma.
