Starting from the β-adrenoceptor agonist isoprenaline and beta-blocker carvedilol, we
designed and synthesized three different chemotypes of agonist/antagonist hybrids …

A plethora of membrane proteins are found along the cell surface and on the convoluted
labyrinth of membranes surrounding organelles. Since the advent of various structural …

Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount
importance to the field of cardiovascular medicine due to the critical physiological roles of …

In this study, we report the β1‐adrenoceptor binding kinetics of several clinically relevant
β1/2‐adrenoceptor (β1/2AR) agonists and antagonists.[3H]‐DHA was used to label CHO …

Brain functions rely on neurotransmitters that mediate communication between billions of
neurons. Disruption of this communication can result in a plethora of psychiatric and …

Bipolar disorder impacts millions of patients in the United States but the mechanistic
understanding of its pathophysiology and therapeutics is incomplete. Atypical antipsychotic …

G protein-coupled receptors (GPCRs) are an important family of membrane proteins
responsible for many physiological functions in human body. High resolution GPCR …

The molecular basis of receptor bias in G protein-coupled receptors (GPCRs) caused by
mutations that preferentially activate specific intracellular transducers over others remains …

G protein-coupled receptors (GPCRs) transduce a diverse variety of extracellular stimuli into
intracellular signaling. These receptors are the most clinically productive drug targets at …

The β 2-adrenergic receptor (β 2 AR) is a membrane-bound G-protein-coupled receptor and
an important drug target for asthma. Clinical studies report that the population variant …