It is estimated that nearly a third of people who abuse drugs started with prescription opioid
medicines. Approximately, 11.5 million Americans used prescription drugs recreationally in …

G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

Positive allosteric modulators (PAMs) of the mu-opioid receptor (MOR) have been
hypothesized as potentially safer analgesics than traditional opioid drugs. This is based on …

The US faces an unprecedented surge in fatal drug overdoses. Naloxone, the only antidote
for opiate overdose, competes at the mu opioid receptor (μOR) orthosteric site. Naloxone …

Endogenous ions play important roles in the function and pharmacology of G-protein
coupled receptors (GPCRs). Historically the evidence for ionic modulation of GPCR function …

Allosteric modulators of G-protein-coupled receptors (GPCRs) enhance signaling by binding
to GPCRs concurrently with their orthosteric ligands, offering a novel approach to overcome …

There is significant need to find effective, nonaddictive pain medications. κ Opioid receptor
(KOPr) agonists have been studied for decades but have recently received increased …

Introduction: Pain relief remains a major public health challenge. The most efficient available
painkillers are opioids targeting the mu opioid receptor (MOR). MORs are expressed in the …

The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs)
reflects their ability to stabilize active receptor states (R*) and is a major determinant of their …

Since the isolation of morphine from the opium poppy over 200 years ago, the molecular
basis of opioid action has remained the subject of intense inquiry. The identification of …