Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X-…

The ability of mu-opioid agonists to activate G proteins has been demonstrated by studying
the binding of the GTP analogue guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTP …

μ-Opioid receptors are among the most studied G protein-coupled receptors because of the
therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However…

Male rats are more sensitive to the antinociceptive effects of morphine than female rats. This
difference is seen across several rat strains using a variety of nociceptive stimuli. However, …

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 idea …

The present study examined the effect of opioid receptor agonists in the rat forced swim
assay. The δ-opioid receptor agonists SNC80 ((+)-4-[(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-…

Opioid receptors are 7‐transmembrane domain receptors that couple to heterotrimeric G
proteins. The endogenous ligands for opioid receptors are peptides which bind to the …

Recent developments in the study of the structure and function of opioid receptors raise
significant challenges for the definition of individual receptor types and the development of a …

Allosteric modulators of G protein-coupled receptors (GPCRs) have a number of potential
advantages compared to agonists or antagonists that bind to the orthosteric site of the receptor…

This study examines the possibility that oripavine opioid receptor agonists bind equally to
both high and low affinity states of the μ-opioid receptor. Studies were performed in C6 cells …