G protein-biased agonists of the μ-opioid receptor (MOPr) have been proposed as an
improved class of opioid analgesics. Recent studies have been unable to reproduce the …

In classical G-protein-coupled receptor (GPCR) activation, GPCRs couple to a variety of
heterotrimeric G proteins on the membrane and then activate downstream signaling …

Biased agonism at G protein–coupled receptors describes the phenomenon whereby some
drugs can activate some downstream signaling activities to the relative exclusion of others …

Abstract The β1-adrenoceptor (β1AR) is a G-protein-coupled receptor (GPCR) that couples
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …

Drug addiction is a worldwide societal problem and public health burden, and results from
recreational drug use that develops into a complex brain disorder. The opioid system, one of …

The leaves of Mitragyna speciosa (commonly known as kratom), a tree endogenous to parts
of Southeast Asia, have been used traditionally for their stimulant, mood-elevating, and …

Abstract Background Kratom, a Southeast Asian plant with opioid-receptor mediated effects,
has emerged as a potential substance of abuse, with limited data on its use and effects. This …

G protein-coupled receptors (GPCRs) are the largest class of drug targets, largely owing to
their druggability, diversity and physiological efficacy. Many drugs selectively target specific …

Opioids are the most effective drugs for the treatment of severe pain, but they also cause
addiction and overdose deaths, which have led to a worldwide opioid crisis. Therefore, the …

Opioids are the most commonly used and effective analgesic treatments for severe pain, but
they have recently come under scrutiny owing to epidemic levels of abuse and overdose …