Opioids are the oldest and most potent drugs for the treatment of severe pain. Their clinical
application is undisputed in acute (eg, postoperative) and cancer pain, but their long-term …

Most evidence indicates that, as for family CG protein–coupled receptors (GPCRs), family A
GPCRs form homo-and heteromers. Homodimers seem to be a predominant species, with …

Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are
2 concepts in contemporary pharmacology that have major implications for the use of drugs …

G protein–coupled receptors (GPCRs) compose one of the largest families of membrane
proteins involved in intracellular signaling. They are involved in numerous physiological and …

Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target
the μ opioid receptor whose activation results in adverse effects like respiratory depression …

Opioids are among the most effective analgesics available and are the first choice in the
treatment of acute severe pain. However, partial efficacy, a tendency to produce tolerance …

Drugs acting at the opioid receptor family are clinically used to treat chronic and acute pain,
though they represent the second line of treatment behind GABA analogs, antidepressants …

κ-Opioid receptor (KOR) agonists do not activate the reward pathway stimulated by
morphine-like μ-opioid receptor (MOR) agonists and thus have been considered to be …

This paper is the thirty-fifth consecutive installment of the annual review of research
concerning the endogenous opioid system. It summarizes papers published during 2012 …

The diversity of receptor signaling is increased by receptor heteromerization leading to
dynamic regulation of receptor function. While a number of studies have demonstrated that …