The original strain of proopiomelanocortin (POMC)-deficient mice (Pomc−/−) was generated
by homologous recombination in 129X1/SvJ (A w/A w)-derived embryonic stem cells using a …

Clinical pain conditions may remain responsive to opiate analgesics for extended periods,
but such persistent acute pain can undergo a transition to an opiate-resistant chronic pain …

Opioid receptors display basal signaling (constitutive, agonist-independent activity), which
seems to be regulated by agonist exposure. Whereas agonist pretreatment desensitizes …

Opioids are powerful analgesics, but also carry significant side effects and abuse potential.
Here we describe a modulator of the μ-opioid receptor (MOR1), the transient receptor …

G protein-coupled receptors (GPCRs) are polytopic membrane proteins that have a pivotal
role in cellular signaling. Like other membrane proteins, they fold in the endoplasmic …

Rationale The novel opioid receptor antagonist, GSK1421498, has been shown to attenuate
reward-driven compulsive behaviours, such as stimulant drug seeking or binge eating, in …

Hedonic reward, dependence and addiction are unwanted effects of opioid analgesics,
linked to the phasic cycle of μ opioid receptor activation, tolerance and withdrawal. In vitro …

We had previously demonstrated that opioid receptors contribute to the induction and
expression of behavioral sensitization induced by repeated daily injection with 2.5 mg/kg of …

Current ligand− receptor binding assays for G-protein coupled receptors cannot directly
measure the system's dissociation constant, K d, without purification of the receptor protein …

1 The purpose of the present study is to compare the capacity of opioid antagonists to elicit
withdrawal jumping in mice following two acute pretreatment doses of the opioid agonist …