Endogenous opioid system dysregulation in depression: implications for new therapeutic approaches
Abstract The United States is in the midst of an opioid addiction and overdose crisis
precipitated and exacerbated by use of prescription opioid medicines. The majority of opioid …
precipitated and exacerbated by use of prescription opioid medicines. The majority of opioid …
Biased ligands of G protein-coupled receptors (GPCRs): Structure–functional selectivity relationships (SFSRs) and therapeutic potential
L Tan, W Yan, JD McCorvy, J Cheng - Journal of medicinal …, 2018 - ACS Publications
G protein-coupled receptors (GPCRs) signal through both G-protein-dependent and G-
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …
In vivo brain GPCR signaling elucidated by phosphoproteomics
INTRODUCTION The G protein–coupled receptor (GPCR) superfamily is a major drug target
for neurological diseases. Functionally selective agonists activate GPCRs, such as the …
for neurological diseases. Functionally selective agonists activate GPCRs, such as the …
Dynorphin/kappa opioid receptor signaling in preclinical models of alcohol, drug, and food addiction
The dynorphin/kappa opioid receptor (KOR) system is implicated in the “dark side” of
addiction, in which stress exacerbates maladaptive responses to drug and alcohol …
addiction, in which stress exacerbates maladaptive responses to drug and alcohol …
Nalfurafine is a G-protein biased agonist having significantly greater bias at the human than rodent form of the kappa opioid receptor
Nalfurafine is a moderately selective kappa opioid receptor (KOR) analgesic with low
incidence of dysphoric side effects in clinical development for the treatment of uremic …
incidence of dysphoric side effects in clinical development for the treatment of uremic …
Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets
S Mallipeddi, DR Janero, N Zvonok… - Biochemical …, 2017 - Elsevier
The phenomenon of functional selectivity, whereby a ligand preferentially directs the
information output of a G-protein coupled receptor (GPCR) along (a) particular effector …
information output of a G-protein coupled receptor (GPCR) along (a) particular effector …
Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after icv administration in mice
M Spetea, SO Eans, ML Ganno… - British Journal of …, 2017 - Wiley Online Library
Background and purpose The κ receptor has a central role in modulating neurotransmission
in central and peripheral neuronal circuits that subserve pain and other behavioural …
in central and peripheral neuronal circuits that subserve pain and other behavioural …
Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors
J De Neve, TMA Barlow, D Tourwé, F Bihel… - RSC Medicinal …, 2021 - pubs.rsc.org
One of the main challenges in contemporary medicinal chemistry is the development of safer
analgesics, used in the treatment of pain. Currently, moderate to severe pain is still treated …
analgesics, used in the treatment of pain. Currently, moderate to severe pain is still treated …
Opioid modulation of prefrontal cortex cells and circuits
Several neurochemical systems converge in the prefrontal cortex (PFC) to regulate cognitive
and motivated behaviors. A rich network of endogenous opioid peptides and receptors …
and motivated behaviors. A rich network of endogenous opioid peptides and receptors …
Docosahexaenoic acid modulates brain-derived neurotrophic factor via GPR40 in the brain and alleviates diabesity-associated learning and memory deficits in mice
GPR40 (Free fatty acid receptor 1) has emerged as an important therapeutic target for
diabetes. Several studies have demonstrated the association of comorbid psychiatric …
diabetes. Several studies have demonstrated the association of comorbid psychiatric …