Results 81 to 90 of about 18,176 (269)
Effect of nalfurafine hydrochloride on the basal pressure of the sphincter of Oddi in anesthetized rabbits [PDF]
, 2017 Background: Opioid analgesics, which are classified as μ-opioid receptor agonists, are known to induce spasms or contraction of the sphincter of Oddi (SO), thereby inducing or exacerbating biliary diseases such as biliary obstruction, gallbladder ...
Kobayashi, Ryosuke +4 more
core +1 more source
4β-Methyl-5-(3-hydroxyphenyl)morphan Opioid Agonist and Partial Agonist Derived from a 4β-Methyl-5-(3-hydroxyphenyl)morphan Pure Antagonist [PDF]
, 2013 In previous studies we reported that addition of 7α-acylamino groups to N-phenylpropyl-4β-methyl-5-(3-hydroxyphenyl)morphan (4) led to compounds that were pure opioid receptor antagonists.
Carroll, F. Ivy +7 more
core +2 more sources
Direct selection of DNA-encoded libraries for biased agonists of GPCRs on live cells [PDF]
, 2023 G protein-coupled receptors (GPCRs) are the largest superfamily of human membrane target proteins for approved drugs. GPCR ligands can have a complex array of pharmacological activities.
Bai, Yuntian +4 more
core +2 more sources
Molecules, 2022 Accumulated preclinical and clinical data show that peripheral restricted opioids provide pain relief with reduced side effects. The peripherally acting opioid analgesic HS-731 is a potent dual μ-/δ-opioid receptor (MOR/DOR) full agonist, and a weak ...
Kristina Puls +3 more
doaj +1 more source
Psychedelic‐assisted treatment for substance use disorder: A narrative systematic review
Addiction, EarlyView.Abstract Background and aims This is the first systematic review of the extant literature on all major psychedelic‐assisted treatment for alcohol use disorder (AUD), tobacco use disorder (TUD) and other substance use disorders (SUD). We aimed to summarise the evidence for efficacy of psychedelic‐assisted treatment for AUD, TUD, and SUD; to evaluate its
Theodore Piper +7 more
wiley +1 more source
British Journal of Pharmacology, EarlyView.Graph‐based algorithms that enable efficient computations of all H‐bonds present in structures in entire datasets allow us to dissect H‐bond fingerprints that characterize distinct GPCRs and the structures sampled along their activation. Abstract Changes in structure and dynamics elicited by agonist ligand binding at the extracellular side of G protein
Éva Bertalan +3 more
wiley +1 more source
Journal of Pharmacological Sciences, 2003 : κ-Opioid receptor agonists decrease the levels of extracellular dopamine in vivo and in vitro. However, the mechanism(s) underlying these actions are unclear.
Nuannoi Chudapongse +3 more
doaj
Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.
PLoS ONE, 2014 Inflammation enhances the peripheral analgesic efficacy of opioid drugs, but the mechanisms involved in this phenomenon have not been fully elucidated. Crotalphine (CRP), a peptide that was first isolated from South American rattlesnake C.d.
Vanessa Olzon Zambelli +6 more
doaj +1 more source
ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
British Journal of Pharmacology, EarlyView.G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison +15 more
wiley +1 more source
IUPHAR Review - Bivalent and bifunctional opioid receptor ligands as novel analgesics
Pharmacological Research, 2023 Though efficacious in managing chronic, severe pain, opioid analgesics are accompanied by significant adverse effects including constipation, tolerance, dependence, and respiratory depression.
Kyle J. Rehrauer +1 more
doaj