Results 21 to 30 of about 72,155 (213)

Mechanistic Characterization of the Pharmacological Profile of HS-731, a Peripherally Acting Opioid Analgesic, at the µ-, δ-, κ-Opioid and Nociceptin Receptors

open access: yesMolecules, 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

Clinical opioids differentially induce co-internalization of μ- and δ-opioid receptors

open access: yesMolecular Pain, 2018
Opioid receptors play an important role in mediating the spinal analgesia. The μ-opioid receptor is the major target of opioid drugs widely used in clinics.
Fenghua Bao   +5 more
doaj   +1 more source

A Narrative Pharmacological Review of Buprenorphine: A Unique Opioid for the Treatment of Chronic Pain

open access: yesPain and Therapy, 2020
Buprenorphine is a Schedule III opioid analgesic with unique pharmacodynamic and pharmacokinetic properties that may be preferable to those of Schedule II full μ-opioid receptor agonists.
Jeffrey Gudin, Jeffrey Fudin
doaj   +1 more source

Opioid Receptors and Protonation-Coupled Binding of Opioid Drugs [PDF]

open access: yes, 2021
Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest to treat pain. Pain may associate with inflamed tissue characterized by acidic pH.
Samo Lešnik   +7 more
core   +1 more source

Chronic morphine treatment attenuates cell growth of human BT474 breast cancer cells by rearrangement of the ErbB signalling network. [PDF]

open access: yes, 2013
There is increasing evidence that opioid analgesics may interfere with tumour growth. It is currently thought that these effects are mediated by transactivation of receptor tyrosine kinase (RTK)-controlled ERK1/2 and Akt signalling.
Weingaertner, Inka Regine   +5 more
core   +1 more source

Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors

open access: yesBMC Neuroscience, 2002
Background The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors.
Clark J   +3 more
doaj   +1 more source

The Use of Computational Approaches in the Discovery and Mechanism Study of Opioid Analgesics

open access: yesFrontiers in Chemistry, 2020
Opioid receptors that belong to class A G protein-coupled receptors (GPCRs) are vital in pain control. In the past few years, published high-resolution crystal structures of opioid receptor laid a solid basis for both experimental and computational ...
Bangyi Zhao, Wei Li, Lijie Sun, Wei Fu
doaj   +1 more source

Historical Review: Opiate Addiction and Opioid Receptors

open access: yesCell Transplantation, 2019
Substance use disorders (SUDs), defined as a collection of symptoms including tolerance and withdrawal, are chronic illnesses characterized by relapse and remission. In the United States, billions of dollars have been lost due to SUDs.
Shaocheng Wang
doaj   +1 more source

BmK-YA, an enkephalin-like peptide in scorpion venom. [PDF]

open access: yesPLoS ONE, 2012
By screening extracts of venom from the Asian scorpion Buthus martensii Karsch (BmK) for their abilities to activate opioid receptors, we have identified BmK-YA, an amidated peptide containing an enkephalin-like sequence. BmK-YA is encoded by a precursor
Yan Zhang   +5 more
doaj   +1 more source

Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.

open access: yesPLoS 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

Home - About - Disclaimer - Privacy