BmK-YA, an enkephalin-like peptide in scorpion venom. [PDF]
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
In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
core +2 more sources
Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates [PDF]
Fentanyl is a powerful opiate analgesic typically used for the treatment of severe and chronic pain, but its prescription is strongly limited by the well-documented side-effects.
Benyhe, Sa ́ndor +18 more
core +1 more source
Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.
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
Phylogenomic analysis reveals extensive phylogenetic mosaicism in the Human GPCR Superfamily [PDF]
A novel high throughput phylogenomic analysis (HTP) was applied to the rhodopsin G-protein coupled receptor (GPCR) family. Instances of phylogenetic mosaicism between receptors were found to be frequent, often as instances of correlated mosaicism and ...
Allaby, Robin G., Woodwark, Mathew
core +1 more source
The effects of pioglitazone, a PPARγ receptor agonist, on the abuse liability of oxycodone among nondependent opioid users [PDF]
Aims: Activation of PPARγ by pioglitazone (PIO) has shown some efficacy in attenuating addictive-like responses in laboratory animals. The ability of PIO to alter the effects of opioids in humans has not been characterized in a controlled laboratory ...
Alonzo +74 more
core +1 more source
Background: Chronic ethanol exposure reduces dopamine transmission in the nucleus accumbens, which may contribute to the negative affective symptoms associated with ethanol withdrawal.
J. Rose +7 more
semanticscholar +1 more source
Molecular and cellular mechanisms of the age-dependency of opioid analgesia and tolerance
The age-dependency of opioid analgesia and tolerance has been noticed in both clinical observation and laboratory studies. Evidence shows that many molecular and cellular events that play essential roles in opioid analgesia and tolerance are actually age-
Zhao Jing +4 more
doaj +1 more source
Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists
Yusuke Karasawa +12 more
doaj +1 more source
Delta-opioid receptor endocytosis in spinal cord after dermenkephalin activation
Background The delta(δ)-opioid receptors belong to the G protein-coupled receptors and in vitro studies have shown that δ-opioid receptors undergo an internalization process in response to agonist stimulation.
Gastard Myriam
doaj +1 more source

