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]
Frontiers in Pharmacology, 2018 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.
Roberta Lattanzi +4 more
doaj +4 more sources
Synthesis, Biological Evaluation, and SAR Studies of 14β-phenylacetyl Substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones Derivatives: Ligands With Mixed NOP and Opioid Receptor Profile [PDF]
Frontiers in Psychiatry, 2018 A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and delta (DOP) opioid receptors and nociceptin/orphanin FQ peptide (NOP ...
Vinod Kumar +6 more
doaj +6 more sources
Pharmacological profiles of opioid ligands at Kappa opioid receptors [PDF]
BMC Pharmacology, 2006 Abstract Background The aim of the present study was to describe the activity of a set of opioid drugs, including partial agonists, in a human embryonic kidney cell system stably expressing only the mouse κ-opioid receptors.
Gharagozlou, Parham +4 more
openaire +2 more sources
The unsolved case of “bone-impairing analgesics”. The endocrine effects of opioids on bone metabolism [PDF]
, 2015 The current literature describes the possible risks for bone fracture in chronic analgesics users. There are three main hypotheses that could explain the increased risk of fracture associated with central analgesics, such as opioids: 1) the increased ...
COLUZZI, FLAMINIA +3 more
core +6 more sources
BJA Open, 2023 Opioids are a mainstay in acute pain management and produce their effects and side effects (e.g., tolerance, opioid-use disorder and immune suppression) by interaction with opioid receptors.
David G. Lambert
doaj +1 more source
An opioid-like system regulating feeding behavior in C. elegans [PDF]
, 2015 Neuropeptides are essential for the regulation of appetite. Here we show that neuropeptides could regulate feeding in mutants that lack neurotransmission from the motor neurons that stimulate feeding muscles. We identified nlp-24 by an RNAi screen of 115
Artyukhin, Alexander B. +3 more
core +3 more sources
Opioid Receptors in Immune and Glial Cells-Implications for Pain Control [PDF]
, 2020 Opioid receptors comprise μ (MOP), δ (DOP), κ (KOP), and nociceptin/orphanin FQ (NOP) receptors. Opioids are agonists of MOP, DOP, and KOP receptors, whereas nociceptin/orphanin FQ (N/OFQ) is an agonist of NOP receptors.
Celik, Melih Ö., Machelska, Halina
core +1 more source
Semisynthetic neoclerodanes as kappa opioid receptor probes [PDF]
Bioorganic & Medicinal Chemistry, 2012 Modification of the furan ring of salvinorin A (1), the main active component of Salvia divinorum, has resulted in novel neoclerodane diterpenes with opioid receptor affinity and activity. Conversion of the furan ring to an aldehyde at the C-12 position (5) has allowed for the synthesis of analogues with new carbon-carbon bonds at that position ...
Lovell, Kimberly M. +10 more
openaire +3 more sources
Stress-induced reinstatement of nicotine preference requires dynorphin/kappa opioid activity in the basolateral amygdala [PDF]
, 2016 UNLABELLED: The dynorphin (DYN)/kappa-opioid receptor (KOR) system plays a conserved role in stress-induced reinstatement of drug seeking for prototypical substances of abuse.
Bruchas, Michael R +4 more
core +2 more sources
Historical Review: Opiate Addiction and Opioid Receptors
Cell 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