Results 1 to 10 of about 705 (79)

Peripheralization Strategies Applied to Morphinans and Implications for Improved Treatment of Pain [PDF]

Molecules, 2023
Opioids are considered the most effective analgesics for the treatment of moderate to severe acute and chronic pain. However, the inadequate benefit/risk ratio of currently available opioids, together with the current ‘opioid crisis’, warrant ...
Helmut Schmidhammer, Mahmoud Al-Khrasani, Susanna Fürst   +2 more
exaly   +4 more sources

Recent Chemical and Pharmacological Developments on 14-Oxygenated-N-methylmorphinan-6-ones [PDF]

Molecules, 2021
Adequate pain management, particularly chronic pain, remains a major challenge associated with modern-day medicine. Current pharmacotherapy offers unsatisfactory long-term solutions due to serious side effects related to the chronic administration of ...
Mariana Spetea, Helmut Schmidhammer
doaj   +2 more sources

A MOR Antagonist with High Potency and Antagonist Efficacy among Diastereomeric C9-Alkyl-Substituted N-Phenethyl-5-(3-hydroxy)phenylmorphans

Molecules, 2023
The 5-(3-hydroxy)phenylmorphan structural class of compounds are unlike the classical morphinans, 4,5-epoxymorphinans, and 6,7-benzomorphans, in that they have an equatorially oriented aromatic ring rather than the axial orientation of that ring found in
Dana R. Chambers, Agnieszka Sulima, Dan Luo, Thomas E. Prisinzano, Arthur E. Jacobson, Kenner C. Rice   +5 more
doaj   +1 more source

Synthesis of Morphinan Alkaloids in Saccharomyces cerevisiae. [PDF]

PLoS ONE, 2015
Morphinan alkaloids are the most powerful narcotic analgesics currently used to treat moderate to severe and chronic pain. The feasibility of morphinan synthesis in recombinant Saccharomyces cerevisiae starting from the precursor (R,S)-norlaudanosoline ...
Elena Fossati, Lauren Narcross, Andrew Ekins, Jean-Pierre Falgueyret, Vincent J J Martin   +4 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

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, Silvia Rief, Helmut Schmidhammer, Lucia Negri, Mariana Spetea   +4 more
doaj   +1 more source

Isoquinoline Alkaloids from the Leaves of

Natural Product Communications, 2007
This study was aimed at investigating the alkaloids present in the leaves of Dehaasia hainanensis. Thirteen isoquinolines were isolated and characterized.
Chien-Kuang Chen, Su-Chang Chen, Chung-Hsiung Chen, Shoei-Sheng Lee   +3 more
doaj   +1 more source

Liquid Chromatography Coupled with Linear Ion Trap Hybrid OrbitrapMass Spectrometry for Determination of Alkaloids in Sinomeniumacutum

Molecules, 2018
The characterization of alkaloids is challenging because of the diversity of structures and the complicated fragmentation of collision induced structural dissociation in mass spectrometry.
Jinjun Shan, Xia Zhao, Cunsi Shen, Jianjian Ji, Jianya Xu, Shouchuan Wang, Tong Xie, Wenjun Tong   +7 more
doaj   +1 more source

Exploring Pharmacological Activities and Signaling of Morphinans Substituted in Position 6 as Potent Agonists Interacting with the μ Opioid Receptor

Molecular Pain, 2014
Background: Opioid analgesics are the most effective drugs for the treatment of moderate to severe pain. However, they also produce several adverse effects that can complicate pain management. The μ opioid (MOP) receptor, a G protein-coupled receptor, is
Tanila Ben Haddou, Davide Malfacini, Girolamo Calo, Mario D Aceto, Louis S Harris, John R Traynor, Andrew Coop, Helmut Schmidhammer, Mariana Spetea   +8 more
doaj   +1 more source

Low dose dextromethorphan attenuates moderate experimental autoimmune encephalomyelitis by inhibiting NOX2 and reducing peripheral immune cells infiltration in the spinal cord

Neurobiology of Disease, 2011
Dextromethorphan (DM) is a dextrorotary morphinan and a widely used component of cough medicine. Relatively high doses of DM in combination with quinidine are used for the treatment of mood disorders for patients with multiple sclerosis (MS). However, at
Olga V. Chechneva, Florian Mayrhofer, Daniel J. Daugherty, David E. Pleasure, Jau-Shyong Hong, Wenbin Deng   +5 more
doaj   +1 more source

Studies toward bivalent κ opioids derived from salvinorin A: heteromethylation of the furan ring reduces affinity

Beilstein Journal of Organic Chemistry, 2013
The recent crystal structure of the κ-opioid receptor (κ-OR) revealed, unexpectedly, that the antagonist JDTic is a bivalent ligand: in addition to the orthosteric pocket occupied by morphinans, JDTic also occupies a distinct (allotopic) pocket ...
Thomas A. Munro, Wei Xu, Douglas M. Ho, Lee-Yuan Liu-Chen, Bruce M. Cohen   +4 more
doaj   +1 more source