Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor [PDF]
The ongoing epidemics of opioid overdose raises an urgent need for effective antiaddiction therapies and addiction-free painkillers. The κ-opioid receptor (KOR) has emerged as a promising target for both indications, raising demand for new chemotypes of ...
Zheng, Zhong +8 more
core +2 more sources
The opium poppy genome and morphinan production [PDF]
Poppy genome reveals evolution of opiates The opium poppy has been a source of painkillers since Neolithic times. Attendant risks of addiction threaten many today. Guo et al. now deliver a draft of the opium poppy genome, which encompasses 2.72 gigabases assembled into 11 chromosomes and predicts more than
Li Guo +10 more
openaire +3 more sources
Characterization of Opioid Agonist Morphine Derivatives with Emphasis on Medicinal Chemistry
The aim of synthesizing new opioid compounds is to produce drugs that are more potent, less addictive, and have fewer side effects, such as respiratory depression and constipation. To achieve this, we evaluated the basicity, lipophilicity, and permeability of 30 opioid compounds, including 11 newly synthesized ones, to better understand the ...
Alaa Malik +7 more
wiley +1 more source
Phenol (bio)isosteres in drug design and development
This review explores the pivotal role of phenol bioisosteres in drug design, highlighting their potential to overcome the limitations of phenolic compounds, such as poor bioavailability and rapid metabolism. By examining diverse bioisosteric replacements, from benzimidazolones to quinolinones, it is demonstrated how these modifications enhance drug ...
Calvin Dunker +2 more
wiley +1 more source
Fragmentation pathways of drugs of abuse and their metabolites based on QTOF MS/MS and MSE accurate-mass spectra [PDF]
A study of the fragmentation pathways of several classes of drugs of abuse (cannabinoids, ketamine, amphetamine and amphetamine-type stimulants (ATS), cocaine and opiates) and their related substances has been made.
Bijlsma, Lubertus +3 more
core +2 more sources
ABSTRACT Papaver somniferum L., a medicinal plant renowned for its pharmaceutical alkaloids, has captivated scientific interest due to its rich secondary metabolite profile. This study explores a novel approach to manipulating alkaloid biosynthesis pathways by integrating virus‐induced gene silencing (VIGS) with macerozyme enzyme pretreatment ...
Deniz Ece Özcan +4 more
wiley +1 more source
Development of the Japanese Anticholinergic Risk Scale: English translation of the Japanese article
Background Anticholinergic burden, reflecting the cumulative impact of medications with anticholinergic properties, significantly predicts adverse drug reactions and geriatric syndromes in older adults. Although anticholinergic risk scales (ARS) have been developed and validated in various countries, none have been tailored specifically for Japan.
Fumihiro Mizokami +15 more
wiley +1 more source
A Cytotoxic, Co-operative Interaction Between Energy Deprivation and Glutamate Release From System x\u3csub\u3ec\u3c/sub\u3e\u3csup\u3e−\u3c/sup\u3e Mediates Aglycemic Neuronal Cell Death [PDF]
The astrocyte cystine/glutamate antiporter (system xc−) contributes substantially to the excitotoxic neuronal cell death facilitated by glucose deprivation. The purpose of this study was to determine the mechanism by which this occurred.
He, Yan +5 more
core +1 more source
Functional diversity of 2-oxoglutarate/Fe(II)-dependent dioxygenases in plant metabolism [PDF]
Oxidative enzymes catalyze many different reactions in plant metabolism. Among this suite of enzymes are the 2-oxoglutarate/Fe(II)-dependent dioxygenases (2-ODDs). Cytochromes P450 (CYPs) as often considered the most versatile oxidative enzymes in nature,
Peter J. Facchini, Scott C. Farrow
core +2 more sources
Inflammation helps the immune system identify and eliminate disease‐causing and foreign stimuli and initiate the healing process. Nonsteroidal anti‐inflammatory drugs have been often used in treating inflammation. Synthetic drugs have been associated with severe effects, necessitating the need for alternative medicinal agents.
Stephen Maina Gitahi +4 more
wiley +1 more source

