New strategic insights into managing fungal biofilms [PDF]
Fungal infections have dramatically increased in the last decades in parallel with an increase of populations with impaired immunity, resulting from medical conditions such as cancer, transplantation or other chronic diseases.
Borghi, Elisa +6 more
core +4 more sources
Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of <sup>18</sup>F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Herrera-Rueda MA +4 more
europepmc +2 more sources
The varieties of the psychedelic experience: A preliminary study of the association between the reported subjective effects and the binding affinity profiles of substituted phenethylamines and tryptamines [PDF]
Classic psychedelics are substances of paramount cultural and neuroscientific importance. A distinctive feature of psychedelic drugs is the wide range of potential subjective effects they can elicit, known to be deeply influenced by the internal state of
Erowid, Earth +6 more
core +2 more sources
Anti-inflammation of spirocyclopiperazinium salt compound LXM-10 targeting α7 nAChR and M4 mAChR and inhibiting JAK2/STAT3 pathway in rats. [PDF]
The present study aims to investigate the therapeutic effects of LXM-10 by intragastric administration in both acute and chronic inflammatory models, and to explore the underlying molecular mechanisms.
Weiwei Zhang +5 more
doaj +1 more source
M4 muscarinic acetylcholine receptor is a G protein-coupled receptor (GPCR) that has been associated with alcohol and cocaine abuse, Alzheimer's disease, and schizophrenia which makes it an interesting drug target.
Maris-Johanna Tahk +10 more
doaj +1 more source
Virtual Affinity Fingerprints for Target Fishing: A New Application of Drug Profile Matching [PDF]
We recently introduced Drug Profile Matching (DPM), a novel virtual affinity fingerprinting bioactivity prediction method. DPM is based on the docking profiles of ca.
Czobor, P. +6 more
core +1 more source
Rat Schwann cells express M1–M4 muscarinic receptor subtypes
AbstractThe expression of different muscarinic receptor subtypes was analyzed in immature Schwann cells obtained from sciatic nerve of 2‐day neonatal rats. By using RT‐PCR analysis, we demonstrated the presence of M1, M2, M3, and M4 receptor subtypes in cultured Schwann cells, with M2 displaying the highest expression levels.
LORETI, Simona +5 more
openaire +3 more sources
Crystal structures of the M1 and M4 muscarinic acetylcholine receptors [PDF]
Muscarinic M1-M5 acetylcholine receptors are G-protein-coupled receptors that regulate many vital functions of the central and peripheral nervous systems. In particular, the M1 and M4 receptor subtypes have emerged as attractive drug targets for treatments of neurological disorders, such as Alzheimer's disease and schizophrenia, but the high ...
David M, Thal +13 more
openaire +2 more sources
Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie +3 more
core +2 more sources
Correction to: From theory to therapy: unlocking the potential of muscarinic receptor activation in schizophrenia with the dual M1/M4 muscarinic receptor agonist xanomeline and trospium chloride and insights from clinical trials. [PDF]
europepmc +3 more sources

