Results 11 to 20 of about 41,494 (257)

SAR exploration of the non‐imidazole histamine H3 receptor ligand ZEL‐H16 reveals potent inverse agonism

open access: yesArchiv der Pharmazie, Volume 356, Issue 1, January 2023., 2023
ZEL‐H16 (1) has been disclosed to be a high‐affinity non‐imidazole H3R (partial) agonist. However, it was found that 1 acts as an inverse agonist for Gαi in various assays. Concise structure–activity relationship studies, molecular pharmacology, and docking were used to shed more light on the properties of 1.
Gábor Wágner   +12 more
wiley   +1 more source

Punica granatum peel supplementation attenuates cognitive deficits and brain injury in rat by targeting the Nrf2‐HO‐1 pathway

open access: yesFood Science &Nutrition, Volume 11, Issue 1, Page 168-180, January 2023., 2023
The hydro‐ethanolic extract of P. granatum peel was standardized. ;The extract increased superoxide dismutase activity and thiol content, while reduced function of AchE and peroxidation of lipid in the scopolamine‐injured rat’s brain. ;P. granatum may attenuate scopolamine injury through targeting nuclear factor‐E2‐related factor 2 pathway ; Abstract ...
Mahsan Akbarian   +5 more
wiley   +1 more source

Are β3‐adrenoceptor gene polymorphisms relevant for urology?

open access: yesNeurourology and Urodynamics, Volume 42, Issue 1, Page 33-39, January 2023., 2023
Abstract Aims β3‐adrenoceptors (ARs) are an important drug target for the treatment of overactive bladder syndrome (OAB) and are under investigation for other indications. The human β3‐AR gene is polymorphic; an exchange of amino acid tryptophan (Trp) for arginine (Arg) in position 64 of the receptor protein is the most frequent and best‐studied ...
Martin C. Michel
wiley   +1 more source

Muscarinic Receptor Agonists and Antagonists [PDF]

open access: yesMolecules, 2001
A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed.
David R. Kelly, Kenneth J. Broadley
openaire   +4 more sources

Enhanced muscarinic M1 receptor gene expression in the corpus striatum of streptozotocin-induced diabetic rats

open access: yesJournal of Biomedical Science, 2009
Acetylcholine (ACh), the first neurotransmitter to be identified, regulate the activities of central and peripheral functions through interactions with muscarinic receptors. Changes in muscarinic acetylcholine receptor (mAChR) have been implicated in the
Mathew Jobin   +3 more
doaj   +1 more source

Memetic Algorithms for Ligand Expulsion from Protein Cavities [PDF]

open access: yesJ. Chem. Phys. 143 (12), 124101, 2015, 2015
Ligand diffusion through proteins is a fundamental process governing biological signaling and enzymatic catalysis. The complex topology of protein tunnels results in difficulties with computing ligand escape pathways by standard molecular dynamics (MD) simulations. Here, two novel methods for searching of ligand exit pathways and cavity exploration are
arxiv   +1 more source

A review of frequently used Kampo prescriptions part 1. Daikenchuto

open access: yesTraditional &Kampo Medicine, Volume 9, Issue 3, Page 151-179, December 2022., 2022
Abstract Background The original formula name for daikenchuto (DKT) was written in ‘Jin Gui Yao Lue (Kinkiyōryaku in Japanese)’. DKT as used in Japan consists of four types of crude drug. Key findings Although there are few examples of its use in Chinese classical records, it has begun to be used extensively in modern Japan for intestinal obstruction ...
Takao Namiki   +5 more
wiley   +1 more source

A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity

open access: yesPharmaceutics, 2023
Anticholinergic burden tools have relevant pharmacological gaps that may explain their limited predictive ability for clinical outcomes. The aim of this study was to provide a universal pharmacological-based list of drugs with their documented affinity ...
Marta Lavrador   +5 more
doaj   +1 more source

All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium

open access: yesScientific Reports, 2017
Clinical and experimental studies indicate that muscarinic acetylcholine receptors are potential pharmacological targets for the treatment of neurological diseases.
Beatrice Mihaela Radu   +13 more
doaj   +1 more source

Muscarinic modulation of M and h currents in gerbil spherical bushy cells.

open access: yesPLoS ONE, 2020
Descending cholinergic fibers innervate the cochlear nucleus. Spherical bushy cells, principal neurons of the anterior part of the ventral cochlear nucleus, are depolarized by cholinergic agonists on two different time scales.
Charlène Gillet   +2 more
doaj   +1 more source

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