Results 11 to 20 of about 2,979 (198)

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

Archiv 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, Tamara A. M. Mocking, Xiaoyuan Ma, Inna Slynko, Daniel Da Costa Pereira, Robin Breeuwer, Niek J. N. Rood, Cas van der Horst, Henry F. Vischer, Chris de Graaf, Iwan J. P. de Esch, Maikel Wijtmans, Rob Leurs   +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

Food 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, Mahmoud Hosseini, Farshad Mirzavi, Sabiheh Amirahmadi, Fahimeh Lavi Arab, Arezoo Rajabian   +5 more
wiley   +1 more source

Are β3‐adrenoceptor gene polymorphisms relevant for urology?

Neurourology 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

A review of frequently used Kampo prescriptions part 1. Daikenchuto

Traditional &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, Takayuki Hoshino, Nobuaki Egashira, Toshiaki Kogure, Mari Endo, Masato Homma   +5 more
wiley   +1 more source

Understanding and treating ejaculatory dysfunction in men with diabetes mellitus

Andrology, Volume 11, Issue 2, Page 379-398, February 2023., 2023
Abstract Diabetes mellitus is a rapidly rising metabolic disorder with important systemic complications. Global figures have demonstrated the prevalence of diabetes mellitus has almost quadrupled from 108 million in 1980 to 422 million in 2014, with a current prevalence of over 525 million.
Ankit Desai, Runzhi Chen, Axel Cayetano, Channa N. Jayasena, Suks Minhas   +4 more
wiley   +1 more source

Manipulation of Chemistry and Biology with Visible Light Using Tetra‐ortho‐Substituted Azobenzenes and Azonium Ions

Angewandte Chemie, EarlyView.
Tetra‐ortho‐Azobenzenes (TOABs) in broad daylight: in recent years, TOAB photoswitches became indispensable tools for all‐visible‐light manipulation of chemistry, biology and materials. This review explores their unique photochemical properties, design and synthetic approaches, offering support in choosing a TOAB for a given application.
Francesca Cardano, Rosa Márquez García, Wiktor Szymanski   +2 more
wiley   +2 more sources

Activation of muscarinic acetylcholine receptors elicits pigment granule dispersion in retinal pigment epithelium isolated from bluegill

BMC Neuroscience, 2004
Background In fish, melanin pigment granules in the retinal pigment epithelium disperse into apical projections as part of the suite of responses the eye makes to bright light conditions.
Crittenden Elizabeth L, González Alfredo, García Dana M   +2 more
doaj   +1 more source

Percolation on interacting, antagonistic networks [PDF]

J. Stat. Mech. (2013) P05005, 2012
Recently, new results on percolation of interdependent networks have shown that the percolation transition can be first order. In this paper we show that, when considering antagonistic interactions between interacting networks, the percolation process might present a bistability of the equilibrium solution.
arxiv   +1 more source

Synthesis and Characterization of Photoswitchable Covalent Ligands for the β2‐Adrenoceptor

Angewandte Chemie, EarlyView.
A structure‐based design of a covalent photoswitchable ligand for the β2‐adrenergic receptor, a therapeutically relevant GPCR, is described. This tool facilitates the modification of the intrinsic activity of the protein by light. Computational analysis of its mechanism of action suggests that the photoswitch takes place within the binding pocket ...
Ulrike Wirth, Eduard Neu, Davide Provasi, Steffen Feustel, Maximilian F. Schmidt, Harald Hübner, Dorothée Weikert, Marta Filizola, Burkhard König, Peter Gmeiner   +9 more
wiley   +2 more sources

Percolation on interdependent networks with a fraction of antagonistic interactions [PDF]

Journal of Statistical Physics, 152,1069 (2013), 2013
Recently, the percolation transition has been characterized on interacting networks both in presence of interdependent and antagonistic interactions. Here we characterize the phase diagram of the percolation transition in two Poisson interdependent networks with a percentage q of antagonistic nodes. We show that this system can present a bistability of
arxiv   +1 more source