Results 61 to 70 of about 1,693 (192)

Functional G-Protein-Coupled Receptor (GPCR) Synthesis: The Pharmacological Analysis of Human Histamine H1 Receptor (HRH1) Synthesized by a Wheat Germ Cell-Free Protein Synthesis System Combined with Asolectin Glycerosomes

Frontiers in Pharmacology, 2018
G-protein-coupled receptors (GPCRs) are membrane proteins distributed on the cell surface, and they may be potential drug targets. However, synthesizing GPCRs in vitro can be challenging. Recently, some cell-free protein synthesis systems have been shown
Yasuyuki Suzuki, Tomio Ogasawara, Yuki Tanaka, Hiroyuki Takeda, Tatsuya Sawasaki, Masaki Mogi, Shuang Liu, Kazutaka Maeyama   +7 more
doaj   +1 more source

Binding characteristics of the doxepin E/Z‐isomers to the histamine H1 receptor revealed by receptor‐bound ligand analysis and molecular dynamics study

Journal of Molecular Recognition, Volume 37, Issue 5, September 2024.
Abstract Doxepin is an antihistamine and tricyclic antidepressant that binds to the histamine H1 receptor (H1R) with high affinity. Doxepin is an 85:15 mixture of the E‐ and Z‐isomers. The Z‐isomer is well known to be more effective than the E‐isomer, whereas based on the crystal structure of the H1R/doxepin complex, the hydroxyl group of Thr1123.37 is
Hiroto Kaneko, Ryunosuke Korenaga, Ryota Nakamura, Shinnosuke Kawai, Tadashi Ando, Mitsunori Shiroishi   +5 more
wiley   +1 more source

Salvia fruticosa Induces Vasorelaxation In Rat Isolated Thoracic Aorta: Role of the PI3K/Akt/eNOS/NO/cGMP Signaling Pathway

Scientific Reports, 2017
Salvia fruticosa (SF) Mill. is traditionally used for its antihypertensive actions. However, little is known about its pharmacologic and molecular mechanisms of action.
M. Akhtar Anwar, Ali A. Samaha, Samar Ballan, Alaaeldin I. Saleh, Rabah Iratni, Ali H. Eid   +5 more
doaj   +1 more source

Assessing the anticholinergic cognitive burden classification of putative anticholinergic drugs using drug properties

British Journal of Clinical Pharmacology, Volume 90, Issue 9, Page 2236-2255, September 2024.
Aims This study evaluated the use of machine learning to leverage drug absorption, distribution, metabolism and excretion (ADME) data together with physicochemical and pharmacological data to develop a novel anticholinergic burden scale and compare its performance to previously published scales.
Geofrey Oteng Phutietsile, Nikoletta Fotaki, Prasad S. Nishtala   +2 more
wiley   +1 more source

Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine‐Independent and Chronic Itch

Advanced Science, Volume 11, Issue 15, April 17, 2024.
The potassium channel Slack is highly expressed in sensory neurons that sense itch. In this study, several new compounds that activate Slack are developed. It is found that the lead molecule, compound 6, effectively inhibits scratching elicited by multiple pruritogens in mice establishing Slack activation as a novel pharmacological strategy for the ...
Annika Balzulat, W. Felix Zhu, Cathrin Flauaus, Victor Hernandez‐Olmos, Jan Heering, Sunesh Sethumadhavan, Mariam Dubiel, Annika Frank, Amelie Menge, Maureen Hebchen, Katharina Metzner, Ruirui Lu, Robert Lukowski, Peter Ruth, Stefan Knapp, Susanne Müller, Dieter Steinhilber, Inga Hänelt, Holger Stark, Ewgenij Proschak, Achim Schmidtko   +20 more
wiley   +1 more source

Brain Histamine Modulates the Antidepressant-Like Effect of the 3-Iodothyroacetic Acid (TA1)

Frontiers in Cellular Neuroscience, 2019
3-iodothyroacetic acid (TA1), an end metabolite of thyroid hormone, has been shown to produce behavioral effects in mice that are dependent on brain histamine.
Annunziatina Laurino, Elisa Landucci, Lorenzo Cinci, Manuela Gencarelli, Gaetano De Siena, Lorenza Bellusci, Grazia Chiellini, Laura Raimondi   +7 more
doaj   +1 more source

Sensitization to ethylenediamine dihydrochloride in patients with contact dermatitis in northeastern Italy from 1996 to 2021

Contact Dermatitis, Volume 90, Issue 3, Page 253-261, March 2024.
Ongoing surveillance on prevalence of contact sensitization contributes to maintaining an up‐to‐date standard series in different geographical areas. Contact allergy to EDD yielded a sensitization prevalence <1% in recent years in northeastern Italy, and we therefore consider no longer justifiable to include this hapten in our baseline patch test ...
Linda Piapan, Anna Belloni Fortina, Erika Giulioni, Francesca Larese Filon   +3 more
wiley   +1 more source

Comparing antihistaminic activity of clemastine and pyrilamine in guinea pig ileum [PDF]

, 2005
O presente trabalho teve como objetivo comparar fármacos utilizados como antihistamínicos na terapêutica de patologias alérgicas em pequenos animais.
Vieira, Luciane Cristina
core  

Additional file 1 of Disruption of histamine/H1R signaling pathway represses cardiac differentiation and maturation of human induced pluripotent stem cells [PDF]

, 2020
Additional file 1 : Figure S1. (related to Fig. 1). Inhibition of H1R minimally affected normal cardiac morphology and birth rates in mice. (A) Representative H&E staining sections of cardiac tissue obtained from neonatal WT and HDC-/- mice on day 1 and ...
Zhiwei Zhang (12077), Junbo Ge (385426), Xiaowei Zhu (24440), Suling Ding (7858091), Jian Wu (41301), Hui Li (32376), Xiangfei Wang (8528514), Yunzeng Zou (188550), Lili Xu (257856), Xiangdong Yang (287443)   +9 more
core   +1 more source

Endothelium-dependent relaxation of rat aorta to a histamine H3 agonist is reduced by inhibitors of nitric oxide synthase, guanylate cyclase and Na+,K+-ATPase

Mediators of Inflammation, 1996
The possible involvement of different effector systems (nitric oxide synthase, guanylate cyclase, β-adrenergic and muscarinic cholinergic receptors, cyclooxygenase and lipoxygenase, and Na+,K+-ATPase) was evaluated in a histamine H3 receptor agonist ...
D. M. Djuric, M. T. Nesic, I. Z. Andjelkovic   +2 more
doaj   +1 more source