Results 71 to 80 of about 3,728 (241)

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

Association of Anticholinergic Burden with Cognitive and Functional Status in a Cohort of Hospitalized Elderly: Comparison of the Anticholinergic Cognitive Burden Scale and Anticholinergic Risk Scale [PDF]

, 2012
Background Drugs with anticholinergic effects are associated with adverse events such as delirium and falls as well as cognitive decline and loss of independence.
CORRAO, Salvatore, Djade, C. D, Franchi, C, Iorio, A, Lucca, U, Mannucci, P. M., Marcucci, M, Marengoni, A, Nobili, A, Pasina, L, Salerno, F, Tettamanti, M, Violi, F   +12 more
core   +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

Marjoram Relaxes Rat Thoracic Aorta Via a PI3-K/eNOS/cGMP Pathway

Biomolecules, 2019
Despite pharmacotherapeutic advances, cardiovascular disease (CVD) remains the primary cause of global mortality. Alternative approaches, such as herbal medicine, continue to be sought to reduce this burden.
Adnan Badran, Elias Baydoun, Ali Samaha, Gianfranco Pintus, Joelle Mesmar, Rabah Iratni, Khodr Issa, Ali H. Eid   +7 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

Hepatic microRNA profiles offer predictive and mechanistic insights after exposure to genotoxic and epigenetic hepatocarcinogens. [PDF]

, 2012
In recent years, accumulating evidence supports the importance of microRNAs in liver physiology and disease; however, few studies have examined the involvement of these noncoding genes in chemical hepatocarcinogenesis.
Currie, RA, Gooderham, NJ, Koufaris, C, Wright, J   +3 more
core   +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

Pharmacology of novel psychoactive substances [PDF]

, 2016
This PhD work consists of an in vitro and in vivo part. In the in vivo part, we investigated the role of dopamine in the acute clinical effects of 3,4-methylenedioxymethamphetamine (MDMA, “ecstasy”) in healthy human subjects.
Rickli, Anna
core   +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