Results 71 to 80 of about 1,083,474 (317)

Adenosine A1 Receptor Agonist 2-chloro-N6-cyclopentyladenosine and Hippocampal Excitability During Brain Development in Rats

Frontiers in Pharmacology, 2019
Objective: The adenosinergic system may influence excitability in the brain. Endogenous and exogenous adenosine has anticonvulsant activity presumably by activating A1 receptors.
Petr Fabera, Petr Fabera, Martina Parizkova, Martina Parizkova, Libor Uttl, Libor Uttl, Katerina Vondrakova, Katerina Vondrakova, Hana Kubova, Grygoriy Tsenov, Grygoriy Tsenov, Pavel Mares   +11 more
doaj   +1 more source

DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo

ACS Pharmacology & Translational Science, 2018
Chemogenetic tools such as designer receptors exclusively activated by designer drugs (DREADDs) are routinely used to modulate neuronal and non-neuronal signaling and activity in a relatively noninvasive manner.
K. Thompson, Elham Khajehali, S. Bradley, Jovana S. Navarrete, Xi Ping Huang, Samuel T. Slocum, Jian Jin, Jing Liu, Y. Xiong, Reid H. J. Olsen, J. Diberto, K. Boyt, M. Pina, Dipanwita Pati, Colin Molloy, C. Bundgaard, P. Sexton, T. Kash, M. Krashes, A. Christopoulos, B. Roth, A. Tobin   +21 more
semanticscholar   +1 more source

Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze [PDF]

, 2012
The role of the histamine H3 receptor (H3R) in anxiety is controversial, due to limitations in drug selectivity and limited validity of behavioral tests used in previous studies. In the present report, we describe two experiments.
Abuhamdah, Rushdie M., Chazot, Paul L., Ennaceur, Abdelkader, Lethbridge, Natasha L., van Rensburg, Ruan   +4 more
core   +1 more source

Identification and Semi-Synthesis of 3-O-Protocatechuoylceanothic Acid, a Novel and Natural GPR120 Agonist †

Molecules, 2019
The identification and three step synthesis of 3-O-protocatechuoylceanothic acid, a novel and natural GPR120 agonist, is described. This ceanothane-type triterpenoid was identified from the components of Ziziphus jujuba roots and was found to be a new ...
Changjin Lim, Jung Gyu Park, Kyo Bin Kang, Young-Ger Suh   +3 more
doaj   +1 more source

Development of Diphenethylamines as Selective Kappa Opioid Receptor Ligands and Their Pharmacological Activities

Molecules, 2020
Among the opioid receptors, the kappa opioid receptor (KOR) has been gaining substantial attention as a promising molecular target for the treatment of numerous human disorders, including pain, pruritus, affective disorders (i.e., depression and anxiety),
Helmut Schmidhammer, Filippo Erli, Elena Guerrieri, Mariana Spetea   +3 more
doaj   +1 more source

STING agonist therapy in combination with PD-1 immune checkpoint blockade enhances response to carboplatin chemotherapy in high-grade serous ovarian cancer

British Journal of Cancer, 2018
High-grade serous carcinoma (HGSC) of the ovary is predominantly diagnosed at late stages and primarily treated with debulking surgery followed by platinum/taxane-based chemotherapy.
A. Ghaffari, Nichole T. Peterson, Kasra Khalaj, N. Vitkin, A. Robinson, J. Francis, M. Koti   +6 more
semanticscholar   +1 more source

Discovery of a Novel Chemo-Type for TAAR1 Agonism via Molecular Modeling

Molecules
The search for novel effective TAAR1 ligands continues to draw great attention due to the wide range of pharmacological applications related to TAAR1 targeting. Herein, molecular docking studies of known TAAR1 ligands, characterized by an oxazoline core,
Giancarlo Grossi, Naomi Scarano, Francesca Musumeci, Michele Tonelli, Evgeny Kanov, Anna Carbone, Paola Fossa, Raul R. Gainetdinov, Elena Cichero, Silvia Schenone   +9 more
doaj   +1 more source

Chemerin Elicits Potent Constrictor Actions via Chemokine‐Like Receptor 1 (CMKLR1), not G‐Protein‐Coupled Receptor 1 (GPR1), in Human and Rat Vasculature

Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2016
BackgroundCirculating levels of chemerin are significantly higher in hypertensive patients and positively correlate with blood pressure. Chemerin activates chemokine‐like receptor 1 (CMKLR1 or ChemR23) and is proposed to activate the “orphan” G‐protein ...
Amanda J. Kennedy, Peiran Yang, Cai Read, Rhoda E. Kuc, Lucy Yang, Emily J. A. Taylor, Colin W. Taylor, Janet J. Maguire, Anthony P. Davenport   +8 more
doaj   +1 more source

Regulations of T Cell Activation by Membrane and Cytoskeleton

Membranes, 2020
Among various types of membrane proteins that are regulated by cytoskeleton, the T cell receptor (TCR) greatly benefits from these cellular machineries for its function.
Yoshihisa Kaizuka
doaj   +1 more source

Allosteric coupling from G protein to the agonist binding pocket in GPCRs

Nature, 2016
G-protein-coupled receptors (GPCRs) remain the primary conduit by which cells detect environmental stimuli and communicate with each other. Upon activation by extracellular agonists, these seven-transmembrane-domain-containing receptors interact with ...
Brian T DeVree, Jacob P. Mahoney, Gisselle A. Vélez-Ruiz, S. Rasmussen, A. Kuszak, E. Edwald, J. Fung, A. Manglik, M. Masureel, Yang Du, R. Matt, E. Pardon, J. Steyaert, B. Kobilka, R. Sunahara   +14 more
semanticscholar   +1 more source