Results 71 to 80 of about 119,693 (290)

Small molecule allosteric modulation of the adenosine A1 receptor

Frontiers in Endocrinology, 2023
G protein-coupled receptors (GPCRs) represent the target for approximately a third of FDA-approved small molecule drugs. The adenosine A1 receptor (A1R), one of four adenosine GPCR subtypes, has important (patho)physiological roles in humans.
Anh T. N. Nguyen, Quan L. Tran, Jo-Anne Baltos, Samantha M. McNeill, Diep T. N. Nguyen, Lauren T. May   +5 more
doaj   +1 more source

The Interaction of Gabapentin and N6-(2-phenylisopropyl)-adenosine R-(-)isomer (R-PIA) on Mechanical Allodynia in Rats with a Spinal Nerve Ligation [PDF]

, 2008
We examined the antiallodynic interaction between gabapentin and adenosine A1 receptor agonist, N6-(2-phenylisopropyl)-adenosine R-(-)isomer (R-PIA), in a rat model of nerve ligation injury. Rats were prepared with ligation of left L5-6 spinal nerves and
Bantel, Chaplan, Chapman, Choca, Cui, Dworkin, Eckhardt, Field, Fink, Gilron, Hwang, In Gu Jun, Jong Yeon Park, Kim, Kim, Klotz, Lee, Leem, Luo, Maneuf, Matthews, Matthews, Petroff, Ralevic, Sawynok, Sawynok, Shimoyama, Sosnowski, Su, Tallarida, Taylor, von Heijne, Yaksh, Yoon   +33 more
core   +2 more sources

TCMD: A High‐Throughput and Rapid Method for Screening Antimicrobial Ingredients from Renewable Bio‐Based Resources

Advanced Science, EarlyView.
This study develops a strategy to screen the active compounds from bio‐mixtures via combining transcriptomic profiling and molecular docking. The proposed method demonstrates 100% correction in three different biobased mixtures and is 3–20 times faster than traditional approaches.
Yongdong Xu, Yueyao Wang, Yongming Chen, Yunxia Wang, Shicheng Zhang, Gang Luo, Fuhao Cui, Taisheng Du, Zhidan Liu   +8 more
wiley   +1 more source

Adenosine A\u3csub\u3e1\u3c/sub\u3e receptor-mediated protection of mouse hippocampal synaptic transmission against oxygen and/or glucose deprivation: A comparative study [PDF]

, 2019
© 2019 the American Physiological Society. Adenosine receptors are widely ex-pressed in the brain, and adenosine is a key bioactive substance for neuroprotection.
Kawamura, Masahito, Masino, Susan A., Ruskin, David N.   +2 more
core   +1 more source

Renal tubule necrosis and apoptosis modulation by A1 adenosine receptor expression [PDF]

, 2007
We have shown that A1 adenosine receptors (A1ARs) are cytoprotective against renal tubular necrosis and apoptosis both in vivo and in vitro. To study the role of A1AR numbers on renal epithelial cell survival, we stably overexpressed the human A1 ...
Emala, C.W., Jan, M., Kim, M., Lee, H.T., Penn, R.B.   +4 more
core   +1 more source

The cumulative analgesic effect of repeated electroacupuncture is modulated by Adora3 in the SCDH of mice with neuropathic pain

Animal Models and Experimental Medicine, EarlyView.
Neuropathic pain management via repeated electroacupuncture. Abstract Background Existing remedial approaches for relieving neuropathic pain (NPP) are challenging and open the way for alternative therapeutic measures such as electroacupuncture (EA). The mechanism underlying the antinociceptive effects of repeated EA sessions, particularly concerning ...
Faisal Ayub Kiani, Hao Li, Panpan Guo, Qiulin Zhang, Mahmoud M. Abouelfetouh, Mingxing Ding, Yi Ding   +6 more
wiley   +1 more source

Pulsed Electromagnetic Fields: A Novel Attractive Therapeutic Opportunity for Neuroprotection After Acute Cerebral Ischemia

Neuromodulation: Technology at the Neural Interface, EarlyView., 2021
Abstract Objectives Acute cerebral ischemia is characterized by several pathological processes evolving during time, which contribute to the final tissue damage. Secondary processes, such as prolonged inflammatory response, impaired mitochondrial function and oxidative stress, are responsible for the progression of brain injury to the peri‐infarct area,
Fioravante Capone, Simona Salati, Fabrizio Vincenzi, Micaela Liberti, Giorgio Aicardi, Francesca Apollonio, Katia Varani, Ruggero Cadossi, Vincenzo Di Lazzaro   +8 more
wiley   +1 more source

An Allosteric Modulator of the Adenosine A1 Receptor Improves Cardiac Function Following Ischaemia in Murine Isolated Hearts

Pharmaceuticals, 2013
The effect of an allosteric modulator of the adenosine A1 receptors was investigated using an ischaemia-reperfusion protocol in murine isolated hearts. Isolated hearts were perfused with Kreb-Henseleit solution gassed with carbogen gas (95% O2 and 5% CO2)
Roselyn B. Rose'Meyer, Shane M. Devine, Peter J. Scammells, Paul J. White, Anna Butcher   +4 more
doaj   +1 more source

Adenosine Deaminase and A1 Adenosine Receptors Internalize Together following Agonist-induced Receptor Desensitization [PDF]

Journal of Biological Chemistry, 1998
A1 adenosine receptors (A1Rs) and adenosine deaminase (ADA; EC 3.5.4. 4) interact on the cell surface of DDT1MF-2 smooth muscle cells. The interaction facilitates ligand binding and signaling via A1R, but it is not known whether it has a role in homologous desensitization of A1Rs. Here we show that chronic exposure of DDT1MF-2 cells to the A1R agonist,
Saura Antolín, Carlos A. (Carlos Alberto), Mallol Montero, Josefa, Canela Campos, Enric I., Lluís i Biset, Carme, Franco Fernández, Rafael   +4 more
openaire   +4 more sources

Uncovering New Therapeutic Targets for Amyotrophic Lateral Sclerosis and Neurological Diseases Using Real‐World Data

Clinical Pharmacology &Therapeutics, EarlyView.
Although attractive for relevance to real‐world scenarios, real‐world data (RWD) is typically used for drug repurposing and not therapeutic target discovery. Repurposing studies have identified few effective options in neurological diseases such as the rare disease, amyotrophic lateral sclerosis (ALS), which has no disease‐modifying treatments ...
Mohammadali Alidoost, Jeremy Y. Huang, Georgia Dermentzaki, Anna S. Blazier, Giorgio Gaglia, Timothy R. Hammond, Francesca Frau, Mary Clare McCorry, Dimitry Ofengeim, Jennifer L. Wilson   +9 more
wiley   +1 more source