Results 161 to 170 of about 19,325 (262)

A Positive Allosteric Modulator of the SERCA Pump Rescues Hippocampal Neuronal Circuits Dysfunction and Cognitive Defects in a Mouse Model of Alzheimer's Disease. [PDF]

J Neurosci
Gerasimov E, Rakovskaya A, Pchitskaya E, Vlasova O, Dahl R, Bezprozvanny I.   +5 more
europepmc   +1 more source

Sodium butyrate ameliorates renal tubular lipid accumulation through a protein phosphatase 2A/transcription factor EB axis in diabetic nephropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Extensive evidence indicates that lipid accumulation causes renal tubular injury, which further contributes to diabetic nephropathy (DN) progression. Short‐chain fatty acids (SCFAs) play an important role in the maintenance of cellular metabolic health.
Jiayin Tao, Sinan Ai, Yaoxian Wang, Yuning Liu, Jingwei Zhou, Qingqing Liu, Xu Wang, Danting Li, Xin Li, Lin Wang, Jinyi Hou, Liang Peng, Zhen Wang   +12 more
wiley   +1 more source

Positive allosteric modulator activity of ginsenosides is restricted to P2X7 and P2X4 receptors

Allum E, Stokes L.
europepmc   +1 more source

Formulation and characterization of CMPI nanoparticles for enhanced targeting of brain nicotinic receptors by positive allosteric modulator. [PDF]

Sci Rep
Aly R, Sulthana S, Beaudoin R, Hamouda AK, Aryal S.   +4 more
europepmc   +1 more source

Molecular basis for a pore block of Tentonin 3 expressed in HEK293 cells by a conopeptide, NMB‐1

British Journal of Pharmacology, EarlyView.
Background and Purpose Tentonin 3 (TTN3/TMEM150C) is a mechanosensitive ion channel that plays critical roles in mechanotransduction processes. TTN3 forms a tetramer with a predicted rectangular shape and a central pore. A conotoxin ρ‐TIA and its synthetic analog, noxious mechanosensation blocker 1 (NMB‐1), were initially developed to inhibit slowly ...
Sujin Lim, Junhyuk Woo, Sungmin Pak, Joonho Paik, Gyu‐Sang Hong, Ji Hun Wi, Sanghee Lee, Cristina Fenollar‐Ferrer, Kyungreem Han, Young Kee Shin, Uhtaek Oh   +10 more
wiley   +1 more source

Mu Opioid Receptor Positive Allosteric Modulator BMS-986122 Confers Agonist-Dependent G Protein Subtype Signaling Bias. [PDF]

Biochemistry
Grieble GM, Knapp BI, Bidlack JM.
europepmc   +1 more source

Critical role of the mast cell/tryptase/PAR2 axis in anastrozole‐induced pain

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Anastrozole, an aromatase inhibitor, is used to treat postmenopausal women with hormone receptor‐positive breast cancer, but also induces musculoskeletal pain and can lead to therapeutic regimen suspension. Aromatase inhibitors promote the release of pro‐inflammatory substances from sensitised nerve fibres, which might ...
Maria Fernanda Pessano Fialho, Raquel Tonello, Evelyne Silva Brum, Gabriela Becker, Nigel W. Bunnett, Sara Marchesan Oliveira   +5 more
wiley   +1 more source

A PK/PD study on antihyperalgesia by an α2/3‐GABAA receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose GABAA receptors (GABAARs) are heteropentameric ion channels that control almost all CNS functions, including spinal nociception. Most GABAARs contain a γ2 subunit but differ in their α and β subunit composition. TPA023B is an α2/α3 subtype selective, non‐sedative, positive allosteric modulator (PAM) with antihyperalgesic
Elena Neumann, Mariana O. Popa, Karen T. Elvers, Misa Oyama, Daniel Ulrich, Marcus Hanley, Gui Jie Feng, Thomas Hathaway, William T. Ralvenius, Thomas Grampp, Dietmar Benke, John R. Atack, Hanns Ulrich Zeilhofer   +12 more
wiley   +1 more source

Further In Vitro and Ex Vivo Pharmacological and Kinetic Characterizations of CCF219B: A Positive Allosteric Modulator of the α_1A-Adrenergic Receptor. [PDF]

Pharmaceuticals (Basel)
Papay RS, Perez DM.
europepmc   +1 more source

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source