Results 241 to 250 of about 22,949 (304)

Discovery of VU0467319: an M₁ Positive Allosteric Modulator Candidate That Advanced into Clinical Trials. [PDF]

ACS Chem Neurosci
Poslunsey MS, Wood MR, Han C, Stauffer SR, Panarese JD, Melancon BJ, Engers JL, Dickerson JW, Peng W, Noetzel MJ, Cho HP, Rodriguez AL, Hopkins CR, Morrison R, Crouch RD, Bridges TM, Blobaum AL, Boutaud O, Daniels JS, Kates MJ, Castelhano A, Rook JM, Niswender CM, Jones CK, Conn PJ, Lindsley CW.   +25 more
europepmc   +1 more source

Targeting the noncatalytic activity of GSK3β modulates neuronal excitability in medium spiny neurons via Nav1.6 interactions

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh, Zahra Haghighijoo, Akanksha Gurtu, Nolan M. Dvorak, Timothy J. Baumgartner, Nana A. Goode, Jully Singh, Matteo Bernabucci, Adam T. Szafran, Michael J. Bolt, Michael A. Mancini, Natalie M. Dvorak, Marijn Lijffijt, Zhiqing Liu, Yu Xue, Alyssa K. Thomas, Alejandro Villasante‐Tezanos, Balaji Krishnan, Jia Zhou, Fernanda Laezza   +19 more
wiley   +1 more source

Enhancing Tetrahydrocannabinol's Therapeutic Efficacy in Inflammatory Bowel Disease: The Roles of Cannabidiol and the Cannabinoid 1 Receptor Allosteric Modulator ZCZ011. [PDF]

Pharmaceuticals (Basel)
Thapa D, Patil M, Warne LN, Carlessi R, Falasca M.   +4 more
europepmc   +1 more source

Prevention of microglial activation and postoperative cognitive deficits by positive allosteric modulation of α5‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Background and Purpose Long‐lasting cognitive deficits after surgery in aged individuals, referred to as perioperative neurocognitive disorder (NCD), are a significant public health concern. Such postoperative cognitive deficits are dependent on the presence of microglia in the brain, which, when activated, trigger neuroinflammation.
Jinrui Lyu, Rajasekar Nagarajan, Dishary Sharmin, Prithu Mondal, Maltesh Kambali, Muxiao Wang, Jinyan Zhou, Makoto Inoue, James M. Cook, Uwe Rudolph   +9 more
wiley   +1 more source

Gut microbe-generated phenylacetylglutamine is an endogenous allosteric modulator of β2-adrenergic receptors. [PDF]

Nat Commun
Saha PP, Gogonea V, Sweet W, Mohan ML, Singh KD, Anderson JT, Mallela D, Witherow C, Kar N, Stenson K, Harford T, Fischbach MA, Brown JM, Karnik SS, Moravec CS, DiDonato JA, Naga Prasad SV, Hazen SL.   +17 more
europepmc   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

ENX-101, a GABA_A receptor α2,3,5-selective positive allosteric modulator, displays antiseizure effects in rodent seizure and epilepsy models. [PDF]

Epilepsia
Serrats J, Vadodaria KC, Brubaker W, Barker-Haliski M, White HS, Evrard A, Roucard C, Taylor E, Vanover KE, Cunningham S, Sudarsan V, Rogawski MA.   +11 more
europepmc   +1 more source

Structure-based identification of a G protein-biased allosteric modulator of cannabinoid receptor CB1. [PDF]

Proc Natl Acad Sci U S A
Shen S, Wu C, Lin G, Yang X, Zhou Y, Zhao C, Miao Z, Tian X, Wang K, Yang Z, Liu Z, Guo N, Li Y, Xia A, Zhou P, Liu J, Yan W, Ke B, Yang S, Shao Z.   +19 more
europepmc   +1 more source

Preclinical pharmacology of alogabat: a novel GABA_A-α5 positive allosteric modulator targeting neurodevelopmental disorders with impaired GABA_A signaling. [PDF]

Front Pharmacol
Cecere G, Ballard TM, Knoflach F, Honer M, Hipp JF, Garces P, Mueggler T, Künnecke B, Bruns A, Prinssen EP, Schoenenberger P, Janz P, Redondo R, Biemans B, Knust H, Olivares-Morales A, Brigo A, Schulz JM, Bertrand D, Saxe M, O'Connor EC, Hernandez MC.   +21 more
europepmc   +1 more source

Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic M₁ positive allosteric modulator VU0467319 for Alzheimer's disease: a single ascending-dose study in healthy participants. [PDF]

Alzheimers Res Ther
Conley AC, Key AP, Blackford JU, Russell JK, Albert KM, Gong X, Bubser M, Rook JM, Conn PJ, Lindsley CW, Jones CK, Newhouse PA.   +11 more
europepmc   +1 more source