Results 11 to 20 of about 4,995,094 (293)

4-Chlorophenylguanidine is an ASIC3 agonist and positive allosteric modulator

Journal of Pharmacological Sciences, 2017
Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems.
Amruta S. Agharkar, Eric B. Gonzales
doaj   +2 more sources

Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator

Journal of Pharmacological Sciences, 2018
Oxytocin (OT) is a 9-amine neuropeptide that plays an essential role in mammalian labor, lactation, maternal bonding, and social affiliation. OT has been reported to exert an analgesic effect in both humans and animals, and the results of certain animal ...
Yoshiyuki Meguro, Kanako Miyano, Shigeto Hirayama, Yuki Yoshida, Naoto Ishibashi, Takumi Ogino, Yuriko Fujii, Sei Manabe, Moeko Eto, Miki Nonaka, Hideaki Fujii, Yoichi Ueta, Minoru Narita, Naohiro Sata, Toshihiko Yada, Yasuhito Uezono   +15 more
doaj   +2 more sources

Positive allosteric modulator activity of ginsenosides is restricted to P2X7 and P2X4 receptors. [PDF]

Purinergic Signal
Positive allosteric modulators of P2X7 receptors hold promise as host-directed immune enhancers in intracellular infections. We have previously reported the use of protopanaxadiol ginsenosides as positive allosteric modulators of human, rat and mouse ...
Allum E, Stokes L.
europepmc   +3 more sources

Positive allosteric modulator selective for adult muscle nicotinic acetylcholine receptor. [PDF]

Proc Natl Acad Sci U S A
The muscle nicotinic acetylcholine receptor (AChR) is the key mediator of neuromuscular signal transmission and is essential for all voluntary movement in our body. In this study, we present DC-98-LC74, a positive allosteric modulator (PAM) for the adult
Webster RG, Alabaf S, Li A, Beerli R, Siehler S, Imbert PE, Lee L, Cossins J, Koziczak-Holbro M, Flotte L, Gaudet L, Gerwin N, Beeson D, Dong YY.   +13 more
europepmc   +2 more sources

Kinetic Benefit(s) of Allosteric Receptor Blockade by Positive Allosteric Modulator Antagonists. [PDF]

ACS Pharmacol Transl Sci
This paper discusses how targeted pharmacologic experiments can elucidate the mechanism of allosteric receptor inhibitors (NAMs) to identify NAMs that may have exceptionally useful properties and target residence times in vivo.
Vauquellin G, Kenakin T.
europepmc   +2 more sources

Characterization of a novel positive allosteric modulator of the α1A-Adrenergic receptor

Current Research in Pharmacology and Drug Discovery, 2023
α1-Adrenergic Receptors (ARs) are G-protein Coupled Receptors (GPCRs) that regulate the sympathetic nervous system via the binding and activation of norepinephrine (NE) and epinephrine (Epi). α1-ARs control various aspects of neurotransmission, cognition,
Robert S. Papay, Jonathan D. Macdonald, Shaun R. Stauffer, Dianne M. Perez   +3 more
doaj   +1 more source

In silico Insights on the Allosteric Modulation of the µ-Opioid Receptor and G protein Complex in the Presence of Agonist Ligand BU72 and Potential Positive Allosteric Modulator BMS-986121 [PDF]

, 2020
The G protein-coupled receptor (GPCR) µ-opioid receptor (µOR) is one of several drug targets of commercially available therapeutics for pain. Various opioid drugs like morphines have been associated to numerous substance abuse-related deaths around the ...
Ricky, Nellas, Mac Kevin, Braza
core   +1 more source

Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]

Proceedings of the National Academy of Sciences, 2013
μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford, Mary J, Clark, Tom S, Wehrman, Samuel W, Gerritz, Martyn, Banks, Jonathan, O'Connell, John R, Traynor, Andrew, Alt   +7 more
openaire   +2 more sources

REPROGRAMMING CBX8-PRC1 FUNCTION WITH A POSITIVE ALLOSTERIC MODULATOR [PDF]

Cell Chemical Biology, 2021
ABSTRACT Canonical targeting of Polycomb Repressive Complex 1 (PRC1) to repress developmental genes is mediated by cell type-specific, paralogous chromobox (CBX) proteins (CBX2, 4, 6, 7 and 8). Based on their central role in silencing and their misregulation associated with human disease including ...
Junghyun L. Suh, Daniel Bsteh, Bryce Hart, Yibo Si, Tyler M. Weaver, Carina Pribitzer, Roy Lau, Shivani Soni, Heather Ogana, Justin M. Rectenwald, Jacqueline L. Norris, Stephanie H. Cholensky, Cari Sagum, Jessica D. Umana, Dongxu Li, Brian Hardy, Mark T. Bedford, Shannon M. Mumenthaler, Heinz-Josef Lenz, Yong-Mi Kim, Gang Greg Wang, Ken H. Pearce, Lindsey I. James, Dmitri B. Kireev, Catherine A. Musselman, Stephen V. Frye, Oliver Bell   +26 more
openaire   +3 more sources

Potentiation and allosteric agonist activation of α7 nicotinic acetylcholine receptors: binding sites and hypotheses

Pharmacological Research, 2023
Considerable progress has been made in recent years towards the identification and characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs).
Victoria R. Sanders, Neil S. Millar
doaj   +1 more source