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 +15 more
doaj +3 more sources
Mapping a novel positive allosteric modulator binding site in the central vestibule region of human P2X7 [PDF]
Scientific Reports, 2019 P2X7 receptors are important in the regulation of inflammatory responses and immune responses to intracellular pathogens such as Mycobacterium tuberculosis and Toxoplasma gondii.
Stefan Bidula +4 more
semanticscholar +4 more sources
Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage [PDF]
Scientific Reports, 2017 Pepcan-12 (RVD-hemopressin; RVDPVNFKLLSH) is the major peptide of a family of endogenous peptide endocannabinoids (pepcans) shown to act as negative allosteric modulators (NAM) of cannabinoid CB1 receptors.
Vanessa Petrucci +6 more
semanticscholar +2 more sources
Allosteric Modulation of Muscarinic Acetylcholine Receptors
Pharmaceuticals, 2010 An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
doaj +2 more sources
A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain
Neuropharmacology, 2017 Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission and are key nervous system drug targets. While diverse pharmacological tools have yielded insight into iGluR extracellular domain function, less is known about molecular ...
Tzu-Ming Wang +2 more
exaly +2 more sources
Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li +5 more
doaj +2 more sources
Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels.
PLoS ONE, 2017 There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity.
Mustafa Nazıroğlu +10 more
doaj +2 more sources
PLoS ONE, 2017 S 47445 is a novel positive allosteric modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors (AMPA-PAM). S 47445 enhanced glutamate's action at AMPA receptors on human and rat receptors and was inactive at NMDA and ...
Sylvie Bretin +18 more
doaj +2 more sources
Gestodene, a novel positive allosteric modulator of PAR1, enhances PAR1-mediated human platelet aggregation [PDF]
Frontiers in PharmacologyBackground: Protease-activated receptor 1 (PAR1) is expressed in human platelets and can be activated by low concentrations of thrombin. Vorapaxar, a selective antagonist of PAR1, inhibits thrombin-induced calcium mobilization in human platelet, which is
So-Hyeon Park +9 more
doaj +2 more sources
A Positive Allosteric Modulator of the Serotonin 5-HT2C Receptor for Obesity.
Journal of Medicinal Chemistry, 2017 The 5-HT2CR agonist lorcaserin, clinically approved for the treatment of obesity, causes important side effects mainly related to subtype selectivity. In the search for 5-HT2CR allosteric modulators as safer antiobesity drugs, a chemical library from Vivia Biotech was screened using ExviTech platform. Structural modifications of identified hit VA240 in
Javier García-Cárceles +14 more
semanticscholar +7 more sources