Results 61 to 70 of about 107,657 (326)
Positive Allosteric Modulator of GABA Lowers BOLD Responses in the Cingulate Cortex. [PDF]
PLoS ONE, 2016 Knowledge about the neural underpinnings of the negative blood oxygen level dependent (BOLD) responses in functional magnetic resonance imaging (fMRI) is still limited.
Susanna A Walter +7 more
doaj +1 more source
Mechanism of β2AR regulation by an intracellular positive allosteric modulator
Science, 2019 Positive reinforcement in a GPCR Many drug discovery efforts focus on G protein–coupled receptors (GPCRs), a class of receptors that regulate many physiological processes.
Xiangyu Liu +13 more
semanticscholar +1 more source
Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R
, 2021 The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R).
Salamone, Stefano +5 more
core +1 more source
De Novo Design of Peptidic Positive Allosteric Modulators Targeting TRPV1 with Analgesic Effects
Advanced Science, 2021 Transient receptor potential vanilloid 1 (TRPV1) ion channel is a nociceptor critically involved in pain sensation. Direct blockade of TRPV1 exhibits significant analgesic effects but also incurs severe side effects such as hyperthermia, causing failures
Lizhen Xu +10 more
doaj +1 more source
Clinical Pharmacokinetics, 2019 SAGE-217, a novel γ-aminobutyric acid A (GABAA) receptor positive allosteric modulator, was evaluated in phase I, double-blind, placebo-controlled, single ascending dose (SAD) and multiple ascending dose (MAD) studies to assess the safety and ...
E. Hoffmann +9 more
semanticscholar +1 more source
Novel positive allosteric modulators of GABAA receptors with anesthetic activity [PDF]
Scientific Reports, 2016 AbstractGABAAreceptors are the main inhibitory neurotransmitter receptors in the brain and are targets for numerous clinically important drugs such as benzodiazepines, anxiolytics and anesthetics. We previously identified novel ligands of the classical benzodiazepine binding pocket in α1β2γ2GABAAreceptors using an experiment-guided virtual screening ...
Maldifassi MC +5 more
openaire +3 more sources
eLife, 2020 Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams +12 more
doaj +1 more source
CGP7930: A Positive Allosteric Modulator of the GABAB Receptor [PDF]
CNS Drug Reviews, 2007 ABSTRACTCGP7930 (3‐(3′,5′‐Di‐tert‐butyl‐4′‐hydroxy)phenyl‐2,2‐dimethylpropanol) is a positive allosteric modulator of the metabotropic GABAB receptor. CGP7930 has been found to modulate the GABAB receptor in the open, or high affinity, state increasing agonist affinity for the receptor and signal transduction efficacy following agonist stimulation. The
C L, Adams, A J, Lawrence
openaire +2 more sources
Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation [PDF]
Journal of Inflammation, 2014 Adenosine is produced at high levels at inflamed sites as a by-product of cellular activation and breakdown. Adenosine mediates its anti-inflammatory activity primarily through the adenosine A2a receptor (A2aR), a member of the G-protein coupled receptors. A2aR agonists have demonstrated anti-inflammatory efficacy, however, their therapeutic utility is
Welihinda, Ajith A, Amento, Edward P
openaire +2 more sources
Saudi Pharmaceutical Journal, 2023 Chemotherapy-induced peripheral neuropathy (CIPN) is one of chemotherapies’ most often documented side effects. Patients with CIPN experience spontaneous burning, numbness, tingling, and neuropathic pain in their feet and hands.
Amina M. Bagher +3 more
doaj +1 more source