EPD1504: a novel μ-opioid receptor partial agonist attenuates obsessive–compulsive disorder (OCD)-like behaviors [PDF]
Frontiers in Psychiatry, 2023 Low doses of μ-opioid receptor (MOR) agonists rapidly ameliorate symptoms in treatment-resistant obsessive–compulsive disorder (OCD) patients (10–50% of OCD patients). However, the utility of MOR agonists is limited by their safety liabilities.
Beth Youngblood +3 more
doaj +2 more sources
Structure–Activity Relationship Development Efforts towards Peripherally Selective Analogs of the Cannabinoid Receptor Partial Agonist BAY 59-3074 [PDF]
Molecules, 2022 Selective modulation of peripheral cannabinoid receptors (CBRs) has potential therapeutic applications in medical conditions, including obesity, diabetes, liver diseases, GI disorders and pain.
George Amato +6 more
doaj +2 more sources
The Efficiency of CD4 Recruitment to Ligand-engaged TCR Controls the Agonist/Partial Agonist Properties of Peptide–MHC Molecule Ligands [PDF]
, 1997 One hypothesis seeking to explain the signaling and biological properties of T cell receptor for antigen (TCR) partial agonists and antagonists is the coreceptor density/kinetic model, which proposes that the pharmacologic behavior of a TCR ligand is ...
Joaquı́n Madrenas +4 more
openalex +4 more sources
The β-blocker Nebivolol Is a GRK/β-arrestin Biased Agonist [PDF]
, 2013 Nebivolol, a third generation β-adrenoceptor (β-AR) antagonist (β-blocker), causes vasodilation by inducing nitric oxide (NO) production. The mechanism via which nebivolol induces NO production remains unknown, resulting in the genesis of much of the ...
Andresen, Bradley T. +9 more
core +13 more sources
Biomolecules, 2023 Opioid analgesics such as morphine and fentanyl induce mu-opioid receptor (MOR)-mediated hyperactivity in mice. Herein, we show that morphine, fentanyl, SR-17018, and oliceridine have submaximal intrinsic efficacy in the mouse striatum using 35S-GTPγS ...
Agnes Acevedo-Canabal +7 more
doaj +1 more source
Frontiers in Psychiatry, 2023 Real-world evidence fills in an important gap by providing data on the effectiveness and tolerability of new medications in everyday patients. In this data collection form a Spanish hospital, the effectiveness and tolerability of cariprazine were ...
Lluis Niell Galmes, Elmars Rancans
doaj +1 more source
Reducing Addiction in Bipolar Disorder via Hacking the Dopaminergic System
Frontiers in Psychiatry, 2021 The dopaminergic system plays a central and decisive role in substance use disorder (SUD), bipolar disorder (BD), and possibly in a subgroup of patients with refractory depression.
Heinz Grunze +5 more
doaj +1 more source
PPAR-γ Partial Agonists in Disease-Fate Decision with Special Reference to Cancer
Cells, 2022 Peroxisome proliferator-activated receptor-γ (PPAR-γ) has emerged as one of the most extensively studied transcription factors since its discovery in 1990, highlighting its importance in the etiology and treatment of numerous diseases involving various ...
Sangeeta Ballav +4 more
doaj +1 more source
Structure and Mechanism of Glycine Receptor Elucidated by Cryo-Electron Microscopy
Frontiers in Pharmacology, 2022 Glycine receptors (GlyRs) are pentameric ion channels that mediate fast inhibitory neurotransmission. GlyRs are found in the central nervous system including the spinal cord, brain stem, and cerebellum, as well as in the retina, sperm, macrophages ...
Hongtao Zhu
doaj +1 more source
Real-Life Clinical Experience With Cariprazine: A Systematic Review of Case Studies
Frontiers in Psychiatry, 2022 BackgroundThe hierarchy of evidence coming from evidence-based medicine favors meta-analyses and randomized controlled trials over observational studies and clinical cases.
Réka Csehi +4 more
doaj +1 more source