Results 1 to 10 of about 205,233 (331)

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, Julio C. Medina, Donald R. Gehlert, Neil Schwartz   +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, Vineetha Vasukuttan, Danni Harris, Lucas Laudermilk, Jennifer Lucitti, Scott Runyon, Rangan Maitra   +6 more
doaj   +2 more sources

Characterization of three vasopressin receptor 2 variants: an apparent polymorphism (V266A) and two loss-of-function mutations (R181C and M311V). [PDF]

, 2013
Arginine vasopressin (AVP) is released from the posterior pituitary and controls water homeostasis. AVP binding to vasopressin V2 receptors (V2Rs) located on kidney collecting duct epithelial cells triggers activation of Gs proteins, leading to increased
Armstrong, Stephen P, Ayoub, Mohammed Akli, Feldman, Brian J, Pfleger, Kevin DG, Seeber, Ruth M   +4 more
core   +13 more sources

(±)VK4-40, a novel dopamine D₃ receptor partial agonist, attenuates cocaine reward and relapse in rodents. [PDF]

Br J Pharmacol, 2020
Jordan CJ, He Y, Bi GH, You ZB, Cao J, Xi ZX, Newman AH.   +6 more
europepmc   +3 more sources

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, Zsófia Borbála Dombi, Zsófia Borbála Dombi, Barbara Sebe, Mária Judit Molnár   +4 more
doaj   +1 more source

Case Report: Functional and Symptomatic Improvement With Cariprazine in Various Psychiatric Patients: A Case Series

Frontiers in Psychiatry, 2022
Cariprazine is a third-generation antipsychotic medication approved for the treatment of schizophrenia and bipolar disorder, with unique pharmacodynamic and pharmacokinetic properties.
Tommaso Vannucchi, Costanza Taddeucci, Lorenzo Tatini   +2 more
doaj   +1 more source

Partial agonist antipsychotic drugs differentially interact with a secondary binding site at the dopamine D2 receptor. [PDF]

Int J Neuropsychopharmacol
Ågren R, Sahlholm K.
europepmc   +2 more sources

Design of κ-Opioid Receptor Agonists for the Development of Potential Treatments of Pain with Reduced Side Effects

Molecules, 2023
The κ-opioid receptor (KOR) has recently emerged as an alternative therapeutic target for the development of pain medications, without deleterious side effects associated with the μ-opioid receptor (MOR).
Federica Santino, Luca Gentilucci
doaj   +1 more source

Quantal Ca2+ release mediated by very few IP3 receptors that rapidly inactivate allows graded responses to IP3

Cell Reports, 2021
Summary: Inositol 1,4,5-trisphosphate receptors (IP3Rs) are intracellular Ca2+ channels that link extracellular stimuli to Ca2+ signals. Ca2+ release from intracellular stores is “quantal”: low IP3 concentrations rapidly release a fraction of the stores.
Ana M. Rossi, Andrew M. Riley, Geneviève Dupont, Taufiq Rahman, Barry V.L. Potter, Colin W. Taylor   +5 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