Results 11 to 20 of about 205,233 (331)

Reducing Addiction in Bipolar Disorder via Hacking the Dopaminergic System

open access: yesFrontiers 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

open access: yesCells, 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

Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine

open access: yesBiomolecules, 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

RGS4 regulates partial agonism of the M2 muscarinic receptor-activated K+ currents. [PDF]

open access: yes, 2014
Partial agonists are used clinically to avoid overstimulation of receptor-mediated signalling, as they produce a submaximal response even at 100% receptor occupancy.
Chen, I-Shan   +3 more
core   +2 more sources

Development of Diphenethylamines as Selective Kappa Opioid Receptor Ligands and Their Pharmacological Activities

open access: yesMolecules, 2020
Among the opioid receptors, the kappa opioid receptor (KOR) has been gaining substantial attention as a promising molecular target for the treatment of numerous human disorders, including pain, pruritus, affective disorders (i.e., depression and anxiety),
Helmut Schmidhammer   +3 more
doaj   +1 more source

Successful high dose antipsychotic treatment with cariprazine in patients on the schizophrenia spectrum: Real-world evidence from a Spanish hospital setting

open access: yesFrontiers 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

Functional Stoichiometry at the Nicotinic Receptor. The Photon Cross Section for Phase 1 Corresponds to Two Bis-Q Molecules per Channel [PDF]

open access: yes, 1982
These experiments examine changes in the agonist-induced conductance that occur when the agonist-receptor complex is perturbed. Voltage-clamped Electrophorus electroplaques are exposed to the photoisomerizable agonist trans-Bis-Q A 1-µs laser flash ...
Lester, Henry A., Sheridan, Robert E.
core   +1 more source

Novel 2-amino-isoflavones exhibit aryl hydrocarbon receptor agonist or antagonist activity in a species/cell-specific context [PDF]

open access: yes, 2012
The aryl hydrocarbon receptor (AhR) mediates the induction of a variety of xenobiotic metabolism genes. Activation of the AhR occurs through binding to a group of structurally diverse compounds, most notably dioxins, which are exogenous ligands ...
BALBONI, GIANFRANCO   +10 more
core   +1 more source

Prolongation of hyperprolactinemia by clozapine: a case report

open access: yesPsychiatry and Clinical Psychopharmacology, 2021
Dopamine antagonism by antipsychotic drugs in the mesolimbic pathway leads to their therapeutic effect, while their D2 receptor antagonism in the tuberoinfindibular pathway causes hyperprolactinemia.
Esra Yancar Demir, Aslihan Sayin
doaj   +1 more source

Cyclic nucleotide-gated channels: structural basis of ligand efficacy and allosteric modulation [PDF]

open access: yes, 1997
Most working proteins, including metabolic enzymes, transcription regulators, and membrane receptors, transporters, and ion channels, share the property of allosteric coupling. The term 'allosteric' means that these proteins mediate indirect interactions
Lester, Henry A.   +2 more
core   +1 more source

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