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Inhibition of prejunctional parasympathetic pathways by β-adrenoceptor agonists in the isolated pig detrusor: comparison with human detrusor studies.
Front Pharmacol
May 2023
Department of Drug Sciences, University of Pavia, Pavia, Italy.
Adrenergic receptors of the β-subtype (β-ADRs) seem to represent a new target for a more effective pharmacological treatment of overactive bladder (OAB), a wide spread urinary disorder. A promising opportunity for OAB therapy might rely on the development of selective β-ADR agonists, but an appropriate preclinical screening, as well as investigation of their pharmacological mechanism(s), is limited by poor availability of human bladder samples and of translational animal models. In this study, we used the porcine urinary bladder as experimental tool to ascertain the functions of β-ADRs in the control the parasympathetic motor drive.
View Article and Find Full Text PDFEffects of Dexamethasone on DNA Synthesis in Lens Epithelial Cells Are Dependent on Cell Type and Growth Factor.
Curr Eye Res
July 2022
Center Department of Ophthalmology and Visual Sciences, Texas Tech University Health Sciences, Lubbock, Texas, USA.
Purpose: To determine the factors that influence the ability of dexamethasone (dex) to inhibit or stimulate the growth of lens epithelial cells.
Method: Different growth factors with or without dex (10 M) were added to quiescent cultures of two clones of Nakano mouse lens epithelial cells (NK11) in serum-free medium. DNA synthesis was then measured after 8-12 hours by the incorporation of tritiated thymidine.
Neuronal networks cause changes in behaviorally important information processing through the vesicular release of neurotransmitters governed by the rate and timing of action potentials (APs). Herein, we provide evidence that dopamine (DA), nonquantally released from the cytoplasm, may exert similar effects in vivo. In mouse slice preparations, (+/-)-3,4-methylenedioxy-methamphetamine (MDMA, or ecstasy) and β-phenylethylamine (β-PEA)-induced DA release in the striatum and nucleus accumbens (NAc), two regions of the brain involved in reward-driven and social behavior and inhibited the axonal stimulation-induced release of tritiated acetylcholine ([ H]ACh) in the striatum.
View Article and Find Full Text PDFSynthesis, Pharmacological, and Biological Evaluation of 2-Furoyl-Based MIF-1 Peptidomimetics and the Development of a General-Purpose Model for Allosteric Modulators (ALLOPTML).
ACS Chem Neurosci
January 2021
Dept. of Organic Chemistry II, University of Basque Country (UPV-EHU), 48940 Leioa, Spain.
This work describes the synthesis and pharmacological evaluation of 2-furoyl-based Melanostatin (MIF-1) peptidomimetics as dopamine D modulating agents. Eight novel peptidomimetics were tested for their ability to enhance the maximal effect of tritiated -propylapomorphine ([H]-NPA) at D receptors (DR). In this series, 2-furoyl-l-leucylglycinamide () produced a statistically significant increase in the maximal [H]-NPA response at 10 pM (11 ± 1%), comparable to the effect of MIF-1 (18 ± 9%) at the same concentration.
View Article and Find Full Text PDFDetermination of binding affinity of molecular imaging agents for steroid hormone receptors in breast cancer.
Am J Nucl Med Mol Imaging
April 2018
Department of Radiology, University of Wisconsin School of Medicine and Public Health 600 Highland Avenue, Madison, WI 53792, USA.
Article Synopsis
- The study investigates two imaging biomarkers, [F]FES and [F]FFNP, for assessing breast cancer through quantitative PET, focusing on their binding parameters to estrogen and progesterone receptors.
- Researchers used breast cancer cell lines to measure binding parameters like the equilibrium dissociation constant (K) and total receptor density (B) through specialized binding assays.
- Results showed strong linear correlations between cell number and tracer uptake, confirming that [F]FES and [F]FFNP effectively quantify receptor binding affinity, validating their use over traditional radioligands in cell-based studies.
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