Several, if not all adrenergic β-blockers (β-Bs), accumulate progressively inside secretory vesicles in a time- and concentration-dependent manner, and could be considered to be false neurotransmitters. This transmitter effect is most likely unrelated to their ability to block adrenergic receptors, but it could explain the delay in lowering arterial pressure in hypertensive patients. We have developed a new drug to monitor the accumulation of β-Bs inside living cells, RCTM-3, which fluoresces in the visible spectrum. Here we describe the procedure to synthesize this new compound, as well as its fluorescent properties, pharmacological profile and its accumulation inside the secretory vesicles of PC12 cells.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4055874 | PMC |
| http://dx.doi.org/10.3390/ph4050713 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Characterization of atypical BAR domain-containing proteins coded by Toxoplasma gondii.
J Biol Chem
December 2024
Université Côte d'Azur, CNRS, INSERM, Institut de Pharmacologie Moléculaire et Cellulaire, Valbonne, France. Electronic address:
Article Synopsis
- * The study identifies and characterizes TgREMIND and TgBAR2, two proteins with BAR domains that play key roles in the creation of essential organelles and vesicular trafficking in the parasite.
- * TgREMIND can bind to and remodel membranes, while TgBAR2 uniquely deforms anionic membranes, highlighting their differing roles in the parasite's membrane dynamics and trafficking system.
The spatial impact of a Western diet in enriching Galectin-1-regulated Rho, ECM, and SASP signaling in a novel MASH-HCC mouse model.
Biomark Res
October 2024
Department of Medical Pathology and Laboratory Medicine, University of California, Davis, Room 3400B, Research Building III, 4645 2nd Ave, Sacramento, CA, 95817, USA.
Background: Hepatocellular carcinoma (HCC) arising from metabolic dysfunction-associated steatohepatitis (MASH) presents a significant clinical challenge, particularly given the prevalence of the Western diet (WD). The influence of diet on the tumor microenvironment remains poorly understood. Galectin-1 (Gal-1) is a biomarker for HCC and has a crucial role in liver carcinogenesis.
View Article and Find Full Text PDFA transporter's doom or destiny: in health and disease, novel molecular targets and emerging therapeutic prospects.
Front Mol Neurosci
August 2024
Institute of Pharmacology, Medical University of Vienna, Vienna, Austria.
As the first member of the solute carrier 6 (SLC6) protein family, the γ-aminobutyric acid (GABA) transporter 1 (GAT1, ), plays a pivotal role in the uptake of GABA from the synaptic cleft into neurons and astrocytes. This process facilitates the subsequent storage of GABA in presynaptic vesicles. The human gene is highly susceptible to missense mutations, leading to severe clinical outcomes, such as epilepsy, in the afflicted patients.
View Article and Find Full Text PDFMicrosporidia secretory effectors and their roles in pathogenesis.
J Eukaryot Microbiol
November 2024
State Key Laboratory of Resource Insects, Southwest University, Chongqing, China.
Microsporidia, a group of unicellular eukaryotic parasites, rely intensely on secretory effectors for successful invasion and proliferation within host cells. This review focuses on the identification, characterization, and functional roles of effectors, including secretory proteins and microRNAs. The adhesion proteins like the Ricin-B-lectin facilitate initial invasion, which binds to the host cell surface.
View Article and Find Full Text PDFGeneration of epithelial-stromal assembloids as an advanced in vitro model of impaired adenomyosis-related endometrial receptivity.
Fertil Steril
August 2024
Gynecology Research Unit, Institute of Experimental and Clinical Research, Université Catholique de Louvain, Brussels, Belgium; Gynecology Department, Cliniques Universitaires Saint-Luc, Brussels, Belgium. Electronic address:
Objective: To create a novel, more advanced in vitro model of human endometrium, using so-called assembloids, looking to explore endometrial receptivity in adenomyosis.
Design: Evaluation of assembloid responsiveness to hormonal stimulation by immunohistochemistry, enzyme-linked immunosorbent assay, and scanning electron microscopy.
Setting: University-based research unit in gynecology.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!