We studied parameters of specific binding for various ligands of imidazole receptors and alpha2-adrenoceptors on human platelets. Pharmacological activity of compounds was evaluated by their effects on platelet aggregation induced by ADP in low concentrations (0.125-1.5 microM). In contrast to alpha2-adrenoceptor agonist norepinephrine inducing reversible aggregation of cells, selective stimulation of imidazole receptors with moxonidine produced a disaggregation effect. The data suggest that human platelets can be used as an experimental test system for screening and study of molecular mechanisms underlying the influence of new compounds.
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http://dx.doi.org/10.1023/a:1025481303002 | DOI Listing |
Zhong Nan Da Xue Xue Bao Yi Xue Ban
July 2024
Department of Endocrinology &Metabolism, West China Hospital, Sichuan University, Chengdu 610041.
Cushing's disease is a rare endocrine disorder characterized by hypercortisolism. Chronic elevated cortisol levels can lead to dysfunction or complications in multiple organs of systems, including cardiovascular, glucose, and bone metabolism, severely impacting patients' quality of life and posing life-threatening risks. Surgery is the first-line treatment for Cushing's disease.
View Article and Find Full Text PDFBackground: Human pluripotent stem cell (hPSC)-derived brain organoids patterned towards the cerebral cortex are valuable models of interactions occurring in vivo in cortical tissue. We and others have used these cortical organoids to model dominantly inherited FTD-tau. While these studies have provided essential insights, cortical organoid models have yet to reach their full potential.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
BioXcel Therapeutics, New Haven, CT, USA.
Background: BXCL501, a sublingual film formulation of dexmedetomidine, a highly selective α2 adrenoceptor agonist, is currently being studied for the acute treatment of agitation associated with dementia.
Method: This was a Phase 1b/2 study assessing efficacy and tolerability of BXCL501 for treatment of acute agitation associated with dementia. Subjects were randomized to active treatment with BXCL501 (30, 40, or 60µg) or placebo.
Mini Rev Med Chem
January 2025
Department of Chemistry, Kurukshetra University, Kurukshetra, Kurukshetra, 136119, India.
Heterocyclic compounds are increasingly used in medicinal chemistry because they are the main components of many biological processes and materials. Benzimidazole remains the core center of the heterocyclic chemical group, with essential traits such as six-five-member connected rings and two nitrogen atoms at the 1,3 position in a six-membered benzene and five-membered imidazole- fused ring system. Molecules with benzimidazole derivatives serve important functions as therapeutic agents and have shown excellent results in clinical and biological research.
View Article and Find Full Text PDFInflamm Res
January 2025
Medical Faculty and University Hospital, Institute of Neural and Sensory Physiology, Heinrich Heine University Düsseldorf, 40225, Düsseldorf, Germany.
Background: Adenosine, an ATP degradation product, is a sleep pressure factor. The adenosine 1 receptor (A1R) reports sleep need. Histaminergic neurons (HN) of the tuberomamillary nucleus (TMN) fire exclusively during wakefulness and promote arousal.
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