A series of guanidine triazinediones were identified as potent PK1 receptor antagonists. A compound in this series inhibited the PK1 invoked prosecretory response in rat ileum tissue.
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[Clinical characteristics and pharmacological treatment of patients with heart failure in a primary health care cohort].
Aten Primaria
January 2025
Fundació Institut Universitari per a la Recerca a l'Atenció Primària de Salut Jordi Gol i Gurina (IDIAPJGol), Barcelona, España; Department of Pharmacology, Therapeutics and Toxicology, Universitat Autònoma de Barcelona, Bellaterra, Cerdanyola del Vallès, Barcelona, España; Institut Català de la Salut, Barcelona, España.
Objective: To characterise patients with heart failure (HF) in Primary Health Care (PHC) and describe their socio-demographic and clinical characteristics and pharmacological treatment.
Design: Descriptive cohort study. SITE: Information System for the Development of Research in Primary Care (SIDIAP), which captures information from the electronic health records of PHC of the Catalan Institute of Health (approximately 80% of the Catalan population).
Effect of Lemborexant on Daytime Functioning in Adults With Insomnia: Patient-Reported Outcomes From a Phase 3 Clinical Trial.
Prim Care Companion CNS Disord
January 2025
Eisai Inc, Nutley, New Jersey.
Insomnia and some insomnia treatments can impact an individual's daytime functioning. Here, we performed post hoc analyses of patient-reported outcomes from a phase 3 clinical trial to assess the impact of lemborexant (LEM), a dual orexin receptor antagonist, on daytime functioning. Adults with insomnia were randomized 1:1:1 to receive placebo, LEM 5 mg (LEM5) or LEM 10 mg (LEM10) for 6 months.
View Article and Find Full Text PDFHuman P2X4 receptor gating is modulated by a stable cytoplasmic cap and a unique allosteric pocket.
Sci Adv
January 2025
Department of Chemical Physiology & Biochemistry, Oregon Health & Science University, Portland, OR 97239, USA.
P2X receptors (P2XRs) are adenosine 5'-triphosphate (ATP)-gated ion channels comprising homomeric and heteromeric trimers of seven subtypes (P2X1-P2X7) that confer different rates of desensitization. The helical recoil model of P2XR desensitization proposes stability of the cytoplasmic cap sets the rate of desensitization, but timing of its formation is unclear for slow-desensitizing P2XRs. We report cryo-electron microscopy structures of full-length wild-type human P2X4 receptor in apo closed, antagonist-bound inhibited, and ATP-bound desensitized states.
View Article and Find Full Text PDFEfficacy and safety of finerenone in patients with chronic kidney disease and type 2 diabetes by diuretic use: A FIDELITY analysis.
Eur J Heart Fail
January 2025
Department of Medicine, University of Chicago Medicine, Chicago, IL, USA.
Aims: This post hoc analysis aimed to assess the efficacy and safety of the non-steroidal mineralocorticoid receptor antagonist finerenone by baseline diuretic use in FIDELITY, a pre-specified pooled analysis of the phase III trials FIDELIO-DKD and FIGARO-DKD.
Methods And Results: Eligible patients with type 2 diabetes (T2D) and chronic kidney disease (CKD; urine albumin-to-creatinine ratio [UACR] ≥30-<300 mg/g and estimated glomerular filtration rate [eGFR] ≥25-≤90 ml/min/1.73 m, or UACR ≥300-≤5000 mg/g and eGFR ≥25 ml/min/1.
PD-L1 as a Biomarker in Gastric Cancer Immunotherapy.
J Gastric Cancer
January 2025
Department of Pathology and Translational Genomics, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, Korea.
Combining chemotherapy with immune checkpoint inhibitors (ICIs) that target the programmed death-1 (PD-1) protein has been shown to be a clinically effective first-line treatment for human epidermal growth factor receptor 2 (HER2)-negative and -positive advanced or metastatic gastric cancer (GC). Currently, PD-1 inhibitors combined with chemotherapy are the standard treatment for patients with HER2-negative/positive locally advanced or metastatic GC. Programmed death-ligand 1 (PD-L1) expression, as assessed using immunohistochemistry (IHC), is a crucial biomarker for predicting response to anti-PD-1/PD-L1 agents in various solid tumors, including GC.
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