AI Article Synopsis
- A new class of selective coronary vasodilators was developed using [(2-aminoheterocycloethoxy)methyl]dihydropyridines.
- The study revealed that both five- and six-membered heterocycles were effective when incorporated at the 2-position of the dihydropyridine ring, with their potency not relying on basicity.
- The structure-activity relationship (SAR) indicated optimal efficacy when a larger ester group was attached to the 3-position rather than the 5-position, highlighting UK-52,831 (IC50 = 6.3 X 10(-9) M) as a notable calcium channel blocker with prolonged action.
Article Abstract
A series of [(2-aminoheterocycloethoxy)methyl]dihydropyridines were prepared as selective coronary vasodilators. Results showed that a wide variety of five- and six-membered heterocycles were acceptable at the 2-position of the dihydropyridine ring and in vitro potency and tissue selectivity was independent of the basicity of these heterocycles. The SAR indicated that activity was optimum when the largest ester group was placed at the 3 rather than 5 position. 2-[[2-[(3-Amino-1H-1,2,4-triazol-5-yl)amino]ethoxy]methyl]-4- (2,3-dichlorophenyl)-3-(ethoxycarbonyl)-5-(methoxycarbonyl)-6-methyl- 1,4-dihydropyridine (3b) (UK-52,831) emerged as a potent (IC50 = 6.3 X 10(-9) M) and tissue-selective calcium channel blocker with a duration of action greater than 7 h in the anaesthetized dog.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm00123a009 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
At least four groups of kratom consumers in the United States: latent-class analysis of motivations for kratom use.
Am J Drug Alcohol Abuse
January 2025
Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA.
Kratom is a plant with alkaloids acting at opioid, serotonergic, adrenergic, and other receptors. Consumers report numerous use motivations. To distinguish subgroups of kratom consumers by kratom-use motivations using latent-class analysis.
View Article and Find Full Text PDFWillingness to Use Long-Acting Injectable Pre-Exposure Prophylaxis among Adolescent Girls and Young Women in Kampala, Uganda.
AIDS Behav
January 2025
Medical Research Council/Uganda Virus Research Institute and London School of Hygiene and Tropical Medicine (MRC/UVRI & LSHTM) Uganda Research Unit, Kampala, Uganda.
Pre-exposure prophylaxis (PrEP) has proven to be a powerful tool in preventing HIV infection. There is limited information about the factors associated with willingness to use different PrEP modalities among adolescent girls and young women (AGYW) in Africa. We assessed willingness to use long-acting injectable PrEP (LAI-PrEP) among 14-24-year-old AGYW at high risk of HIV in Uganda, and associated factors determined using multivariable complementary log-log regression.
View Article and Find Full Text PDFRecurrence of skin and soft tissue infections: identifying risk factors and treatment strategies.
Curr Opin Infect Dis
January 2025
Department of Medical and Surgical Sciences, Alma Mater Studiorum University of Bologna.
Purpose Of Review: Recurrent skin and soft tissue infections (RSSTIs) are challenging for the clinicians due to morbidity and healthcare-related costs. Here, we review updates on risk factors and management.
Recent Findings: RSSTIs rates range between 7 and 45%.
Role of Long-Acting Porcine Sequence ACTH (Acton Prolongatum) Stimulated Cortisol in Assessing Glucocorticoid Status in COVID-19 Patients.
Indian J Endocrinol Metab
December 2024
Department of Endocrinology, Gandhi Medical College, Musheerabad, Secunderabad, Telangana, India.
Introduction: Conflicting research on cortisol levels and COVID-19 mortality prompted this study to comprehensively assess glucocorticoid status, its links to severity and outcomes, and the role of Acton prolongatum-stimulated cortisol.
Methods: This is a prospective observational study, conducted in 100 RT-PCR-positive COVID-19 patients of mild, moderate, and severe grades from June 2021 to May 2023. Random cortisol, plasma ACTH, and action prolongatum stimulated cortisol were measured, categorized, and analyzed.
Trends in Formulary Restrictions for Long-Acting Injectable Antipsychotic Medications Among Medicare Drug Plans, 2019-2023.
Psychiatr Serv
January 2025
Department of Psychiatry and Behavioral Neuroscience (Bunting, Gray), Department of Pharmacy (Gray), and Pritzker School of Medicine (Chalmers), University of Chicago, Chicago; Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, Atlanta (Cotes); Department of Psychiatry, University of Washington, Seattle (Chalmers); Department of Health Management and Policy, School of Public Health, University of Michigan, Ann Arbor (Nguyen).
Objective: Long-acting injectable antipsychotics (LAIAPs) enable safe and effective long-term management of chronic psychotic disorders but are underused in clinical practice. The authors examined whether Medicare formulary restrictions (prior authorization [PA] or step therapy) impose barriers to LAIAP uptake.
Methods: The authors analyzed formulary restrictions and patient cost-sharing for several LAIAPs and estimated the percentage of plans (N=2,494 were available per year) applying formulary restrictions.
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!