FR 172357, a new non-peptide antagonist of the kinin B(2) receptor was tested in three isolated vessels, the human umbilical vein, the rabbit jugular vein, and the pig coronary artery, to evaluate its antagonistic activities against bradykinin. FR 172357 displaced to the right the concentration-response curves of bradykinin. The displacements were parallel to the controls without reduction of the maximum effect in the human umbilical vein and in the rabbit jugular vein, but not in the pig coronary artery. Schild plots confirmed that FR 172357 acts as a competitive antagonist in the human umbilical vein (pA(2) 8.65) and in the rabbit jugular vein (pA(2) 9. 07), and as a non-competitive antagonist in the pig coronary artery (pK(B) 10.14). FR 172357 is selective for the kinin B(2) receptor since it does not influence the effects of Lys-des-Arg(9)-bradykinin in the human umbilical vein, in the rabbit aorta, and in the pig renal vein. It is specific because it does not affect the contractions induced by angiotensin II, noradrenaline, 5-hydroxytryptamine, or endothelin-1 in the human umbilical vein. It, however, interacts with the tachykinin NK(1) receptor of the rabbit jugular vein and pig coronary artery. Compared to other bradykinin B(2) receptor antagonists, FR 172357 emerges as a very potent compound, which may represent a choice for experimental (and clinical?) applications.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0014-2999(99)00711-6 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Development of Electrospinning Setup for Vascular Tissue-Engineering Application with Thick-Hierarchical Fiber Alignment.
Tissue Eng Regen Med
January 2025
College of Materials Science and Engineering, Hunan University, Changsha, 410072, People's Republic of China.
Background: Tissue engineering holds promise for vascular repair and regeneration by mimicking the extracellular matrix of blood vessels. However, achieving a functional and thick vascular wall with aligned fiber architecture by electrospinning remains a significant challenge.
Methods: A novel electrospinning setup was developed that utilizes an auxiliary electrode and a spring.
Combined negative pressure wound therapy with new wound dressings to repair a ruptured giant omphalocele in a neonate: a case report and literature review.
BMC Pediatr
January 2025
Department of Neonatology Nursing, West China Second University Hospital, Sichuan University, No. 20, Section 3, South Renmin Road, Chengdu, Sichuan Province, China.
Background: Current treatment of giant omphalocele in newborns is not standardized. The main treatments include one-time repair and staged surgery using synthetic and biologic mesh, or silos. However, surgery can lead to various postoperative complications.
View Article and Find Full Text PDFEvolution of the umbilical cord blood proteome across gestational development.
Sci Rep
January 2025
Department of Pediatrics, Division of Infectious Diseases, Ann & Robert H. Lurie Children's Hospital of Chicago, Northwestern University Feinberg School of Medicine, Chicago, IL, USA.
Neonatal health is dependent on early risk stratification, diagnosis, and timely management of potentially devastating conditions, particularly in the setting of prematurity. Many of these conditions are poorly predicted in real-time by clinical data and current diagnostics. Umbilical cord blood may represent a novel source of molecular signatures that provides a window into the state of the fetus at birth.
View Article and Find Full Text PDFImprovement of measured and perceived disability in overweight patients with Multiple Sclerosis trough different patterns of Mediterranean hypocaloric diet.
Mult Scler Relat Disord
January 2025
Department of Human Neurosciences, Sapienza University of Rome, Rome, Italy. Electronic address:
Objectives: overweight and other cardiovascular risk factors are known contributors to disability accrual in Multiple Sclerosis (MS). We aimed to explore the impact of three hypocaloric dietetic patterns, based on the Mediterranean diet, on cardiovascular risk and clinical status in overweight persons with MS (pwMS).
Material And Methods: overweight pwMS (body mass index-BMI ≥25 kg/m) were prospectively enrolled, randomly allocated to three hypocaloric dietetic plans differing in macronutrients composition (carbohydrates/proteins/lipids: diet A 65 %/15 %/20 %; diet B 35 %/25 %/40 %; diet C 50 %/20 %/30 %) and followed-up for 1 year (6 months of dietetic intervention + 6 months of observation).
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!