Effects of the non-peptide B2 antagonist FR173657 on kinin-induced smooth muscle contraction and relaxation, vasoconstriction and prostaglandin release

British Journal of Pharmacology
T GriesbacherH Juan

Abstract

1. The non-peptide bradykinin (BK) antagonist (E)-3-(6-acetamido-3-pyridyl)-N-[N-[2,4-dichloro-3-[(2-methyl-8-quinolin yl) oxymethyl]phenyl]-N-methylaminocarbonylmethyl]acrylamide (FR173657) was tested in intestinal, uterine, tracheal and vascular in vitro preparations. The investigation aimed at determining the antagonistic potency, duration of action, specificity for BK receptors and apparent mode of antagonistic action of FR173657. 2. Contractions of the isolated ileum of the guinea-pig in response to BK were inhibited by FR173657 (10-300 nM) in a concentration-dependent manner. The inhibition lasted for up to 90 min after wash-out of FR173657. Cumulative concentration-response curves to BK were shifted to the right with a concomitant decrease in the maximum effect. A pKB value of 8.7 was determined. FR173657 had no effect on contractions induced by acetylcholine, histamine, 5-hydroxytryptamine, substance P, angiotensin II or caerulein. 3. The concentration-response curves for B2 receptor-mediated relaxations of the rat isolated duodenum induced by BK were shifted to the right together with a concomitant reduction of the maximum BK effect in the presence of FR173657 (10-300 nM). A pKB of 9.0 +/- 0.2 was calculated. FR173657 ...Continue Reading

References

Jan 1, 1978·General Pharmacology·H Juan
Jul 1, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·T Griesbacher
Nov 1, 1992·Pharmacology & Therapeutics·J M Hall
Mar 1, 1991·British Journal of Pharmacology·F J HockJ Knolle
Mar 1, 1991·British Journal of Pharmacology·K WirthJ Knolle
Feb 18, 1992·European Journal of Pharmacology·T Griesbacher, F Lembeck
Feb 1, 1991·British Journal of Pharmacology·F LembeckJ Knolle
Jan 1, 1986·Advances in Experimental Medicine and Biology·J M Stewart, R J Vavrek
Nov 1, 1983·Naunyn-Schmiedeberg's Archives of Pharmacology·H Juan, W Sametz
Aug 1, 1995·British Journal of Pharmacology·D ScherrerJ P Gies
Dec 1, 1993·Trends in Pharmacological Sciences·T Kenakin
May 24, 1994·Proceedings of the National Academy of Sciences of the United States of America·D G SawutzM M Awad
Aug 1, 1993·Canadian Journal of Physiology and Pharmacology·D RegoliN E Rhaleb
Aug 20, 1993·Journal of Medicinal Chemistry·J M SalvinoD G Sawutz
Oct 1, 1995·British Journal of Pharmacology·D PruneauP Bélichard
Jul 1, 1995·Canadian Journal of Physiology and Pharmacology·K J WirthB A Schölkens
Jun 1, 1997·Canadian Journal of Physiology and Pharmacology·N InamuraK Nakahara
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

❮ Previous
Next ❯

Citations

Dec 25, 2002·European Journal of Pharmacology·Mariem El Sayah, João B Calixto
Jan 9, 1999·European Journal of Pharmacology·T S SalehJ B Calixto
Aug 11, 2001·British Journal of Pharmacology·I HayashiM Majima
Mar 29, 2016·Annals of Medicine·Sacha Zeerleder, Marcel Levi
Jun 18, 2003·Critical Reviews in Toxicology·Edward J Calabrese, Linda A Baldwin
May 31, 2001·Clinical and Experimental Pharmacology & Physiology·K R Bentley, B Jarrott
Jan 19, 2019·Research and Practice in Thrombosis and Haemostasis·Marcel LeviSacha Zeerleder
May 19, 2009·European Journal of Pharmacology·Stefania MeiniCarlo Alberto Maggi

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.