ArticleProceedings of the National Academy of Sciences of the United States of America1994
The nonpeptide WIN 64338 is a bradykinin B2 receptor antagonist.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
14 citing papers in PubMed, 89 citations in OpenAlex.
- Molecular mechanisms for subtype selectivity of kinin receptors' antagonists.Nature communications · 2026Article
- Function and structure of bradykinin receptor 2 for drug discovery.Acta pharmacologica Sinica · 2023Review
- Transcriptomics-Based Phenotypic Screening Supports Drug Discovery in Human Glioblastoma Cells.Cancers · 2021Article
- Exploiting Knowledge on Structure-Activity Relationships for Designing Peptidomimetics of Endogenous Peptides.Biomedicines · 2021Review
- A Robust Bioassay of the Human Bradykinin BPharmaceuticals (Basel, Switzerland) · 2021Review
- New insights into the stereochemical requirements of the bradykinin B2 receptor antagonists binding.Journal of computer-aided molecular design · 2016Article
- Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.British journal of pharmacology · 2000Article
- Pharmacological characterization of the bradykinin B2 receptor: inter-species variability and dissociation between binding and functional responses.British journal of pharmacology · 1999Article
- Kinin receptors.Clinical reviews in allergy & immunology · 1998Review
- Characterization of the bradykinin receptor in the human nasal airway using the binding of [125I]-Hoe 140.British journal of pharmacology · 1996Article
- Rationally designed non-peptides: variously substituted piperazine libraries for the discovery of bradykinin antagonists and other G-protein-coupled receptor ligands.Molecular diversity · 1996Article
- Antinociceptive profile of the pseudopeptide B2 bradykinin receptor antagonist NPC 18688 in mice.British journal of pharmacology · 1996Article
- Inhibition of bradykinin-evoked trigeminal nerve stimulation by the non-peptide bradykinin B2 receptor antagonist WIN 64338 in vivo and in vitro.British journal of pharmacology · 1995Article
- Pharmacological evidence for a single bradykinin B2 receptor in the guinea-pig.British journal of pharmacology · 1995Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We report the synthesis and in vitro biological activity of the nonpeptide bradykinin receptor antagonist WIN 64338, [[4-[[2-[[bis(cyclohexylamino)methylene]amino]-3-(2- naphthyl)-1-oxopropyl]amino]phenyl]methyl]tributylphosphonium chloride monohydrochloride. WIN 64338 inhibits [3H]-bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a binding inhibition constant (Ki) of 64 +/- 8 nM and demonstrates competitive inhibition of bradykinin-stimulated 45Ca2+ efflux from IMR-90 cells (pA2 = 7.1). The antagonist inhibits bradykinin-mediated guinea pig ileum contractility (pA2 = 8.2) and has significantly weaker activity against acetylcholine-induced contractility in the same preparation. WIN 64338 is not active in a rabbit aorta bradykinin B1 receptor assay, demonstrating that it is a selective bradykinin B2 receptor antagonist. The compound inhibits [3H]quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki = 350 nM) but is 25- to 100-fold more selective for the bradykinin receptor compared with other receptors against which it has been tested. Synthesis of WIN 64338 has provided a nonpeptide competitive bradykinin B2 antagonist active in both bradykinin radioligand binding and functional assays.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.