Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Griesbacher, T; Legat, FJ.
Effects of the non-peptide B2 receptor antagonist FR173657 in models of visceral and cutaneous inflammation.
Inflamm Res. 2000; 49(10):535-540
Doi: 10.1007/s000110050628
Web of Science
PubMed
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- Führende Autor*innen der Med Uni Graz
- Griesbacher Thomas
- Co-Autor*innen der Med Uni Graz
- Legat Franz
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- Abstract:
- The non-peptide B2 receptor 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 compared to the peptide antagonist icatibant in models of visceral and cutaneous inflammation. Pancreatitis was induced by caerulein in anaesthetized Sprague-Dawley rats. Acute cystitis was induced by intravesical instillation of xylene or i.p. cyclophosphamide injection. Cutaneous inflammation was induced in anaesthetized guinea-pigs by s.c. injection of collagenase from Clostridium histolyticum. FR173657 inhibited oedema formation and tissue enzyme retention during pancreatitis at 500 nmol/kg and above after peroral administration, and from 30 nmol/kg after s.c. injection; icatibant was effective at 3 nmol/kg s. c. Protein extravasation in both cystitis models was abolished by s.c. FR173657 at 300 nmol/kg. Collagenase-induced oedema was attenuated equieffectively by FR173657 and icatibant at doses of 10 micomol/kg and 300 nmol/kg s.c., respectively. FR173657 inhibits kinin-mediated effects in visceral and cutaneous inflammation at doses that are about 10 times higher than those of icatibant. However, FR173657 is also active following oral administration.
- Find related publications in this database (using NLM MeSH Indexing)
- Animals -
- Anti-Inflammatory Agents, Non-Steroidal - therapeutic use
- Blood Proteins - metabolism
- Bradykinin Receptor Antagonists -
- Capillary Permeability - drug effects
- Cystitis - drug therapy
- Dermatitis - drug therapy
- Dose-Response Relationship, Drug -
- Female -
- Guinea Pigs -
- Pancreatitis - drug therapy
- Quinolines - therapeutic use
- Rats -
- Rats, Sprague-Dawley -
- Receptor, Bradykinin B2 -
- Find related publications in this database (Keywords)
- bradykinin antagonists
- FR173657
- pancreatitis
- cystitis
- collagenase