An endothelin receptor (ETA) antagonist isolated from Streptomyces misakiensis
| Autor: | Toshihiko Saeki, Katsuhisa Kojiri, Masaru Nishikibe, Takahiro Fukuroda, Masaki Ihara, Hiroyuki Suda, Mitsuo Yano |
|---|---|
| Rok vydání: | 1991 |
| Předmět: |
medicine.medical_specialty
Swine Vasodilator Agents Biophysics Blood Pressure Receptors Cell Surface Peptide hormone Biology In Vitro Techniques Biochemistry Iliac Artery Peptides Cyclic Rats Inbred WKY Muscle Smooth Vascular chemistry.chemical_compound Internal medicine medicine Animals Receptor Molecular Biology Aorta Cells Cultured BQ-123 Kidney Receptors Endothelin Endothelins Antagonist Cell Biology Streptomyces misakiensis Streptomyces Rats Kinetics Endocrinology medicine.anatomical_structure chemistry Organ Specificity Vasoconstriction Rabbits medicine.symptom Endothelin receptor |
| Zdroj: | Biochemical and biophysical research communications. 178(1) |
| ISSN: | 0006-291X |
| Popis: | A competitive endothelin (ET) antagonist, BE-18257B, was isolated from the fermentation products of Streptomyces misakiensis. It is a novel cyclic pentapeptide, cyclo(-D-Glu-L-Ala-allo-D-Ile-L-Leu-D-Trp-), and binds to ETA receptors (ET-1 selective) in cardiovascular tissues, but not to ETB receptors (equally sensitive to isopeptides of ET family) in kidney, adrenal gland and cerebellum tissues. BE-18257B also antagonizes ET-1-induced vasoconstriction in rabbit iliac artery and pressor action in rats. Thus it is a selective ETA antagonist and should provide a valuable tool for elucidation of the pharmacological and pathophysiological roles of ET-1. |
| Databáze: | OpenAIRE |
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