A POTENT AND SPECIFIC AGONIST, SUC-[GLU9,ALA11,15]-ENDOTHELIN-1(8-21), IRL-1620, FOR THE ETB RECEPTOR

A series of C-terminal linear peptides of endothelin (ET)-1 and their N alpha-succinyl (Suc) analogs were synthesized and their binding affinities for the two subtypes of ET receptor, ETA and ETB, in porcine lung membranes were examined. Among the synthetic analogs, Suc-[Glu9,Ala11,15]-ET-1(8-21), I...

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Veröffentlicht in:	Biochemical and biophysical research communications 1992-04, Vol.184 (2), p.953-959
Hauptverfasser:	TAKAI, M, UMEMURA, YAMASAKI, K, WATAKABE, T, FUJITANI, Y, ODA, K, URADE, Y, INUI, T, YAMAMURA, T, OKADA, T
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Animals Binding, Competitive Biochemistry & Molecular Biology Biological and medical sciences Biophysics Blood vessels and receptors Cell Membrane - metabolism Endothelins - chemical synthesis Endothelins - metabolism Endothelins - pharmacology Fundamental and applied biological sciences. Psychology Guinea Pigs In Vitro Techniques Kinetics Life Sciences & Biomedicine Lung - metabolism Male Molecular Sequence Data Muscle Contraction - drug effects Muscle, Smooth - drug effects Muscle, Smooth - physiology Peptide Fragments - chemical synthesis Peptide Fragments - pharmacology Peptides - chemical synthesis Peptides - pharmacology Receptors, Cell Surface - drug effects Receptors, Cell Surface - metabolism Receptors, Endothelin Science & Technology Structure-Activity Relationship Swine Trachea - drug effects Trachea - physiology Vertebrates: cardiovascular system
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Zusammenfassung:	A series of C-terminal linear peptides of endothelin (ET)-1 and their N alpha-succinyl (Suc) analogs were synthesized and their binding affinities for the two subtypes of ET receptor, ETA and ETB, in porcine lung membranes were examined. Among the synthetic analogs, Suc-[Glu9,Ala11,15]-ET-1(8-21), IRL 1620, was the most potent and specific ligand for the ETB receptor (KiETA/KiETB approximately equal to 120,000) as judged by the Ki values for ETA (1.9 microM) and ETB (16 pM) receptors. IRL 1620 was 60 times more selective for the ETB receptor than ET-3 (KiETA/KiETB approximately equal to 1,900). IRL 1620 (10(-9)-10(-7) M) induced contractions of the guinea pig trachea with a comparable potency to those of ET-1 or ET-3, suggesting that IRL 1620 is a potent ETB receptor agonist.
ISSN:	0006-291X 1090-2104
DOI:	10.1016/0006-291X(92)90683-C