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Molecular Pharmacology

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Abstract

RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin.

T Tanaka, E Tsukuda, M Nozawa, H Nonaka, T Ohno, H Kase, K Yamada and Y Matsuda
Molecular Pharmacology April 1994, 45 (4) 724-730;
T Tanaka
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E Tsukuda
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M Nozawa
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H Nonaka
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T Ohno
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H Kase
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K Yamada
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Y Matsuda
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Abstract

The unique cyclic peptide designated RES-701-1 blocked the binding of 125I-labeled endothelin (ET)-1 to bovine cerebellar membranes. ETB receptors are predominant in bovine cerebellum. However, in bovine lung membranes, where both ETA and ETB receptors are expressed, RES-701-1 inhibited 125I-ET-1 binding by up to 70%; RES-701-1, in the presence of the ETA-selective antagonist BQ-123 at 1 microM, displaced 125I-ET-1 binding completely. With membranes from transfected Chinese hamster ovary cells expressing the human ETA or ETB receptors, RES-701-1 inhibited 125I-ET-1 binding to the ETB receptor with an IC50 value of 10 nM but had no effect on 125I-ET-1 binding to the ETA receptor. Thus, RES-701-1 is highly specific for the ETB receptor; it has no effect on a number of other receptors. RES-701-1 selectively inhibited the ET-1-induced increase in intracellular Ca2+ concentration in COS-7 cells expressing the ETB receptor but did not inhibit the Ca2+ transient in ETA-expressing cells. When injected intravenously (250 nmol/kg) into anesthetized rats, RES-701-1 abolished the initial depressor response to ET-1 but enhanced the subsequent pressor response. These results suggest that RES-701-1 is a potent and specific antagonist for the ETB receptor and that RES-701-1 will be a powerful tool for understanding the physiological roles of this receptor.

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Molecular Pharmacology
Vol. 45, Issue 4
1 Apr 1994
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Abstract

RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin.

T Tanaka, E Tsukuda, M Nozawa, H Nonaka, T Ohno, H Kase, K Yamada and Y Matsuda
Molecular Pharmacology April 1, 1994, 45 (4) 724-730;

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Abstract

RES-701-1, a novel, potent, endothelin type B receptor-selective antagonist of microbial origin.

T Tanaka, E Tsukuda, M Nozawa, H Nonaka, T Ohno, H Kase, K Yamada and Y Matsuda
Molecular Pharmacology April 1, 1994, 45 (4) 724-730;
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