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Molecular Pharmacology

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Abstract

Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells.

I Aramori, H Nirei, M Shoubo, K Sogabe, K Nakamura, H Kojo, Y Notsu, T Ono and S Nakanishi
Molecular Pharmacology February 1993, 43 (2) 127-131;
I Aramori
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H Nirei
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M Shoubo
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K Sogabe
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K Nakamura
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H Kojo
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Y Notsu
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T Ono
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S Nakanishi
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Abstract

We investigated the receptor-binding properties and the antagonist activities of FR139317, a novel endothelin (ET) antagonist, in transfected Chinese hamster ovary cells permanently expressing the two ET receptor subtypes (ETA and ETB). In displacement analysis using membrane preparations derived from the receptor-expressing cells, FR139317 showed a high affinity for ETA (Ki = 1 nM) and a lower affinity for ETB (Ki = 7.3 microM). FR139317 inhibited ETA-mediated phosphatidylinositol hydrolysis and arachidonic acid release and produced a parallel shift in the dose-response curve for ET-1, with respective pA2 values of 8.2 and 7.7. In contrast, FR139317 had no inhibitory effects on these ET-1-induced responses in ETB-expressing cells. FR139317 itself showed no stimulatory effects on phosphatidylinositol hydrolysis and arachidonic acid release in ETA- and ETB-expressing cells. Thus, FR139317 is a potent, competitive, and highly selective antagonist for ETA. This compound should be a powerful tool for investigation of the physiological properties of ETA and exploration of its role in diseases.

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Molecular Pharmacology
Vol. 43, Issue 2
1 Feb 1993
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Abstract

Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells.

I Aramori, H Nirei, M Shoubo, K Sogabe, K Nakamura, H Kojo, Y Notsu, T Ono and S Nakanishi
Molecular Pharmacology February 1, 1993, 43 (2) 127-131;

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Abstract

Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells.

I Aramori, H Nirei, M Shoubo, K Sogabe, K Nakamura, H Kojo, Y Notsu, T Ono and S Nakanishi
Molecular Pharmacology February 1, 1993, 43 (2) 127-131;
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