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[3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype.

Abstract：

:The mode of binding of [3H]BQ-123 (cyclo(-D-Trp-D-Asp-[prolyl-3,4 (n)-[3H]]Pro-D-Val-Leu)), an endothelin receptor antagonist radioligand, was evaluated in the human neuroblastoma cell line SK-N-MC at 37 degrees C. Scatchard analysis indicated the presence of a single class of [3H]BQ-123 binding sites with a high affinity of 3.2 nM. [3H]BQ-123 binding achieved steady state within 7 min and dissociated with a half-time of 1.4 min, while [125I] endothelin-1 binding barely reached a steady state even after 6 h and showed little dissociation. [3H]BQ-123 binding was sensitive to endothelin-1 and endothelin-2 (Ki values = 0.058 and 0.10 nM, respectively) and the endothelin ETA receptor-selective antagonist BQ-123 (Ki = 3.3 nM), while showing low affinity for endothelin-3 (Ki = 50 nM), the endothelin ETB receptor-selective agonist BQ-3020 (Ki = 970 nM) and other bioactive peptides. Thus, [3H]BQ-123 is a specific and reversible radioligand for endothelin ETA receptors. The rapid reversibility of [3H]BQ-123 binding should provide a tool for estimating the equilibrium inhibition constants (Ki values) of various compounds for endothelin ETA receptors.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Ihara M,Yamanaka R,Ohwaki K,Ozaki S,Fukami T,Ishikawa K,Towers P,Yano M

doi

10.1016/0014-2999(94)00670-3

subject

Has Abstract

pub_date

1995-02-14 00:00:00

pages

1-6

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(94)00670-3

journal_volume

274

pub_type

杂志文章

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