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[3H]BQ-123, a Highly Specific and Reversible Radioligand for the Endothelin ETA Receptor Subtype

[3H]BQ-123, a Highly Specific and Reversible Radioligand for the Endothelin ETA Receptor Subtype

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

Eur J Pharmacol. 1995 Feb 14;274(1-3):1-6.

PMID: 7768260

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP136553816	BQ-123		136553-81-6	Price

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