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Titolo:
[H-3] BQ-123, A HIGHLY SPECIFIC AND REVERSIBLE RADIOLIGAND FOR THE ENDOTHELIN ET(A) RECEPTOR SUBTYPE
Autore:
IHARA M; YAMANAKA R; OHWAKI K; OZAKI S; FUKAMI T; ISHIKAWA K; TOWERS P; YANO M;
Indirizzi:
BANYU PHARMACEUT CO LTD,TSUKUBA RES INST,OKUBO 3 TSUKUBA IBARAKI 30033 JAPAN AMERSHAM INT PLC,CARDIFF LABS CARDIFF S GLAM WALES
Titolo Testata:
European journal of pharmacology
fascicolo: 1-3, volume: 274, anno: 1995,
pagine: 1 - 6
SICI:
0014-2999(1995)274:1-3<1:[BAHSA>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
BINDING-SITES; ETA RECEPTOR; ANTAGONIST; POTENT; SELECTIVITY; IRL-1620; TISSUES; AGONIST; CELLS;
Keywords:
ENDOTHELIN; ENDOTHELIN ET(A) RECEPTOR; [H-3] BQ-123;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
25
Recensione:
Indirizzi per estratti:
Citazione:
M. Ihara et al., "[H-3] BQ-123, A HIGHLY SPECIFIC AND REVERSIBLE RADIOLIGAND FOR THE ENDOTHELIN ET(A) RECEPTOR SUBTYPE", European journal of pharmacology, 274(1-3), 1995, pp. 1-6

Abstract

The mode of binding of [H-3]BQ-123 D-Trp-D-Asp-[prolyl-3,4(n)-[H-3]]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 [H-3]BQ-123 binding sites with a high affinity of 3.2 nM. [H-3]BQ-123 bindingachieved steady state within 7 min and dissociated with a half-time of 1.4 min, while [I-125]endothelin-1 binding barely reached a steady state even after 6 h and showed little dissociation. [H-3]BQ-123 binding was sensitive to endothelin-1 and endothelin-2 (K-i values = 0.058 and 0.10 nM, respectively) and the endothelin ET(A) receptor-selective antagonist BQ-123 (K-i = 3.3 nM), while showing low affinity for endothelin-3 (K-i = 50 nM), the endothelin ET(A) receptor-selective agonistBQ-3020 (K-i = 970 nM) and other bioactive peptides. Thus, [H-3]BQ-123 is a specific and reversible radioligand for endothelin ET(A) receptors. The rapid reversibility of [H-3]BQ-123 binding should provide a tool for estimating the equilibrium inhibition constants (K-i values) of various compounds for endothelin ET(A) receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 13:02:53