Characterization of [125I]-endothelin-1 and [125I]-BQ3020 binding to rat cerebellar endothelin receptors

British Journal of Pharmacology

Volumn 118, Issue 8, 1996, Pages 2126-2130

  Widdowson, P S ^a,b   Kirk, C N P ^a  

^a ASTRAZENECA   (United Kingdom)

^b ROYAL LIVERPOOL UNIVERSITY HOSPITAL   (United Kingdom)

Author keywords

Endothelin receptor subtypes; Rat cerebellum; 125I BQ3020; 125I endothelin 1; 125I PD1 51242

Indexed keywords

4 TERT BUTYL N [6 (2 HYDROXYETHOXY) 5 (3 METHOXYPHENOXY) 4 PYRIMIDINYL]BENZENESULFONAMIDE; 5 DIMETHYLAMINO N (3,4 DIMETHYL 5 ISOXAZOLYL) 1 NAPHTHALENESULFONAMIDE; BOSENTAN; BRAIN RECEPTOR; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); ENDOTHELIN 1; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR; ENDOTHELIN A RECEPTOR ANTAGONIST; ENDOTHELIN B RECEPTOR; ENDOTHELIN B RECEPTOR AGONIST; ENDOTHELIN RECEPTOR; IODINE 125; N (2,6 DIMETHYLPIPERIDINOCARBONYL) 4 METHYLLEUCYL DEXTRO (1 METHOXYCARBONYLTRYPTOPHANYL) DEXTRO NORLEUCINE; N ACETYL 3,3 DIPHENYL DEXTRO ALANYLLEUCYLASPARTYLISOLEUCYLISOLEUCYLTRYPTOPHAN; N ACETYLENDOTHELIN 1 [6-21][11,15 ALANINE]; SARAFOTOXIN S6C; SUCCINYLENDOTHELIN 1 [8-21][9 GLUTAMIC ACID 11,15 ALANINE]; ENDOTHELIN; PEPTIDE FRAGMENT; RADIOACTIVE IODINE;

ANIMAL TISSUE; ARTICLE; BINDING SITE; CEREBELLUM; FEMALE; MALE; NONHUMAN; PRIORITY JOURNAL; RADIOASSAY; RAT; RECEPTOR AFFINITY; RECEPTOR BINDING; ANIMAL; BINDING COMPETITION; DOSE RESPONSE; DRUG EFFECT;

ANIMALS; BINDING, COMPETITIVE; CEREBELLUM; DOSE-RESPONSE RELATIONSHIP, DRUG; ENDOTHELIN-1; ENDOTHELINS; IODINE RADIOISOTOPES; PEPTIDE FRAGMENTS; RATS; RECEPTORS, ENDOTHELIN;

EID: 0029658139     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1476-5381.1996.tb15652.x     Document Type: Article

References (35)

1. ARAI, H., HORI, S., ARAMORI, I., OHKUBO, H. & NAKANISHI, S. (1990). Cloning and expression of a cDNA encoding an endothelin receptor. Nature, 348, 730-732.
2. BAX, W.A. & SAXENA, P.R. (1994). The current endothelin receptor classification: time for reconsideration? Trends Pharmacol. Sci., 15, 379-386.
3. BOUSSO-MITTLER, D., GALRON, R. & SOKOLOVSKY, M. (1991). Endothelin/sarafotoxin receptor heterogeneity: evidence for different glycosylation in receptors from different tissues. Biochem. Biophys. Res. Commun., 178, 921-926.
4. B receptors. FEBS Lett., 334, 210-214.
5. B receptors. Br. J. Pharmacol., 112, 1251-1257.
6. CLOZEL, M., BREU, V., BURRI, K., CASSAL, J-M., FISCLI, W., GREY, GA., HIRTH, G., LOFFLER, B-M., MULLER, M., NEIDHART, W. & RAMUZ, H. (1993). Pathological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature, 365, 759-761.
7. CLOZEL, M., BREU, V., GREY, G.A., KALINA, B., LOFFLER, B-M., BURRI, K., CASSAL, J-M., HIRTH, G., MULLER, M., NEIDHART, W. & RAMUZ, H. (1994). Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J. Pharmacol. Exp. Ther., 270, 228-235.
8. DOUGLAS, S.A., EDWARDS, R.M., ELLIOTT, J.D. & OHLSTEIN, E.H. (1995). In vivo pharmacological characterization of the non-peptide endothelin receptor antagonist SB 209670. Br. J. Pharmacol., 114, 405-413.
9. EMORI, T., HIRATA, Y. & MARUMO, F. (1990). Specific receptors for endothelin-3 in cultured bovine endothelin cells and its mechanism of action. FEBS Lett., 263, 261-264.
10. GULATI, A. & REBELLO, S. (1992). Characteristics of endothelin receptors in the central nervous system of spontaneously hypertensive rats. Neuropharmacology, 31, 243-250.
11. B receptor. Am. J. Physiol., 264, R777-R783.
12. INOUE, A., YANAGISAWA, M., KIMURA, S., KASUYA, Y., MIYAUCHI, T., GOTO, K. & MASAKI, T. (1989). The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc. Natl. Acad. Sci. U.S.A., 86, 2863-2867.
13. ISHIKAWA, K., IHARA, M., NOGUCHI, K., MASE, T., MINO, N., SAEKI, T., FUKURODA, T., OZAKI, S., NAGASE, T., NISHIKIBE, M. & YANO, M. (1994). Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc. Natl Acad. Sci. U.S.A., 91, 4892-4896.
14. 125I]BQ3020. Brain Res., 665, 33-38.
15. C receptor) from Xenopus Laevis dermal melanophores. J. Biol. Chem., 268, 19126-19133.
16. LIN, H.Y., KAJI, E.H., WINKEL, G.K., IVES, H.E. & LODISH, H.F. (1991). Cloning and functional expression of a vascular smooth muscle endothelin 1 receptor. Proc. Natl. Acad. Sci. U.S.A., 88, 3185-3189.
17. MACCUMBER, M.W., ROSS, C.A. & SNYDER, S.H. (1990). Endothelin in brain: receptors, mitogenesis and biosynthesis in glial cells. Proc. Natl. Acad. Sci. U.S.A., 87, 2359-2363.
18. MASAKI, T., VANE, J.R. & VANHOUTE, P.M. (1994). International union of pharmacology nomenclature of endothelin receptors. Pharmacol. Rev., 46, 137-139.
19. NAMBI, P., PULLEN, M. & FEUERSTEIN, G. (1990). Identification of endothelin receptors in various regions of rat brain. (1990). Neuropeptides. 16, 195-199.
20. 125I]IRL-1620, a potent agonist specific for endothelin-B receptors. J. Pharmacol. Exp. Ther., 268, 202-207.
21. 125I]PD151242. Br. J. Pharmacol., 113, 156P.
22. 3H]epibatidine: a novel high affinity ligand at neuronal nicotinic acetylcholine receptors. Br. J. Pharmacol., (in press).
23. B agonistic activity. Biochem. Biophys. Res. Commun., 179, 286-292.
24. SAKURAI, T., YANAGISAWA, M., TAKUWA, Y., MIYAZAKI, H., KIMURA, S., GOTO, K. & MASAKI, T. (1990). Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor. Nature, 348, 732-735.
25. SCHVARTZ, I., ITTOOP, O. & HAZUM. E. (1991). Direct evidence for multiple endothelin receptors. Biochemistry, 30, 5325-5327.
26. SUPPATTAPONE, S., SIMPSON, A.W.M. & ASHLEY, C.C. (1989). Free calcium rise and mitogenesis in glial cells caused by endothelin. Biochem. Biophys. Res. Commun., 3, 1115-1122.
27. TANAKA, T., TSUKUDA, E., NOZAWA, M., OHNO, T., KASE, H., YAMADA, K. & MATSUDA, Y. (1994). RES-701-1, a novel, potent, endothelin type B receptor selective antagonist of microbial origin. Mol. Pharmacol., 45, 724-730.
28. WARNER, T.D., ALLCOCK, G.H., CORDER, R. & VANE, J.R. (1993a). Use of the endothelin antagonists BQ-123 and PD 142893 to reveal three endothelin receptors mediating smooth muscle contraction and release of EDRF. Br. J. Pharmacol., 110, 777-782.
29. WARNER, T.D., ALLCOCK, G.H., MICKLEY, E.J., CORDER, R. & VANE, J.R. (1993b). Comparative studies with the endothelin receptor antagonists BQ-123 and PD142893 indicate at least three endothelin receptors. J. Cardiorasc. Pharmacol., 22, suppl. 8, S117-S120.
30. 125I]endothelin binding in rat cerebellum is increased following L-2-chloropropionic acid-induced granule cell necrosis. Peptides, 16, 897-902.
31. WILLIAMS, D.L., JONES, K.L., PETTIBONE, D.J., LIS, E.V. & CLINESCHMIDT, B.V. (1991). Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes. Biochem. Biophys. Res. Commun., 175, 556-561.
32. YAMAMOTO, T., SHIMOYAMA, N., ASANO, H. & MIZUGUCHI, T. (1994). Analysis of the role of endothelin-A and endothelin-B receptors on nociceptive information transmission in the spinal cord with FR139317. an endothelin-A receptor antagonist and sarafotoxin S6c, an endothclin-B receptor agonist. J. Pharmacol. Exp. Ther., 27, 156-163.
33. YANAGISAWA, M., INOUE, A., ISHIKAWA, T., KASUYA, Y., KIMURA, S., KUMAGAYE, S-L, NAKAJIMA, K., WATANABE, T.X., SAKIBARA, S., GOTO, K. & MASAKI, T. (1988). Primary structure, synthesis and biological activity of rat endothelin, an endothelin-derived vasoconstrictor peptide. Proc. Natl. Acad. Sci. U.S.A., 85, 6964-6967.
34. YANAGISAWA, M. & MASAKI, T. (1989). Molecular biology and biochemistry of the endothelins. Trends Pharmacol. Sci., 10, 374-378.
35. YU, J.C.M., PICKARD, J.D. & DAVENPORT, A.P. (1995). Characterisation of endothelin receptors in cultured human cerebral vascular smooth muscle cells. Br. J. Pharmacol., 114, 195P.