CHARACTERIZATION OF ENDOTHELIN-A RECEPTORS IN THE CEREBRAL-CIRCULATION

被引：43

作者：

ADNER, M ^{[1
]}

YOU, JP ^{[1
]}

EDVINSSON, L ^{[1
]}

机构：

[1] UNIV LUND HOSP, DEPT INTERNAL MED, S-22185 LUND, SWEDEN

来源：

NEUROREPORT | 1993年 / 4卷 / 04期

关键词：

ENDOTHELIN-1; ANTAGONIST FR-139317; MIDDLE CEREBRAL ARTERIES; CONTRACTION; PHARMACOLOGY INVITRO;

D O I：

10.1097/00001756-199304000-00026

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

ENDOTHELIN-1 (ET-1), a 21-amino acid peptide produced by the vascular endothelium, mediates contraction. In the present study we demonstrate that both ET-1 (E(max): 238 +/- 29% of potassium contraction) and ET-2 (E((max): 231 +/- 36%) produce strong concentration-dependent contractions of circular segments of guinea-pig middle cerebral artery, whereas ET-3 has only weak effects (E(max): 32 +/- 13%). FR 139317 (10(-6)M), a selective endothelin(A) (ET(A)) receptor antagonist, shifted the ET-1 response curve to the right (pD2:7.86 +/- 0.09 with and 8.76 +/- 0.09 without the antagonist) in a competitive manner (pA2 = 6.83). These findings are the first to show the presence of ET(A) receptors in cerebral vessels.

引用

页码：441 / 443

页数：3

共 13 条

[1] CLONING AND EXPRESSION OF A CDNA-ENCODING AN ENDOTHELIN RECEPTOR [J].

ARAI, H ;

HORI, S ;

ARAMORI, I ;

OHKUBO, H ;

NAKANISHI, S .

NATURE, 1990, 348 (6303) :730-732

[2] 2 FUNCTIONAL ENDOTHELIN RECEPTORS IN GUINEA-PIG PULMONARY-ARTERIES [J].

CARDELL, LO ;

UDDMAN, R ;

EDVINSSON, L .

NEUROCHEMISTRY INTERNATIONAL, 1991, 18 (04) :571-574

[3]

CARDELL LO, 1993, IN PRESS BR J PHARM

[4]

EKELUND U, 1993, IN PRESS ACTA PHYSL

[5] VASOCONSTRICTIVE RESPONSES ELICITED BY ENDOTHELIN IN BOVINE CEREBRAL-ARTERIES [J].

ENCABO, A ;

FERRER, M ;

MARIN, J ;

VILLAMOR, J ;

BALFAGON, G .

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM, 1992, 23 (02) :263-267

[6] MECHANICAL-PROPERTIES OF RAT CEREBRAL-ARTERIES AS STUDIED BY A SENSITIVE DEVICE FOR RECORDING OF MECHANICAL-ACTIVITY IN ISOLATED SMALL BLOOD-VESSELS [J].

HOGESTATT, ED ;

ANDERSSON, KE ;

EDVINSSON, L .

ACTA PHYSIOLOGICA SCANDINAVICA, 1983, 117 (01) :49-61

[7] BIOLOGICAL PROFILES OF HIGHLY POTENT NOVEL ENDOTHELIN ANTAGONISTS SELECTIVE FOR THE ETA RECEPTOR [J].

IHARA, M ;

NOGUCHI, K ;

SAEKI, T ;

FUKURODA, T ;

TSUCHIDA, S ;

KIMURA, S ;

FUKAMI, T ;

ISHIKAWA, K ;

NISHIKIBE, M ;

YANO, M .

LIFE SCIENCES, 1992, 50 (04) :247-255

[8] MECHANISMS OF ACTION OF ENDOTHELIN ON ISOLATED FELINE CEREBRAL-ARTERIES - INVITRO PHARMACOLOGY AND ELECTROPHYSIOLOGY [J].

JANSEN, I ;

FALLGREN, B ;

EDVINSSON, L .

JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM, 1989, 9 (06) :743-747

[9]

MASAOKA H, 1989, LANCET, V2, P1402

[10] CLONING OF A CDNA-ENCODING A NON-ISOPEPTIDE-SELECTIVE SUBTYPE OF THE ENDOTHELIN RECEPTOR [J].

SAKURAI, T ;

YANAGISAWA, M ;

TAKUWA, Y ;

MIYAZAKI, H ;

KIMURA, S ;

GOTO, K ;

MASAKI, T .

NATURE, 1990, 348 (6303) :732-735

← 1 2 →