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PMID: 8564254 Published · ppublish English Journal Article

Haemodynamic effects of losartan and the endothelin antagonist, SB 209670, in conscious, transgenic ((mRen-2)27), hypertensive rats.

British journal of pharmacology ·Vol. 116 ·No. 4 ·1995-10-00 ·Pages 2237-44

Gardiner SM, March JE, Kemp PA, Mullins JJ, Bennett T

Abstract

1. Hypertensive transgenic (TGR(mRen-2)27) (abbreviated to TG) rats (n = 6) and their normotensive Sprague-Dawley (SD) control strain (n = 7) were chronically instrumented for the measurement of cardiac haemodynamics. The hypertension in TG rats (mean blood pressure 181 +/- 9 mmHg) was entirely attributable to a reduction in total peripheral conductance (TG rats = 169 +/- 7, SD rats = 292 +/- 15 microliters min-1 mmHg-1 100g-1) since cardiac index was not different in the two strains (TG rats = 30.5 +/- 1.2, SD rats = 29.5 +/- 1.6 ml min-1 100g-1). 2. In other animals instrumented for the assessment of regional haemodynamics, the extent of peripheral vasoconstriction was similar in renal, mesenteric and hindquarters vascular beds in the TG rats (reduction in vascular conductance relative to SD rats = 42%, 46% and 49%, respectively). 3. During an 8 h observation period with saline infusion, or following injection of losartan (10 mg kg-1) in SD rats there was no hypotension or regional vasodilation. With infusion of the endothelin antagonist, SB 209670 (10 micrograms kg-1 min-1), there was a slight hypotension, but no significant vasodilation; co-administration of losartan and SB 209670 caused a similar profile of effect, although the hypotension was increased. 4. With the same experimental protocol in TG rats, losartan caused a biphasic, progressive fall in mean arterial blood pressure accompanied by renal, mesenteric and hindquarters vasodilation. Although the response to SB 209670 was not biphasic, its hypotensive and vasodilator effects were not different from those of losartan after 8 h. In the combined presence of losartan and SB 209670, mean arterial blood pressure (116 +/- 5 mmHg) was significantly lower than with SB 209670 (132+/-4 mmHg) or losartan(136 +/- 6 mmHg) alone, and renal, mesenteric and hindquarters vascular conductances (61 +/- 3, 90+/-14 and 52+/-4 [kHz nmHg-1]103, respectively) were higher than the corresponding values following either SB 209670 (49 +/- 4, 52 +/- 4 and 34 +/- 3 [kHz mmHg- 1]103, respectively) or losartan (43 +/- 5, 59 +/- 13 and 35+/-4 [kHz mmHg-1]103, respectively) alone. These results indicate the maintenance of hypertension inTG rats is dependent upon renal, mesenteric and hindquarters vasoconstriction, mediated by angiotensinII (AII) and endothelin (ET). Since we found that plasma ET-1 levels in TG rats (12.06+/-2.87 pmol 1-1)were lower than in SD rats (21.53 +/- 3.94 pmol 1-1), then it is possible that locally-generated, rather than circulating ET-l contributes to the widespread vasoconstriction in TG rats.

MeSH Terms
Angiotensin II/metabolism Angiotensin Receptor Antagonists Angiotensin-Converting Enzyme Inhibitors/pharmacology Animals Animals, Genetically Modified Antihypertensive Agents/pharmacology Biphenyl Compounds/pharmacology Endothelin Receptor Antagonists Endothelins/antagonists & inhibitors,metabolism Hemodynamics/drug effects Hypertension/genetics,physiopathology Imidazoles/pharmacology Indans/pharmacology Losartan Male Rats Rats, Sprague-Dawley Receptors, Endothelin/drug effects Regional Blood Flow/drug effects Tetrazoles/pharmacology
Chemicals
Angiotensin Receptor Antagonists Angiotensin-Converting Enzyme Inhibitors Antihypertensive Agents Biphenyl Compounds Endothelin Receptor Antagonists Endothelins Imidazoles Indans Receptors, Endothelin Tetrazoles 1H-Indene-2-carboxylic acid, 1-(1,3-benzodioxol-5-yl)-3-(2- (carboxymethoxy)-4-methoxyphenyl)-2,3-dihydro-5-propoxy-, (1S,2R,3S)- Angiotensin II Losartan
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Gardiner S M
Department of Physiology & Pharmacology, University of Nottingham Medical School, Queen's Medical Centre, Nottingham.
March J E
Kemp P A
Mullins J J
Bennett T
References (32)
32 references, click to expand
  1. Renal effects of captopril and nitrendipine in transgenic rats with an extra renin gene.
    Hypertension. 1994 May;23(5):626-31 PMID: 8175172
  2. Antihypertensive effects of the endothelin receptor antagonist BQ-123 in conscious spontaneously hypertensive rats.
    J Cardiovasc Pharmacol. 1993;22 Suppl 8:S321-4 PMID: 7509976
  3. Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065.
    Br J Pharmacol. 1994 May;112(1):207-13 PMID: 8032643
  4. SB 209670, a rationally designed potent nonpeptide endothelin receptor antagonist.
    Proc Natl Acad Sci U S A. 1994 Aug 16;91(17):8052-6 PMID: 8058755
  5. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension.
    J Hypertens. 1994 May;12(5):561-7 PMID: 7930556
  6. Antihypertensive effects of BQ-123, a selective endothelin ETA receptor antagonist, in spontaneously hypertensive rats treated with DOCA-salt.
    Eur J Pharmacol. 1994 Jul 11;259(3):339-42 PMID: 7982465
  7. Beta-adrenergic neuroeffector mechanisms in cardiac hypertrophy of renin transgenic rats.
    Hypertension. 1994 Dec;24(6):653-62 PMID: 7995621
  8. Myocardial remodeling in hypertensive Ren-2 transgenic rats.
    Hypertension. 1995 Jan;25(1):98-104 PMID: 7843762
  9. In vivo pharmacological characterization of the non-peptide endothelin receptor antagonist SB 209670.
    Br J Pharmacol. 1995 Jan;114(2):405-13 PMID: 7881741
  10. Antihypertensive actions of the novel nonpeptide endothelin receptor antagonist SB 209670.
    Hypertension. 1995 Apr;25(4 Pt 2):818-22 PMID: 7721437
  11. Role of endothelin-1 and the ETA receptor in the maintenance of deoxycorticosterone acetate-salt-induced hypertension.
    Br J Pharmacol. 1995 Mar;114(5):925-30 PMID: 7780646
  12. Friedman and Quade tests: BASIC computer program to perform nonparametric two-way analysis of variance and multiple comparisons on ranks of several related samples.
    Comput Biol Med. 1987;17(2):85-99 PMID: 3581810
  13. Transforming growth factor-beta stimulates the expression of endothelin mRNA by vascular endothelial cells.
    Biochem Biophys Res Commun. 1989 Mar 31;159(3):1435-40 PMID: 2649101
  14. A sensitive radioimmunoassay measuring endothelin-like immunoreactivity in human plasma: comparison of levels in patients with essential hypertension and normotensive control subjects.
    Clin Sci (Lond). 1990 Mar;78(3):261-4 PMID: 2156645
  15. Fulminant hypertension in transgenic rats harbouring the mouse Ren-2 gene.
    Nature. 1990 Apr 5;344(6266):541-4 PMID: 2181319
  16. Regional haemodynamic effects of endothelin-1 and endothelin-3 in conscious Long Evans and Brattleboro rats.
    Br J Pharmacol. 1990 Jan;99(1):107-12 PMID: 2139584
  17. Differential regional haemodynamic effects of the non-peptide angiotensin II antagonist, DuP 753, in water-replete and water-deprived Brattleboro rats.
    Life Sci. 1991;48(8):733-9 PMID: 1994182
  18. Regional and cardiac haemodynamic responses to glyceryl trinitrate, acetylcholine, bradykinin and endothelin-1 in conscious rats: effects of NG-nitro-L-arginine methyl ester.
    Br J Pharmacol. 1990 Nov;101(3):632-9 PMID: 2127552
  19. Cytokine stimulated endothelin release from endothelial cells.
    Life Sci. 1991;48(14):1379-84 PMID: 1901127
  20. Differential effects of (+/-)-dobutamine and human alpha-CGRP on cardiac and on regional haemodynamics in conscious Long Evans rats.
    Br J Pharmacol. 1991 Jun;103(2):1500-8 PMID: 1884104
  21. Cellular mechanism of endothelin-1 release by angiotensin and vasopressin.
    Hypertension. 1991 Aug;18(2):165-70 PMID: 1909304
  22. Chronic synergistic effect of endothelin-1 and angiotensin II on blood pressure in conscious rats.
    J Cardiovasc Pharmacol. 1991;17 Suppl 7:S514-6 PMID: 1725429
  23. Role of tissue renin in the pathophysiology of hypertension in TGR(mREN2)27 rats.
    Hypertension. 1992 Jun;19(6 Pt 2):681-6 PMID: 1592468
  24. Induction of endothelin-1 gene by angiotensin and vasopressin in endothelial cells.
    Hypertension. 1992 Jun;19(6 Pt 2):753-7 PMID: 1592477
  25. Regulation of endothelin-1 synthesis in cultured guinea pig airway epithelial cells by various cytokines.
    Biochem Biophys Res Commun. 1992 Aug 14;186(3):1594-9 PMID: 1510683
  26. Endothelin-1 augments pressor response to angiotensin II infusion in rats.
    Hypertension. 1992 Sep;20(3):292-7 PMID: 1516947
  27. Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model.
    Life Sci. 1993;52(8):717-24 PMID: 8446001
  28. Comparison of the regional haemodynamic effects of the AT1-receptor antagonists, losartan and EXP 3174, in water-deprived Brattleboro rats.
    Br J Pharmacol. 1993 Mar;108(3):684-8 PMID: 8467356
  29. Increased endothelin-1 content in blood vessels of deoxycorticosterone acetate-salt hypertensive but not in spontaneously hypertensive rats.
    Hypertension. 1993 Mar;21(3):294-300 PMID: 8478038
  30. Circadian blood pressure variation in transgenic hypertensive rats.
    Hypertension. 1993 Jul;22(1):97-101 PMID: 8319999
  31. Characterization of endothelin isoforms in human heart: endothelin-2 demonstrated.
    J Cardiovasc Pharmacol. 1993;22 Suppl 8:S26-8 PMID: 7509960
  32. Mechanisms of hypertension in transgenic rats expressing the mouse Ren-2 gene.
    Am J Physiol. 1994 Apr;266(4 Pt 2):R1273-9 PMID: 8184972
Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
Published
1995-10-00
Pages
2237-44
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1908969
Subset
IM
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