Drug receptors and control of the cardiovascular system: Recent advances

Rr, Ruffolo; Jp, Hieble; Dp, Brooks; Gz, Feuerstein; Aj, Nichols

doi:10.1007/978-3-0348-7136-5_4

Cited by 6 publications

(2 citation statements)

References 950 publications

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“…Vascular α 1 -adrenoceptor plays a primary role in maintaining systemic arterial pressure and arteriolar resistance [5-7]. Recent studies have shown that the α 1D -adrenoceptor plays a major role in vasoconstriction of mesenteric arteries [13,14] and that the α 1A -adrenoceptor is responsible for vascular contraction in distal mesenteric arteries [13].…”

Section: Discussionmentioning

confidence: 99%

“…In blood vessels, post-junctional α 1 -adrenoceptors play an important role in controlling vascular smooth muscle tone and thus modulate peripheral arterial resistance [5-7]. Radioligand binding, molecular cloning studies and isolated tissue experiments have identified three α 1 -adrenoceptor subtypes that are designated α 1A , α 1B , and α 1D [8,9] and the functional dominance in adrenergic responses varies with tissue and species [10].…”

Section: Introductionmentioning

confidence: 99%

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Gender difference and change of α₁-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Park

Bahk

et al. 2011

Korean J Anesthesiol

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BackgroundThe purpose of this study was to evaluate the gender-related changes in the function and distribution of α1-adrenoceptors in the distal mesenteric artery of streptozotocin (STZ)-induced diabetic rats at the level of α1-adrenoceptor subtypes.MethodsDiabetes was induced by intravenous injection of STZ in a dose of 60 mg/kg through the tail vein in 8 week-old male or female Sprague-Dawley rats (n = 13/group). Age-matched normal rats (n = 15) were used as a control group. Four weeks after STZ injection, the change in mean arterial pressure caused by a 45° tilting was recorded. The α1-adrenoceptor subtypes mediating contractions of the distal mesenteric artery were investigated using the agonist, phenylephrine as well as subtype-selective antagonists including prazocin, 5-methylurapidil, and BMY 7378. The expression of α1-adrenoceptor subtypes of each artery was examined by immunofluorescence staining and western blotting using subtype selective antibodies.ResultsCompared with normal male rats, the contractile response to phenylephrine was decreased in the distal mesenteric artery in normal female rats. Moreover, a decrease in contractile force was observed in STZ-induced diabetic rats compared with age-matched controls. Western blotting revealed that there was the difference between normal male and female rats in manifestation of the α1D-adrenoceptor. In STZ-induced male and female diabetic rats, all α1-adrenoceptor subtypes were decreased in distal mesenteric arteries, compared with normal rats.ConclusionsThere was the gender-related functional difference of α1-adrenoceptors in normal rats. In both male and female rats, diabetes decreased the contractile response in mesenteric arteries, which might be caused by the overall change in α1-adrenoceptor.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Gender difference and change of α₁-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Park

Bahk

et al. 2011

Korean J Anesthesiol

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Antihypertensive activity of the non-peptide angiotensin II receptor antagonist, SK&F 108566, in rats and dogs

Brooks

Fredrickson

Weinstock

et al. 1992

Naunyn-Schmiedeberg's Arch Pharmacol

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The antihypertensive activity of the nonpeptide angiotensin II receptor antagonist, SK&F 108566 (E)-alpha-[[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5- yl]methylene]-2-thiophene propanoic acid), was examined in rats and dogs. SK&F 108566 produced dose-dependent decreases in blood pressure in renin-dependent hypertensive rats. At 10 mg/kg intraduodenally, mean arterial blood pressure fell from between 150-160 mm Hg to approximately 124 mm Hg. A sustained infusion of SK&F 108566 at 25 micrograms/min intraduodenally normalized blood pressure during 3 days of infusion and for 18 h following cessation of the infusion. Evaluation of the systemic hemodynamic effects of SK&F 108566 in chronically instrumented renin-dependent hypertensive rats demonstrated that the antihypertensive effects of SK&F 108566 were accompanied by a significant increase in cardiac output with little change in stroke volume. In dogs made acutely hypertensive by an intravenous infusion of angiotensin I, SK&F 108566 resulted in dose-dependent decreases in blood pressure. The antihypertensive activity of SK&F 108566 at 10 mg/kg p.o. was maintained for between 13-15 h, a similar duration of action as observed with enalapril (1 mg/kg, p.o.). Administration of DuP 753 (losartan) intravenously caused a small and short-lived fall in blood pressure in the angiotensin I-infused hypertensive dog. However, the active metabolite of losartan, EXP 3174, resulted in a response of longer duration. In dogs made hypertensive by placement of an ameroid constrictor on the left renal artery, SK&F 108566 (10 mg/kg, p.o.) or enalapril (1 mg/kg, p.o.) resulted in antihypertensive responses of at least 12 h duration. The data indicate that SK&F 108566 is a long-acting antihypertensive agent in the rat and dog.

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Endothelium-dependent relaxation of porcine pulmonary arteries via 5-HT1C-like receptors

Glusa

Richter

1993

Naunyn-Schmiedeberg's Arch Pharmacol

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In PGF2 alpha-precontracted pulmonary arteries with intact endothelium, 5-hydroxytryptamine (5-HT, 1.0-100 nmol/l) caused a concentration-dependent reversible relaxation, at higher concentrations the contractile response prevailed. In endothelium-denuded vessels relaxation was absent. 5-HT-induced relaxation of precontracted pulmonary arteries was probably mediated by release of an endothelium-derived relaxing factor (EDRF). Preincubation of the arteries with methylene blue or NG-nitro-L-arginine (200 mumol/l) attenuated the relaxant effect. The 5-HT-induced relaxation was accompanied by an increase in cGMP. Indomethacin (3 mumol/l) did not influence the 5-HT-induced relaxation indicating that eicosanoids are not involved in the relaxant response to 5-HT. The 5-HT1C and 5-HT2 receptor agonist alpha-methyl-5-HT was as potent as 5-HT in inducing relaxation. The rank order of relaxant potency of the agonists investigated was alpha-methyl-5-HT > 5-HT > 5-methoxytryptamine > tryptamine > omega-methyl-5-HT > 5-carboxamidotryptamine > 2-methyl-5-HT > 5,6-dihydroxytryptamine > m-chlorophenylpiperazine > sumatriptan > 8-OH-DPAT. Phentolamine, pindolol and ICS 205-930 did not interfere with the relaxant effect. The 5-HT2 receptor antagonist ketanserin (1 mumol/l) inhibited the contractile response but did not alter vasodilatation. Apart from the blockade of the contractile effects, mesulergine, cyproheptadine and mianserin (0.1-3.0 mumol/l, each) induced a parallel shift to the right of the concentration-response curve for the relaxation induced by alpha-methyl-5-HT or 5-HT. Spiperone (0.3 mumol/l) exerted weak inhibitory effects on relaxation and contraction.(ABSTRACT TRUNCATED AT 250 WORDS)

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Drug receptors and control of the cardiovascular system: Recent advances

Cited by 6 publications

References 950 publications

Gender difference and change of α₁-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Gender difference and change of α₁-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Antihypertensive activity of the non-peptide angiotensin II receptor antagonist, SK&F 108566, in rats and dogs

Endothelium-dependent relaxation of porcine pulmonary arteries via 5-HT1C-like receptors

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Drug receptors and control of the cardiovascular system: Recent advances

Cited by 6 publications

References 950 publications

Gender difference and change of α1-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Gender difference and change of α1-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Antihypertensive activity of the non-peptide angiotensin II receptor antagonist, SK&F 108566, in rats and dogs

Endothelium-dependent relaxation of porcine pulmonary arteries via 5-HT1C-like receptors

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Gender difference and change of α₁-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats

Gender difference and change of α₁-adrenoceptors in the distal mesenteric arteries of streptozotocin-induced diabetic rats