Abstract:
:1. The aim of the present study was to explore the effects of CPU0213, a dual endothelin ET(A)/ET(B) receptor antagonist, and nifedipine, a calcium antagonist, in relieving pulmonary hypertension (PH). Both endothelin receptor and calcium antagonists have been reported to be effective in alleviating the remodelling of pulmonary arteries induced by monocrotaline (MCT) in rats. 2. After an initial single dose of 60 mg/kg, s.c., MCT, CPU0213 was administered to rats at doses of 25, 50 or 100 mg/kg, p.o., for 28 days. In addition, nifedipine was administered to another group of rats at a dose of 10 mg/kg, p.o., for 28 days. The haemodynamics of the right ventricle, pulmonary vascular activity, remodelling of the pulmonary arterioles (< 150 microm) and biochemical changes were evaluated. 3. Right ventricular systolic pressure (RVSP), central venous pressure (CVP), the maximum rate of uprising pressure (dP/dT(max)) and the weight index of the right ventricle were significantly elevated in MCT-treated rats. In addition, increases in pulmonary endothelin-1, malonyldialdehyde (MDA) and hydroxyproline content and a reduction in superoxide dismutase activity was found after MCT treatment. The thickness and area of the pulmonary arterial wall were significantly increased in MCT-treated rats compared with control rats. At all three doses tested, CPU0213 ameliorated these changes in a dose-dependent manner and the effects were associated with a greater reduction in the remodelling of pulmonary arterioles. However, nifedipine was only partially effective in amelerioating biochemical and haemodynamic changes induced by MCT, significantly reducing RVSP, CVP, +dp/dt(max), tissue MDA, inducible nitric oxide synthase and hydroxyproline content, increasing -dp/dt(min) and having no effect on the other parameters investigated. In addition, nifedipine had no effect on remodelling of the arterial wall. 4. In conclusion, CPU0213 is more effective than nifedipine in suppressing the remodelling of pulmonary arterioles in PH induced by MCT treatment of rats. Furthermore, CPU0213 may have promise in treating PH secondary to connective tissue disease.
journal_name
Clin Exp Pharmacol Physioljournal_title
Clinical and experimental pharmacology & physiologyauthors
Cui B,Cheng YS,Dai DZ,Li N,Zhang TT,Dai Ydoi
10.1111/j.1440-1681.2008.05044.xsubject
Has Abstractpub_date
2009-02-01 00:00:00pages
169-75issue
2eissn
0305-1870issn
1440-1681pii
CEP5044journal_volume
36pub_type
杂志文章abstract::The inhibitory effect of morphine on intestine was observed by following the intestinal transit of a charcoal meal. This inhibitory effect of morphine was antagonized by naloxone. In addition, the inhibitory effect of morphine was also suppressed by prior administration of yohimbine and phentolamine. However, prazosin...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1984.tb00873.x
更新日期:1984-11-01 00:00:00
abstract::Prostaglandin (PG) efflux into ureteral (UE) and venous effluents (VE) of rabbit isolated perfused kidneys was determined by superfusion bioassay and radioimmunoassay (RIA), in response to injections of arginine-vasopressin (AVP), the non-pressor vasopressin analogue 1-deamino-8-D-arginine vasopressin (dDAVP) and arac...
journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1986.tb00942.x
更新日期:1986-08-01 00:00:00
abstract::Doxorubicin (DOX) is the most commonly used anticancer drug; however, it has limited use because prolonged administration may result in severe cardiotoxicity. Simvastatin (SIM), generally prescribed for hypercholesterolaemia, has also shown salubrious results in the monotherapy or combinational drug therapy of differe...
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doi:10.1111/1440-1681.13071
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pub_type: 杂志文章,评审
doi:10.1111/1440-1681.13303
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
doi:10.1111/j.1440-1681.1988.tb01099.x
更新日期:1988-06-01 00:00:00
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doi:10.1111/1440-1681.12818
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pub_type: 杂志文章
doi:10.1111/j.1440-1681.2008.04996.x
更新日期:2008-10-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
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更新日期:1998-10-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2001-04-01 00:00:00
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更新日期:2006-01-01 00:00:00
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doi:10.1111/1440-1681.12601
更新日期:2016-09-01 00:00:00
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pub_type: 杂志文章
doi:10.1046/j.1440-1681.2002.03598.x
更新日期:2002-01-01 00:00:00
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更新日期:2017-02-01 00:00:00
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更新日期:1994-04-01 00:00:00
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更新日期:2000-11-01 00:00:00
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更新日期:1992-05-01 00:00:00
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更新日期:2001-03-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
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更新日期:1995-09-01 00:00:00
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更新日期:2010-08-01 00:00:00
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更新日期:2020-07-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
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journal_title:Clinical and experimental pharmacology & physiology
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更新日期:2011-12-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
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更新日期:1997-03-01 00:00:00
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journal_title:Clinical and experimental pharmacology & physiology
pub_type: 杂志文章
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更新日期:1984-07-01 00:00:00