Abstract：
:The qualitative and quantitative effects of the (+)-S and (-)-R enantiomers and of the racemic mixture of the Ca2+ channel antagonist, nicardipine, were compared on the isolated porcine coronary artery with intact and removed endothelium. All three forms of nicardipine inhibited the contractions induced by KCl (5-90 mM) in both vessel preparations. The potency (IC50) of the (+)-S and (-)-R enantiomers and of the racemic mixture was 6.6, 31.8 and 10.9 nM in the vessel with endothelium and 6.4, 41.9 and 9.8 nM in the vessel without endothelium. The parameters of the concentration-response curves for each form of nicardipine at a submaximal KCl (60 mM) concentration and the potency ratios between the two enantiomers ((+)-S/(-)-R) were not statistically significantly different (P>0.05) in the two vessel preparations. In conclusion, qualitatively, all three forms of nicardipine showed only Ca2+ channel antagonistic effects in both vessel preparations. Quantitatively, the inhibition of contraction was stereoselective, the (+)-S enantiomer being the most potent, and was endothelium-independent.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Japelj I,Budihna MV,Stanovnik L,Krisch Idoi
10.1016/s0014-2999(99)00049-7keywords:
subject
Has Abstractpub_date
1999-03-12 00:00:00pages
43-7issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(99)00049-7journal_volume
369pub_type
杂志文章abstract：:We have reported previously that ugonin K, a flavonoid isolated from Helminthostachys zeylanica (L.) Hook, potently induces cell differentiation and mineralization of MC3T3-E1 mouse osteoblast-like cells. Here we aimed to elucidate whether ugonin K evoked osteogenesis required interaction with estrogen receptor. Resul...
journal_title：European journal of pharmacology
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abstract：:Insulin resistance is a condition in which the glycemic response to insulin is less than normal. The change in insulin sensitivity leads to several sets of responses. One set effects the beta cell and leads to its accelerated destruction and the development of diabetes mellitus. The other set generates a series of non...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2004.02.051
更新日期：2004-04-19 00:00:00
abstract：:Influenza is a major disease in humans. The reemergence of avian influenza A viruses has indicated that hyperinflammatory responses are closely related to the severity of disease. Influenza virus infection induces nuclear transcription factor kappaB (NF-kappaB) activation. NF-kappaB and NF-kappaB-dependent gene produc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.03.073
更新日期：2006-07-17 00:00:00
abstract：:Therapeutic angiogenesis is a promising strategy for treating ischemia. The lysophospholipid mediator sphingosine-1-phosphate (S1P) acts on vascular endothelial cells to stimulate migration and tube formation, and plays the critical role in developmental angiogenesis. We developed poly(lactic-co-glycolic-acid) (PLGA)-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.02.038
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abstract：:Barbiturates derived by minor structural changes to the butenyl sidechain of the convulsant 5-ethyl-5-(3'-methyl-but-2'-enyl)-barbituric acid are almost devoid of convulsant activity, but all have anaesthetic and anticonvulsant effects. Anticonvulsant activity is also observed in the convulsant barbiturate. Increased ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90382-0
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abstract：:The pharmacological mechanisms involved in the interactions between C-fibers, cholinergic fibers and mast cells were investigated in tracheally perfused rabbit lungs by measuring the simultaneous release of substance P and histamine in lung effluents. The amounts of substance P and histamine released in lung superfusa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1999-04-23 00:00:00
abstract：:In the Brattleboro rat with diabetes insipidus vasopressin V2 receptor mRNA and the mRNA of various adenylyl cyclase (AC) isoforms are moderately reduced compared with those of normal rats. In the present study renal vasopressin V2 receptor mRNA was modestly higher (by 34%), as was expression of AC 5, 6 and 9 mRNAs (u...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01461-1
更新日期：1998-01-02 00:00:00
abstract：:Behavioural evidence has accumulated that supports the hypothesis that specific territories of the striatum contribute differentially to the control of motor behaviours. The present experiments compare the behavioural effects of microinjections of amphetamine (20 microg/0.5 microl) with those elicited by the D2-class ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00752-3
更新日期：1998-12-04 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1985-08-07 00:00:00
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journal_title：European journal of pharmacology
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更新日期：1999-08-06 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90055-m
更新日期：1991-09-12 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.07.013
更新日期：2013-08-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(02)01433-4
更新日期：2002-04-12 00:00:00
abstract：:The effects of local application of a cream containing nitric oxide (NO) donors, S-nitroso-N-acetylpenicillamine (SNAP) or isosorbide dinitrate were studied in a rat model of incision pain. An incision was made in the plantar aspect of a hind paw and the cream was applied inside the surgical wound. SNAP (1-10%) or iso...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01413-9
更新日期：2002-04-19 00:00:00
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90250-3
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：2018-05-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.02.038
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：2015-07-05 00:00:00
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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更新日期：1996-09-12 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00124-1
更新日期：1998-04-24 00:00:00
