Abstract：
:Naftopidil exerts its antihypertensive action via alpha 1-adrenoceptor blockage and Ca2+ antagonism in vascular smooth muscle. Since the chemically similar 1-(1-naphthyl) piperazine is known to be a 5-hydroxytryptamine2 receptor antagonist, the 5-hydroxytryptamine (5-HT) antagonistic properties of naftopidil were tested by examining 5-HT-induced aggregation and 5-HT uptake in platelets from 12 healthy volunteers after oral administration of 60 mg naftopidil or placebo. Platelet aggregation in vitro was inhibited by naftopidil with a Ki value of 1.1 microM, the pIC50 was 5.09 with induction of aggregation by 1 microM 5-HT. After oral administration of naftopidil, 5-HT-induced aggregation was significantly inhibited by 36%. 4 h after naftopidil administration, 5-HT uptake velocity was reduced by 33%. Naftopidil not only cancelled the circadian increase in 5-HT-induced aggregation velocity observed during placebo application, but also caused a decrease in aggregation velocity directly after peak plasma naftopidil levels. 5-HT uptake in platelets was also reduced following peak naftopidil plasma concentrations. The 5-HT inhibitory action of naftopidil adds a third possible antihypertensive property to naftopidil's alpha 1-adrenoceptor blocking and Ca2+ antagonistic properties.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Kirsten R,Breidert M,Nelson K,Heine A,Rosenkranz S,Erdeg B,Niebch G,Borbe HO,Siebert-Weigel M,Respondek Jdoi
10.1007/BF00192561subject
Has Abstractpub_date
1994-01-01 00:00:00pages
271-4issue
3eissn
0031-6970issn
1432-1041journal_volume
46pub_type
临床试验,杂志文章,随机对照试验abstract：OBJECTIVE:Valsartan (V), a specific inhibitor of the angiotensin II receptor subtype, AT1, has been developed for treatment of hypertension. Combination therapy with a beta-adrenoceptor blocking agent might be considered in cases with insufficient efficacy of V alone. Therefore, an interaction trial was performed to ev...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/s002280050318
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abstract：:The pharmacokinetics, hypotensive effect and tolerability of a new vasodilator, tolmesoxide (T), have been studied in 6 uncontrolled hypertensive patients receiving atenolol and diuretic. After a 50 mg oral dose mean (+/- SD) peak plasma concentration of T was 1.13 +/- 0.29 micrograms/ml-1 and occurred 0.79 +/- 0.40 h...
journal_title：European journal of clinical pharmacology
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pub_type： 杂志文章,meta分析,评审
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abstract：OBJECTIVE:To examine the impact of medication and medical conditions on the fall risk in older hospitalized patients. DESIGN:Matched case-control study. SETTING:Large regional hospital in a mid-sized German city. SUBJECTS:Four hundred eighty-one inpatients aged ≥ 65 years who fell during hospitalization ("cases") an...
journal_title：European journal of clinical pharmacology
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journal_title：European journal of clinical pharmacology
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journal_title：European journal of clinical pharmacology
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journal_title：European journal of clinical pharmacology
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journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
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journal_title：European journal of clinical pharmacology
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journal_title：European journal of clinical pharmacology
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更新日期：1993-01-01 00:00:00
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journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
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pub_type： 杂志文章,meta分析,评审
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journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：European journal of clinical pharmacology
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journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：European journal of clinical pharmacology
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