Naftopidil inhibits 5-hydroxytryptamine-induced platelet aggregation and 5-hydroxytryptamine uptake in platelets of healthy volunteers
Abstract Naftopidil exerts its antihypertensive action via $ α_{1} $-adrenoceptor blockage and $ Ca^{2+} $ antagonism in vascular smooth muscle. Since the chemically similar 1-(1-naphthyl) piperazine is known to be a 5-$ hydroxytryptamine_{2} $ 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 $ K_{i} $ value of 1.1 μM, the $ pIC_{50} $ was 5.09 with induction of aggregation by 1 μM 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 $ α_{1} $-adrenoceptor blocking and $ Ca^{2+} $ antagonistic properties..
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
1994 |
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| Erschienen: |
1994 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:46 |
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| Enthalten in: |
European journal of clinical pharmacology - 46(1994), 3 vom: Apr., Seite 271-274 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Kirsten, R. [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Anmerkungen: |
© Springer-Verlag 1994 |
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| doi: |
10.1007/BF00192561 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
OLC2064072152 |
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| 100 | 1 | |a Kirsten, R. |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Naftopidil inhibits 5-hydroxytryptamine-induced platelet aggregation and 5-hydroxytryptamine uptake in platelets of healthy volunteers |
| 264 | 1 | |c 1994 | |
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| 520 | |a Abstract Naftopidil exerts its antihypertensive action via $ α_{1} $-adrenoceptor blockage and $ Ca^{2+} $ antagonism in vascular smooth muscle. Since the chemically similar 1-(1-naphthyl) piperazine is known to be a 5-$ hydroxytryptamine_{2} $ 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 $ K_{i} $ value of 1.1 μM, the $ pIC_{50} $ was 5.09 with induction of aggregation by 1 μM 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 $ α_{1} $-adrenoceptor blocking and $ Ca^{2+} $ antagonistic properties. | ||
| 700 | 1 | |a Breidert, M. |4 aut | |
| 700 | 1 | |a Nelson, K. |4 aut | |
| 700 | 1 | |a Heine, A. |4 aut | |
| 700 | 1 | |a Rosenkranz, S. |4 aut | |
| 700 | 1 | |a Erdeg, B. |4 aut | |
| 700 | 1 | |a Niebch, G. |4 aut | |
| 700 | 1 | |a Borbe, H. O. |4 aut | |
| 700 | 1 | |a Siebert-Weigel, M. |4 aut | |
| 700 | 1 | |a Respondek, J. |4 aut | |
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| 773 | 1 | 8 | |g volume:46 |g year:1994 |g number:3 |g month:04 |g pages:271-274 |
| 856 | 4 | 1 | |u https://doi.org/10.1007/BF00192561 |z lizenzpflichtig |3 Volltext |
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