| Online-Ressource |
Verfasst von: | Hesse, Christiane [VerfasserIn]  |
| Luntz, Steffen P. [VerfasserIn]  |
| Siedler, Heike [VerfasserIn]  |
| Unnebrink, Kristina [VerfasserIn]  |
| Mikus, Gerd [VerfasserIn]  |
| Bruijn, Marianne [VerfasserIn]  |
| Zondag, Edu [VerfasserIn]  |
| Vries, Michiel [VerfasserIn]  |
| Seibert-Grafe, Monika [VerfasserIn]  |
| Haefeli, Walter E. [VerfasserIn]  |
Titel: | Kinetics and dynamics of the peripheral neurokinin-1 receptor antagonist SLV317 in healthy individuals |
Verf.angabe: | Christiane Hesse, Steffen P. Luntz, Heike Siedler, Kristina Unnebrink, Gerd Mikus, Marianne de Bruijn, Edu Zondag, Michiel de Vries, Monika Seibert‐Grafe & Walter E. Haefeli |
E-Jahr: | 2006 |
Jahr: | 24 January 2006 |
Umfang: | 6 S. |
Fussnoten: | Gesehen am 17.05.2021 |
Titel Quelle: | Enthalten in: British journal of clinical pharmacology |
Ort Quelle: | Oxford : Wiley-Blackwell, 1974 |
Jahr Quelle: | 2006 |
Band/Heft Quelle: | 61(2006), 4, Seite 414-419 |
ISSN Quelle: | 1365-2125 |
Abstract: | Aims To investigate the pharmacokinetics and the pharmacodynamic effects in dorsal hand veins of the neurokinin-1 receptor antagonist SLV317. Methods In a randomized, double-blind, placebo-controlled cross-over study 19 healthy men received a single oral dose of SLV317 or placebo. Blood samples were collected for analysis of SLV317 plasma concentrations and the inhibition of the venodilator response to substance P was evaluated using the hand vein compliance method. Results Administration of 250 mg SLV317 as an oral solution was well tolerated and resulted in mean peak plasma concentrations (± SEM) of 77 ± 9 ng ml−1 within 47 ± 3 min; the mean half-life was 9.9 ± 1.6 h. In hand veins preconstricted with phenylephrine, local infusion of substance P resulted in a mean venodilation of 56 ± 8% and 49 ± 6% (P = 0.91) before administration of SLV317 or placebo, respectively. SLV317 caused a substantial inhibition of substance P-induced venodilation, whereas placebo had no effect (P < 0.001). The maximum antagonizing effect of SLV317 averaged 95 ± 8% and was observed after 1.47 ± 00.24 h. Correspondingly, the mean area under the effect curve after administration of SLV317 [278 ± 67% h−1; 95% confidence interval (CI) 198, 358] was significantly higher compared with placebo (49 ± 12% h−1; 95% CI −24, 122; P < 0.001). Conclusions This study demonstrates that the neurokinin-1 receptor antagonist SLV317 is an orally active and highly effective antagonist of substance P-induced effects in humans. |
DOI: | doi:10.1111/j.1365-2125.2006.02590.x |
URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/https://doi.org/10.1111/j.1365-2125.2006.02590.x |
| Volltext: https://bpspubs.onlinelibrary.wiley.com/doi/abs/10.1111/j.1365-2125.2006.02590.x |
| DOI: https://doi.org/10.1111/j.1365-2125.2006.02590.x |
Datenträger: | Online-Ressource |
Sprache: | eng |
Sach-SW: | neurokinin-1 receptor antagonist |
| pharmacokinetics |
| SLV317 |
| substance P |
| vein |
K10plus-PPN: | 1757916059 |
Verknüpfungen: | → Zeitschrift |
Kinetics and dynamics of the peripheral neurokinin-1 receptor antagonist SLV317 in healthy individuals / Hesse, Christiane [VerfasserIn]; 24 January 2006 (Online-Ressource)