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Verfasst von:Hesse, Christiane [VerfasserIn]   i
 Luntz, Steffen P. [VerfasserIn]   i
 Siedler, Heike [VerfasserIn]   i
 Unnebrink, Kristina [VerfasserIn]   i
 Mikus, Gerd [VerfasserIn]   i
 Bruijn, Marianne [VerfasserIn]   i
 Zondag, Edu [VerfasserIn]   i
 Vries, Michiel [VerfasserIn]   i
 Seibert-Grafe, Monika [VerfasserIn]   i
 Haefeli, Walter E. [VerfasserIn]   i
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

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