Effect of Y-24180, a receptor antagonist to platelet-activating factor (PAF), on allergic cutaneous reactions in actively sensitized mice

Abstract

Y-24180 was demonstrated not only to suppress the IPR and LPR, but also to show strong suppressive effects in combination with topical hydrocortisone. Therefore, Y-24180 is expected to contribute to the treatment of inflammatory skin diseases including atopic dermatitis.

Anti‐inflammatory effects of nitric oxide‐releasing hydrocortisone NCX 1022, in a murine model of contact dermatitis

“…Irritant contact dermatitis was induced by applying 5% benzalkonium chloride (Sigma, St Louis, MO, U.S.A.), dissolved in olive oil : acetone (1 : 5 v v −1 ) on the surface of either the dorsal aspect of both ears (20 μ l per site), or on the observed unshaved abdominal skin (intravital microscopy experiments) as previously described ( Seeliger et al ., 2003 ). Groups of mice (6–8‐weeks old) have received topically (100 μ l per site applied directly on the skin) treatment with hydrocortisone (0.3, 3 or 30 nmol per site), NO‐hydrocortisone (0.3, 3 or 30 nmol per site) or their vehicle (ethanol : sterile water 1 : 1), 15 min before (pre‐treatment), or 5 min after (post‐treatment) the induction of irritant contact dermatitis ( Yamaguchi et al ., 2000 ). Animals were treated with DETA‐NONOate (3 nmol) or its vehicle (ethanol : sterile water 1 : 1), topically 5 min after benzalkonium chloride application.…”

Effect of Y-24180 on Ca2+ movement and proliferation in renal tubular cells

“…The novel finding of this study is that Y-24180, a chemical conventionally thought to exert its in vivo and in vitro actions purely via acting as a specific antagonist of PAF receptors (Cailleaux et al, 1999;Cunningham, 1990;Iwahisa et al, 1996;Kagoshima et al, 1997;Kawaguchi et al, 2001;Komatsu and Amano, 1997;Kuitert and Barnes, 1995;Kusuhara et al, 2000;Michel and Dubertret, 1992;Mizuki et al, 1999;Okamoto et al, 1992;Oshiro et al, 2000;Prozialeck and Niewenhuis, 1991;Stafforini, 2001;Stewart et al, 1990;Suzuki et al, 1998;Terasawa et al, 1990;Watanabe et al, 1991;Yamaguchi et al, 1997Yamaguchi et al, , 1999Yamaguchi et al, , 2000 induces significant increases in [Ca 2 + ] i in renal tubular cells. An increase in [Ca 2 + ] i may cause numerous cellular events including protein activation, gene expression, cell growth (Bootman et al, 1997), just to name a few.…”

Διερεύνηση Της Ύπαρξης Του Παράγοντα Ενεργοποίησης Αιμοπεταλίων (PAF) Ή Άλλων Μεσολαβητών Σε Κυανοφύκη Σπηλαίων

“…Ένα ακόµα παράγωγο των τριαζολοθειενοδιαζεπινών, το Υ-24180 αναστέλλει τη προκαλούµενη από τον PAF συσσώρευση των αιµοπεταλίων του κουνελιού και του ανθρώπου µε τιµές IC 50 4,1 και 0,72nm αντίστοιχα, είναι δηλαδή πολύ πιο δραστικό από το WEB 2086. ∆εν εµφανίζει ανασταλτική δράση στη συσσώρευση αιµοπεταλίων που προκαλείται από το ADP και το αραχιδονικό οξύ , Yamaguchi, S. et al 2000.…”