Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF).
Overall, rupatadine combines histamine and PAF antagonist activities in vivo with high potency, the antihistamine properties being similar to or higher than those of loratadines, whereas rup atadine's PAF antagonists effects were near those of WEB-2066.
Acclimatization of rats after ground transportation to a new animal facility
- S. Capdevila, M. Giral, J. L. Ruíz de la Torre, R. Russell, K. Kramer
- BiologyLaboratory Animals. Journal of the Laboratory…
- 1 April 2007
Results suggest that rats take three days to acclimatize to a new environment, as measured by the physiological parameters of body weight, HR and activity.
Effects of PAF‐antagonists in mouse ear oedema induced by several inflammatory agents
- M. Merlos, L. Gómez, M. Giral, M. L. Vericat, J. García-Rafanell, J. Forn
- Medicine, BiologyBritish Journal of Pharmacology
- 1 December 1991
The results suggest that topical formulations containing PAF‐antagonists could be useful in the treatment of some inflammatory skin diseases and provide evidence on the involvement of PAF in these inflammatory processes.
Effects of UR‐12633, a new antagonist of platelet‐activating factor, in rodent models of endotoxic shock
- M. Giral, D. Balsa, R. Ferrando, M. Merlos, J. García-Rafanell, J. Forn
- Biology, MedicineBritish Journal of Pharmacology
- 1 July 1996
In spite of the multifactorial nature of endotoxic shock, the new potent PAF antagonist, UR‐12633, proved effective in protecting against changes in most shock markers, as shown by prevention of haemoconcentration and, to a lesser degree, the increase in Evans blue dye extravasation.
Dual effect of a new compound, rupatadine, on edema induced by platelet‐activating factor and histamine in dogs: Comparison with antihistamines and PAF antagonists
- M. Queralt, M. Merlos, M. Giral, A. Puigdemont
- Biology, Medicine
- 1 September 1996
The histamine‐and PAF‐induced wheal model in dogs proved useful for independent evaluation of histamine and PAF antagonist properties of the tested compounds, as pure antagonists blocked the effect of only one of the mediators.
(Pyridylcyanomethyl)piperazines as orally active PAF antagonists.
- E. Carceller, C. Almansa, J. Forn
- Chemistry, BiologyJournal of Medicinal Chemistry
- 30 October 1992
Three of the most active compounds, 1-acyl-4-cyano-4-(4-pyridylcyanomethyl)piperazine, 100, 114, and 115 have been selected for further pharmacological development.
[(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine.
- E. Carceller, M. Merlos, J. Forn
- Chemistry, BiologyJournal of Medicinal Chemistry
- 19 August 1994
Optimum structure 19 (UR-12592) incorporating a (5-methyl-3-pyridyl)methyl radical displayed an unique dual activity inhibiting both PAF-induced effects and H1 antihistamine activity, and showed itself to be devoid of CNS depressant effects.
Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF antagonists.
- E. Carceller, M. Merlos, J. Forn
- Chemistry, BiologyJournal of Medicinal Chemistry
- 1 October 1993
Three different types of acyl substituents of similar potency emerge from this work: N-(diphenylmethylamino)acetyl, 3-substituted 3-hydroxy-3-phenylpropionyl, and N- substituting 3-amino-3 -phenyl Propionyl groups.
4-substituted 2-alkoxytetrahydrofurans as potent and long-lasting PAF antagonists.
- E. Carceller, M. Merlos, M. Giral, J. Bartrolí, J. García-Rafanell, J. Forn
- Chemistry, BiologyJournal of Medicinal Chemistry
- 21 February 1992
Comparison with previously reported carba analogues suggests that the presence of the acetal group is the structural characteristic that confers its long-lasting activity.
Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity.
- E. Carceller, J. Salas, J. Forn
- Chemistry, BiologyJournal of Medicinal Chemistry
- 4 August 2001
The synthesis of a series of azo compounds able to deliver 5-aminosalicylic acid (5-ASA) and a potent platelet activating factor (PAF) antagonist in a colon-specific manner for the purpose of treating ulcerative colitis suggests that UR-12746 (70) provides an attractive new approach to the treatment of ulceratives colitis.
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