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.
Depolarization-induced phosphorylation of specific proteins, mediated by calcium ion influx, in rat brain synaptosomes.
Effect of aging on the adenyl cyclase and phosphodiesterase activity of isolated fat cells of rat.
New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones.
In vitro 20 was superior to fluconazoles, itraconazole, SCH-42427, and TAK-187 and roughly similar to voriconazole and ER-30346, and in vivo 20 showed excellent protection levels in an immunocompromised rat model of disseminated aspergillosis.
Synthesis and antifungal activity of new azole derivatives containing an N-acylmorpholine ring.
A series of azole derivatives carrying an N-acylmorpholine ring are described. The compounds were chemically designed to simulate the lanosterol D ring, taking advantage of the conformational…
Depolarizing agents and cyclic nucleotides regulate the phosphorylation of specific neuronal proteins in rat cerebral cortex slices.
- J. Forn, P. Greengard
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 1 October 1978
Incubation of the brain slices with 8-bromo cyclic AMP, 3-isobutyl-1-methylxanthine, high K+, or veratridine increased the state of phosphorylation of proteins Ia and Ib, and increased the number of neuronal proteins found in extracts of the slices.
Stimulation by dopamine of adenosine cyclic 3',5'-monophosphate formation in rat caudate nucleus: effect of lesions of the nigro-neostriatal pathway.
The data suggest that contralateral circling, induced by dopamine agonist in animals with unilateral lesions in the nigro-neostriatal pathway, may be due to an increased ability of the dopamine agonists to stimulate cyclic AMP formation on the lesioned side.
Adenosine 3',5'-Monophosphate Content in Rat Caudate Nucleus: Demonstration of Dopaminergic and Adrenergic and Receptors
The results suggest that in rat caudate nucleus there are two distinct catecholamine receptors capable of causing increased concentrations of adenosine 3',5'-monophosphate, one having the characteristic of dopamine receptor, and the other having the characteristics of β-adrenergic receptor.
Synthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines.
Modification of the pyrimidine substituents showed that 6,7-disubstitution provided the best activity and led to the identification of 3-(4-fluorophenyl)-6, 7-dimethyl-2-( 4-methylsulfonylphenyl)pyrazolo[1,5-a]pyrimidine (10f) as one of the most potent and selective COX-2 inhibitor in this series.
Active transport of 5-hydroxyindoleacetic acid by the rabbit choroid plexus in vitro. Blockade by probenecid and metabolic inhibitors.
- J. Forn
- Biology, ChemistryBiochemical Pharmacology
- 1 March 1972