Preclinical evidence of azelastine hydrochloride activity

Lieberman, Phillip

doi:10.1016/s0011-393x(02)80061-3

Cited by 3 publications

(3 citation statements)

References 56 publications

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“…Second-generation antihistamines are characterized by reduced lipophilicity, large size, and extensive protein binding, and specifi city for the H 1 -receptor [6]. We compared effects of selected 2nd generation H 1 -antihistamines on the respiratory burst of rat phagocytes with those of dithiaden, a fi rst-generation H 1 -antihistamine.…”

Section: Resultsmentioning

confidence: 99%

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Effect of H1-antihistamines on the oxidative burst of rat phagocytes

et al. 2006

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Section: Resultsmentioning

confidence: 99%

“…Other possible mechanisms for this inhibitory effect of antihistamines could be via interference with calcium ion movement, enzymatic pathways or second messengers [6].…”

Section: Resultsmentioning

confidence: 99%

Effect of H1-antihistamines on the oxidative burst of rat phagocytes

et al. 2006

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“…Inhibition of ROS generation by antihistamines might beneficially contribute to the treatment of allergic noninfectious inflammation and support the treatment of acute exacerbation of pathological inflammation (Thurmond et al 2008). It has been suggested that the suppression of CL by antihistamines is not a result of their direct scavenging activities; rather, it originates from their interference with calcium movement, enzyme pathways, or second messenger interaction (Lieberman 2002;Králová et al 2006). However, compounds without any intracellular effect should not interfere with generation of ROS in neutrophils.…”

Section: Discussionmentioning

confidence: 99%

Molecular pharmacology of antihistamines in inhibition of oxidative burst of professional phagocytes

Nosáľ¹,

Jancinová²,

Drábiková³

et al. 2015

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Antihistamines of the H 1 and H 3 /H 4 groups interfere with oxidative burst of human professional phagocytes in vitro. In the concentration of 10 μM, H 1 antihistamines of the 1 st and 2 nd generation inhibited oxidative burst of human neutrophils in the rank order of potency: dithiaden > loratadine > brompheniramine > chlorpheniramine > pheniramine. Of the H 1 antihistamines, the most effective was dithiaden in suppressing oxidative burst of whole human blood and dosedependently the chemiluminescence of isolated neutrophils at extra-and intracellular level. Inhibition of free oxygen radical generation in isolated neutrophils by dithiaden resulted from the inhibition of protein kinase C activation. The potentiation of recombinant caspase-3 by dithiaden is supportive of the antiinflammatory effect of dithiaden and suggestive of increasing the apoptosis of professional phagocytes. Of the H 3 /H 4 antihistamines, the most effective was JNJ7777120 in decreasing chemiluminescence in whole blood and also at extra-and intracellular sites of isolated neutrophils. JNJ 10191584 and thioperamide were less effective and the latter significantly potentiated free oxygen radical generation intracellularly. The results demonstrated that, compared with the H 3 /H 4 antihistamines investigated, H 1 antihistamines were much more potent in inhibiting free oxygen radical generation in human professional phagocytes. This finding should be taken into account therapeutically.

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