Effect of Olopatadine and Other Histamine H&lt;sub&gt;1&lt;/sub&gt; Receptor Antagonists on the Skin Inflammation Induced by Repeated Topical Application of Oxazolone in Mice

Tamura, Tadafumi; Masaki, Shigehiro; Ohmori, Kenji; Karasawa, Akira

doi:10.1159/000086272

Cited by 11 publications

(7 citation statements)

References 43 publications

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“…Interestingly, one of our drug hits, fexophenadine (137), was reported to possess potent anti-rheumatic and anti-inflammatory properties [85] suggesting their ERb affinities, which further validates our molecular modeling approach and conclusions.…”

Section: In Silico Screeningsupporting

confidence: 79%

Pharmacophore and QSAR modeling of estrogen receptor β ligands and subsequent validation and in silico search for new hits

Taha

Tarairah

Zalloum

et al. 2010

Journal of Molecular Graphics and Modelling

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Section: In Silico Screeningsupporting

confidence: 79%

Pharmacophore and QSAR modeling of estrogen receptor β ligands and subsequent validation and in silico search for new hits

Taha

Tarairah

Zalloum

et al. 2010

Journal of Molecular Graphics and Modelling

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“…On the other hand, the other histamine H 1 receptor antagonists did not significantly suppress the increase in ear thickness. Moreover, they did not affect the production of cytokines in the lesioned ear [26] . In the present study, olopatadine inhibited the increases in ear swelling and the increased level of IFN ␥ .…”

Section: Discussionmentioning

confidence: 86%

Olopatadine Ameliorates Rat Experimental Cutaneous Inflammation by Improving Skin Barrier Function

et al. 2007

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Olopatadine hydrochloride (olopatadine) is an antiallergic agent with histamine H₁ receptor antagonistic action. We investigated the possible efficacies of olopatadine on the chronic inflammatory dermatitis and the impaired skin barrier functions induced by repeated application of oxazolone in rats. Oxazolone-sensitized rats were challenged with oxazolone applied to the ear every 3 days. Olopatadine was orally administered once daily (1 and 3 mg/kg/day). The effects of the drug were quantified by measurements of ear thickness, levels of cytokines in the lesioned ear and the number of scratching episodes. As parameters of skin barrier function, transepidermal water loss (TEWL) and hyaluronic acid (HA) levels in the lesioned ear were measured. The effect of olopatadine on the production of HA by cultured dermal fibroblasts was also measured. Repeated topical application of oxazolone to rat ears induced local inflammation that was exemplified by swelling. In inflamed ears, the amount of IFNγ increased at both the protein and mRNA level, but IL-4 levels changed minimally. Olopatadine significantly decreased ear swelling and the number of scratching episodes. The drug also significantly inhibited the increase of IFNγ and nerve growth factor production in inflamed ears. Olopatadine significantly inhibited the increase in TEWL and the decrease in HA in lesioned ears. Furthermore, the drug stimulated the production of HA by cultured dermal fibroblasts. These results suggest that olopatadine suppressed inflammation and scratching not only by inhibiting cytokine production, but also by repairing skin barrier function.

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“…In clinical settings, chlorpheniramine is regarded as ineffective against itching and/or scratching in atopic dermatitis patients [17] . On the other hand, olopatadine decreased the production of various cytokines, and tachykinin and chemical mediator release had inhibitory effects [18][19][20][21] . Therefore, the inhibition of scratching behavior by olopatadine induced by TNCB might have been generated by the above pharmacological properties.…”

Section: Discussionmentioning

confidence: 96%

Synergetic Effects of Prednisolone and Olopatadine on Atopic Dermatitis Model of Hairless Mice

Kagawa

Izawa²,

Yano³

et al. 2010

Pharmacology

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We investigated the synergetic effects of glucocorticoid and histamine H1 receptor antagonists on an atopic dermatitis model. Hairless mice were used in this study and an atopic dermatitis model was made by repeated application of 2,4,6-trinitrochlorobenzene. The effects of glucocorticoid, histamine H1 receptor antagonists, and the simultaneous use of these drugs were investigated by measuring scratching behavior, skin symptoms and nerve growth factor (NGF) in the skin. Topical application of prednisolone significantly inhibited scratching behavior, skin symptoms and NGF contents in the skin by repeated application. Olopatadine also showed a significant effect on scratching behavior and NGF contents in the skin, whereas chlorpheniramine showed no significant inhibitory effect on these indices. Furthermore, the combined use of prednisolone and olopatadine potentiated the inhibition of scratching behavior, skin symptoms, and NGF in the skin. From these findings, olopatadine potentiated the inhibitory effect of prednisolone on the symptoms of atopic dermatitis by inhibiting NGF.

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Effect of Olopatadine and Other Histamine H<sub>1</sub> Receptor Antagonists on the Skin Inflammation Induced by Repeated Topical Application of Oxazolone in Mice

Cited by 11 publications

References 43 publications

Pharmacophore and QSAR modeling of estrogen receptor β ligands and subsequent validation and in silico search for new hits

Pharmacophore and QSAR modeling of estrogen receptor β ligands and subsequent validation and in silico search for new hits

Olopatadine Ameliorates Rat Experimental Cutaneous Inflammation by Improving Skin Barrier Function

Synergetic Effects of Prednisolone and Olopatadine on Atopic Dermatitis Model of Hairless Mice

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