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These receptors interact with adhesion molecules expressed on the conjunctival endothelium and may be a target to treat this disease. We synthesized DS\u201070, a novel \u03b1\/\u03b2\u2010peptidomimetic \u03b1<jats:sub>4<\/jats:sub> integrin antagonist, to prevent the conjunctival infiltration of immune cells and clinical symptoms in a model of allergic conjunctivitis.<\/jats:p><\/jats:sec><jats:sec><jats:title>Experimental Approach<\/jats:title><jats:p><jats:italic>In vitro,<\/jats:italic> DS\u201070 was pharmacologically characterized using a scintillation proximity procedure to measure its affinity for \u03b1<jats:sub>4<\/jats:sub>\u03b2<jats:sub>1<\/jats:sub> integrin, and its effect on cell adhesion mediated by different integrins was also evaluated. The effects of DS\u201070 on vascular cell adhesion molecule\u20101 (VCAM\u20101)\u2010mediated degranulation of a human mast cell line and an eosinophilic cell line, which both express \u03b1<jats:sub>4<\/jats:sub>\u03b2<jats:sub>1<\/jats:sub>, and on VCAM\u20101\u2010mediated phosphorylation of ERK 1\/2 in Jurkat E6.1 cells were investigated. Effects of DS\u201070 administered in the conjunctival fornix of ovalbumin\u2010sensitized guinea pigs were evaluated.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key Results<\/jats:title><jats:p>DS\u201070 bound to integrin \u03b1<jats:sub>4<\/jats:sub>\u03b2<jats:sub>1<\/jats:sub> with nanomolar affinity, prevented the adhesion of \u03b1<jats:sub>4<\/jats:sub> integrin\u2010expressing cells, antagonized VCAM\u20101\u2010mediated degranulation of mast cells and eosinophils and ERK 1\/2 phosphorylation. Only 20% was degraded after an 8\u00a0h incubation with serum. DS\u201070 dose\u2010dependently reduced the clinical symptoms of allergic conjunctivitis, conjunctival \u03b1<jats:sub>4<\/jats:sub> integrin expression and conjunctival levels of chemokines and cytokines in ovalbumin\u2010sensitized guinea pigs.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusions and Implications<\/jats:title><jats:p>These findings highlight the role of \u03b1<jats:sub>4<\/jats:sub> integrin in allergic conjunctivitis and suggest that DS\u201070 is a potential treatment for this condition.<\/jats:p><\/jats:sec>","DOI":"10.1111\/bph.14458","type":"journal-article","created":{"date-parts":[[2018,7,27]],"date-time":"2018-07-27T04:55:20Z","timestamp":1532667320000},"page":"3891-3910","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":29,"title":["DS\u201070, a novel and potent \u03b1<sub>4<\/sub> integrin antagonist, is an effective treatment for experimental allergic conjunctivitis in guinea pigs"],"prefix":"10.1111","volume":"175","author":[{"given":"Samantha Deianira","family":"Dattoli","sequence":"first","affiliation":[{"name":"Department of Pharmacy and Biotechnology University of Bologna  Bologna Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Monica","family":"Baiula","sequence":"additional","affiliation":[{"name":"Department of Pharmacy and Biotechnology University of Bologna  Bologna Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rossella","family":"De Marco","sequence":"additional","affiliation":[{"name":"Department of Chemistry \u201cG. Ciamician\u201d University of Bologna  Bologna Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andrea","family":"Bedini","sequence":"additional","affiliation":[{"name":"Department of Pharmacy and Biotechnology University of Bologna  Bologna Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michele","family":"Anselmi","sequence":"additional","affiliation":[{"name":"Department of Chemistry \u201cG. Ciamician\u201d University of Bologna  Bologna Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9134-3161","authenticated-orcid":false,"given":"Luca","family":"Gentilucci","sequence":"additional","affiliation":[{"name":"Department of Chemistry \u201cG. 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