Alcaftadine - CAS 147084-10-4
Catalog number: 147084-10-4
Category: Inhibitor
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Histamine Receptor
Alcaftadine(R89674) is a H1 histamine receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis.
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1.Topical Olopatadine in the Treatment of Allergic Conjunctivitis: A Systematic Review and Meta-analysis.
Kam KW;Chen LJ;Wat N;Young AL Ocul Immunol Inflamm. 2017 Oct;25(5):663-677. doi: 10.3109/09273948.2016.1158282. Epub 2016 May 18.
PURPOSE: ;To assess the safety and efficacy of topical olopatadine versus placebo and other topical anti-allergic medications in treating allergic conjunctivitis.;METHODS: ;We systematically searched the literature for randomized-controlled trials that included patients with allergic conjunctivitis, compared olopatadine versus placebo or alternative anti-allergic medications, and examined itch, conjunctival hyperemia, composite symptom or sign scores, and/or occurrence of adverse events. We assessed the safety and efficacy of topical olopatadine when compared with placebo or alternative anti-allergic medications using meta-analysis.;RESULTS: ;When compared with placebo, topical olopatadine is associated with a pooled-mean difference (MD) in ocular itch of -1.33 (p < 0.00001) and ocular hyperemia of -0.92 (p < 0.00001). When compared with other agents, olopatadine was inferior to alcaftadine on ocular itch (pooled-MD = 0.39; p < 0.00001) but comparable with epinastine and ketotifen.;CONCLUSIONS: ;Topical olopatadine is a safe and effective treatment modality for allergic conjunctivitis, whereas alcaftadine appears to be superior to olopatadine in reducing ocular itch.
2.Polypharmacological in Silico Bioactivity Profiling and Experimental Validation Uncovers Sedative-Hypnotic Effects of Approved and Experimental Drugs in Rat.
Drakakis G;Wafford KA;Brewerton SC;Bodkin MJ;Evans DA;Bender A ACS Chem Biol. 2017 Jun 16;12(6):1593-1602. doi: 10.1021/acschembio.7b00209. Epub 2017 May 1.
In this work, we describe the computational ("in silico") mode-of-action analysis of CNS-active drugs, which is taking both multiple simultaneous hypotheses as well as sets of protein targets for each mode-of-action into account, and which was followed by successful prospective in vitro and in vivo validation. Using sleep-related phenotypic readouts describing both efficacy and side effects for 491 compounds tested in rat, we defined an "optimal" (desirable) sleeping pattern. Compounds were subjected to in silico target prediction (which was experimentally confirmed for 21 out of 28 cases), followed by the utilization of decision trees for deriving polypharmacological bioactivity profiles. We demonstrated that predicted bioactivities improved classification performance compared to using only structural information. Moreover, DrugBank molecules were processed via the same pipeline, and compounds in many cases not annotated as sedative-hypnotic (alcaftadine, benzatropine, palonosetron, ecopipam, cyproheptadine, sertindole, and clopenthixol) were prospectively validated in vivo. Alcaftadine, ecopipam cyproheptadine, and clopenthixol were found to promote sleep as predicted, benzatropine showed only a small increase in NREM sleep, whereas sertindole promoted wakefulness.
3.A multicenter evaluation of the efficacy and duration of action of alcaftadine 0.25% and olopatadine 0.2% in the conjunctival allergen challenge model.
Ackerman S;D'Ambrosio F Jr;Greiner JV;Villanueva L;Ciolino JB;Hollander DA J Asthma Allergy. 2013 Apr 8;6:43-52. doi: 10.2147/JAA.S38671. eCollection 2013.
BACKGROUND: ;The purpose of this study was to evaluate the efficacy and duration of action of once-daily dosing with alcaftadine 0.25% ophthalmic solution and olopatadine 0.2% ophthalmic solution as compared with placebo in the prevention of ocular itching, and to directly compare the efficacy of alcaftadine 0.25% with olopatadine 0.2% in the prevention of ocular itching associated with allergic conjunctivitis using the conjunctival allergen challenge model.;METHODS: ;Subjects with allergic conjunctivitis (n = 127) were enrolled in a multicenter, double-masked, randomized, active-controlled and placebo-controlled clinical trial. Using the conjunctival allergen challenge model, this study was conducted over the course of approximately 5 weeks. Subjects were randomized into one of three treatment arms: alcaftadine 0.25% ophthalmic solution, olopatadine 0.2% ophthalmic solution, or placebo. Study medications were administered twice over the course of the trial. The primary efficacy measure for the study was ocular itching evaluated by the subject at 3, 5, and 7 minutes post challenge. Secondary endpoints, measured at 7, 15, and 20 minutes post challenge, included conjunctival, ciliary, and episcleral redness, lid swelling, chemosis, and tearing.
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CAS 147084-10-4 Alcaftadine

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