Setastine
Chemical compound
title: "Setastine" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["h1-receptor-antagonists", "4-chlorophenyl-compounds", "ethers", "azepanes", "peripherally-selective-drugs", "ethanolamines"] description: "Chemical compound" topic_path: "general/h1-receptor-antagonists" source: "https://en.wikipedia.org/wiki/Setastine" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0
::summary Chemical compound ::
| IUPAC_name = 1-[2-[1-(4-chlorophenyl)-1-phenyl-ethoxy]ethyl]azepane | image = Setastine.png | image_class = skin-invert-image | image2 = Setastine-3D-balls.png | image_class2 = bg-transparent
| tradename = | pregnancy_category = | legal_status = | routes_of_administration =
| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =
| index2_label = HCl | CAS_number2_Ref = | CAS_number2 = 59767-13-4 | UNII2_Ref = | UNII2 = T2MB6P84ON
| CAS_number = 64294-95-7 | ATC_prefix = | ATC_suffix = | PubChem = 43082 | ChemSpiderID = 39258 | UNII_Ref = | UNII = 6G3OCF528J
| C=22 | H=28 | Cl=1 | N=1 | O=1 | smiles = CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCN3CCCCCC3
Setastine (Loderix) is an antihistamine used to treat allergies and rhinitis.
Pharmacology
Pharmacodynamics
Setastine acts as a highly selective H1 receptor antagonist. It has no anticholinergic, antiadrenergic, or antiserotonergic effects.
Pharmacokinetics
Setastine penetrates the blood-brain-barrier poorly so it is only mildly sedating compared to related molecules like diphenhydramine.
References
References
- (1991). "Loderix (setastine) tablets in the treatment of allergic rhinoconjunctivitis". Therapia Hungarica.
- (1989). "Results obtained with Loderix tablet in chronic rhinitis patients". Therapia Hungarica.
- (December 1990). "Pharmacology of the new H1-receptor antagonist setastine hydrochloride". Arzneimittel-Forschung.
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