Setastine

Setastine (Loderix) is an antihistamine used to treat allergies and rhinitis.[1][2]

Setastine
Identifiers
IUPAC name
  • 1-[2-[1-(4-chlorophenyl)-1-phenyl-ethoxy]ethyl]azepane
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC22H28ClNO
Molar mass357.92 g·mol−1
3D model (JSmol)
SMILES
  • CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCN3CCCCCC3

Pharmacology

Pharmacodynamics

Setastine acts as a highly selective H1 receptor antagonist.[3] 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.[3]

See also

References

  1. Lantos A; Tóth A; Zsiray M (1991). "Loderix (setastine) tablets in the treatment of allergic rhinoconjunctivitis". Therapia Hungarica (English Edition). 39 (1): 22–4. PMID 1677500.
  2. Hirschberg A; Ribári O; Krasznai M (1989). "Results obtained with Loderix tablet in chronic rhinitis patients". Therapia Hungarica (English Edition). 37 (4): 202–4. PMID 2576575.
  3. Porszász J, Varga F, Porszász KG, et al. (December 1990). "Pharmacology of the new H1-receptor antagonist setastine hydrochloride". Arzneimittel-Forschung. 40 (12): 1340–5. PMID 1982751.


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