68844-77-9 Category:
  • #LGM Pharma is a Astemizole CAS# 68844-77-9 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
  • #Questions? Call our customer API support number 1-(800)-881-8210.
  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 68844-77-9
  • AHFC code:
  • Synonyms:
  • ATC Code: R06AX11
  • Chemical Formula: C22H29FO5
  • Molecular Weight: 458.5703
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00637 (APRD00585)
  • PubChem: 2247
  • IUPAC: 1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine

Additional Details

Astemizole was indicated for use in the relieving allergy symptoms, particularly rhinitis and conjunctivitis. It has been withdrawn from the market however due to concerns of arrhythmias.
Astemizole is a second generation H1-receptor antagonist. It does not significantly cross the blood brain barrier and therefore does not cause drowsiness or CNS depression at normal doses.
Mode of Action:
Astemizole competes with histamine for binding at H_-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. This reversible binding of astemizole to H_-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. As the drug does not readily cross the blood-brain barrier and preferentially binds at H_ receptors in the peripehery rather than within the brain, CNS depression is minimal. Astemizole may also act on H_-receptors, producing adverse effects.
Almost completely metabolized in the liver and primarily excreted in the feces.
LD50=2052mg/kg in mice
General Reference:
Wang X, Hockerman GH, Green HW 3rd, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL: Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J. 2006 Jul;20(9):1531-3. Epub 2006 May 24. Pubmed Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr: A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2. Pubmed
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