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Astemizole

CAS No:
68844-77-9 Category:
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Product Details:

  • Product Name: Astemizole
  • CAS #: 68844-77-9
  • 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.

  • Pharmacodynamics:

    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.

  • Metabolism:

    Almost completely metabolized in the liver and primarily excreted in the feces.

  • Toxicity:

    LD50=2052mg/kg in mice

  • IUPAC: 1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1, 3-benzodiazol-2-amine
  • ATC: R06AX11
  • PubChem: 2247
  • DrugBank: DB00637 (APRD00585)
  • Formula: C22H29FO5
  • Molecular Mass: 458.5703
  • SMILES: COC1=CC=C(CCN2CCC(CC2)NC2=NC3=CC=CC=C3N2CC2=CC=C(F)C=C2)C=C1
  • InChl: GXDALQBWZGODGZ-UHFFFAOYSA-N
  • General Reference:

    1. 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
    2. 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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