A selective histamine H1-receptor antagonist
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Active Metabolite(s)
27303Azacyclonol 18191Fexofenadine (hydrochloride)
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Terfenadine

Item No. 20305

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
CAS Number
50679-08-8
Synonyms
  • MDL 9918
  • NSC 665802
  • (±)-Terfenadine
  • DL-Terfenadine
Molecular Formula
C32H41NO2
Formula Weight
471.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.33 mg/mlDMSO: 10 mg/mlEthanol: 0.25 mg/ml
SMILES
CC(C)(C)C1=CC=C(C(O)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2)C=C1
InChi Code
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
InChi Key
GUGOEEXESWIERI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 mg

    $36

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    1 g

    $61

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    5 g

    $96

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    Product Description

    Terfenadine is a selective histamine H1-receptor antagonist with anti-allergic effects that lacks central nervous system depressant activity.1 It is a prodrug that undergoes extensive first-pass hepatic metabolism by the cytochrome P450 enzyme CYP3A4 to its pharmacologically active metabolite fexofenadine (Item No. 18191).2 Terfenadine is reported to be cardiotoxic, inducing QT interval prolongation by blocking cardiac potassium channels.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Baroody, F.M., and Naclerio, R.M. Antiallergic effects of H1-receptor antagonists. Allergy 55(Suppl 64), 17-27 (2000).

    2. Amichai, B., Grunwald, M.H., and Brenner, L. Fexofenadine hydrochloride--a new anti-histaminic drug. Isr. Med. Assoc. J. 3(3), 207-209 (2001).

    3. Zünkler, B.J., Kühne, S., Rustenbeck, I., et al. Mechanism of terfenadine block of ATP-sensitive K+ channels. Br. J. Pharmacol. 130(7), 1571-1574 (2000).