We use analytics and advertising cookies, which you can accept or reject; see our privacy policy.

Current choice:

Histamine Receptors

Histamine receptor antagonists and related ligands target H1 to H4, the four G protein-coupled receptors for histamine. H1 receptors mediate allergic and smooth muscle responses, whereas H2 receptors control gastric acid secretion. Black and colleagues defined the H2 receptor in 1972 as a histamine receptor that classic H1 antagonists failed to block. The H3 receptor acts mainly as a presynaptic autoreceptor in the brain, and its human gene was cloned in 1999. H4, the most recently described subtype, is expressed largely on immune cells. Ligands here include the H1 antagonist chlorpheniramine maleate and the H2 antagonist cimetidine. Ciproxifan blocks H3, while JNJ7777120 is a widely used H4 antagonist.

1 Item

  • Terfenadine
    Cat. No.
    A17373
    CAS No.
    50679-08-8

    Terfenadine

    Synonyms: BRN 5857899; Seldane; Terfen

    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 and induces p73, Noxa.

    In stock View Details
    50 mg
    $30.00
    100 mg
    $45.00
    All 5 sizes

1 Item

Added to your cart

View Cart Checkout

    Loading...