Home Transmembrane Transporters Potassium Channel inhibitor - Histamine Receptor antagonist - Caspase activator - Calcium Channel modulator - NCX inhibitor Terfenadine For research use only.

Terfenadine

Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. 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.

Terfenadine Chemical Structure

Terfenadine Chemical Structure

CAS No. 50679-08-8

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Terfenadine Related Products

Signaling Pathway

Potassium Channel Signaling Pathways

Potassium Channel Signaling Pathway

Biological Activity

Description Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. 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.
Targets
Caspase-4 [6] Caspase-2 [6] Caspase-9 [6] Ca2+ homeostasis [6] H1 histamine receptor [6] Click to View More Targets
In vitro
In vitro

Terfenadine is equipotent to quinidine as a blocker of the delayed rectifier potassium current in isolated feline myocytes. [1] Terfenadine inhibits the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fashion. [2] Terfenadine (2 μM) blocks the steady-state maximum current at 0 mV by 65% in Xenopus oocytes. Terfenadine block is dose dependent and equally potent on the maximal steady-state and tail currents, its Kd values are 350 nM and 390 nM, respectively. Terfenadine blocks Kv1.5 (a member of the Kv1 subfamily of voltage-dependent K+ channels) in human atrial myocytes and in the human embryonic kidney cell expression system. Terfenadine (10 μM) produces a dose-dependent block with a 60% reduction of steady-state current in Xenopus oocytes. [3] Terfenadine is oxidated into oxidative N-dealkylation to 4-(hydroxydiphenylmethyl)-piperidine and oxidation of a tert-butyl methyl group to a primary alcohol, which is subsequently oxidized to a carboxylic acid, which is markedly inhibited by gestodene, a selective mechanism-based inactivator of P-450 3A enzymes but not by any of several other P-450 inhibitors. [4] Terfenadine significantly increases action potential duration of guinea pig myocytes. Terfenadine potently blocks the rapidly activating component of the delayed rectifier, IKr, with IC50 values of 1.5 nM and 50 nM, respectively. Terfenadine (10 μM) blocks the slowly activating component of the delayed rectifier, IKs (58.4%), and the inward rectifier, IK1 (20.5%). [5]
In Vivo
In vivo

Terfenadine (1.0 to 3.0 mg/kg, i.v.) significantly prolongs the QTc interval and ventricular effective refractory period in chloralose-anesthetized dogs. [5]

Chemical Information & Solubility

Molecular Weight 471.67 Formula

C32H41NO2
CAS No. 50679-08-8 SDF Download Terfenadine SDF
Smiles CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (199.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 27 mg/mL

Water : Insoluble


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