1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    Metabolic Enzyme/Protease
  2. Calcium Channel
    Drug Metabolite
  3. Norverapamil

Norverapamil (Synonyms: (±)-Norverapamil; D591)

Cat. No.: HY-135328
Handling Instructions

Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

For research use only. We do not sell to patients.

Norverapamil Chemical Structure

Norverapamil Chemical Structure

CAS No. : 67018-85-3

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Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].

IC50 & Target

Calcium channel blocker[1]
P-glycoprotein (P-gp) inhibitor[2]

In Vitro

Norverapamil ((±)-Norverapamil) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil[1].
Verapamil and its major metabolite Norverapamil were identified to be both mechanism-based inhibitors and substrates of CYP3A and reported to have non-linear pharmacokinetics in clinic[3].

In Vivo

Norverapamil (9 mg/kg; p.o.), a major metabolite of verapamil, has terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng▪h/ml, and 41.6 ng/mL, respectively[4].

Animal Model: Male Sprague-Dawley rats[4]
Dosage: 9 mg/kg (Pharmacokinetic Study)
Administration: Oral administration
Result: t1/2=9.4 hours; AUC=260 ng▪h/mL; Cmax=41.6 ng/mL.
Molecular Weight









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Norverapamil(±)-NorverapamilD591D 591D-591Calcium ChannelP-glycoproteinDrug MetaboliteCa2+ channelsCa channelsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243metabolitemycobacterialeffluxpumpsM. tuberculosisInhibitorinhibitorinhibit

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