1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. N-Demethyldiltiazem

N-Demethyldiltiazem is a metabolite of Diltiazem (HY-B0632). N-Demethyldiltiazem increases coronary blood flow, modulates cardiac function, decreases systemic blood pressure and heart rate, and alters papillary muscle developed tension.

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N-Demethyldiltiazem

N-Demethyldiltiazem Chemical Structure

CAS No. : 86408-45-9

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Description

N-Demethyldiltiazem is a metabolite of Diltiazem (HY-B0632). N-Demethyldiltiazem increases coronary blood flow, modulates cardiac function, decreases systemic blood pressure and heart rate, and alters papillary muscle developed tension[1][2].

In Vitro

N-Demethyldiltiazem is a major N-monodemethylated metabolite of Diltiazem (HY-B0632)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

N-Demethyldiltiazem (15-500 μg/kg; i.v.; single dose) produces dose-dependent coronary vasodilation, hypotension, and increased left ventricular dP/dtmax in anesthetized open-chest mongrel dogs[1].
N-Demethyldiltiazem (1.5-1500 μg; i.a.; single dose or 1 μg/min; continuous infusion; 20 minutes) produces dose-dependent coronary vasodilation with minimal negative inotropic effects in blood-perfused canine papillary muscles[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mongrel dogs (male, 12-22 kg, anesthetized, open-chest preparation)[1]
Dosage: 15, 50, 150, 500 μg/kg
Administration: i.v.; single dose
Result: Increased coronary blood flow and left ventricular dP/dt_max, and decreased blood pressure, left ventricular pressure, and heart rate, with effects lasting ~10 minutes.
Exhibited a relative potency of 1/5 for inducing a 50% increase in coronary blood flow, and 1/3 for inducing a 10% decrease in mean blood pressure, relative to Diltiazem (potency 1).
Caused a <10% decrease in mean blood pressure at doses that increased coronary blood flow by 50%.
Molecular Weight

400.49

Formula

C21H24N2O4S

CAS No.
SMILES

CC(O[C@@H]1[C@H](C2=CC=C(C=C2)OC)SC3=CC=CC=C3N(C1=O)CCNC)=O

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N-Demethyldiltiazem
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HY-183138
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