| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H24N4O4 |
| Molecular Weight | 360.4076 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCNC(=O)OC1CCN(CC1)C2=NN=CC3=C2C=C(OC)C(OC)=C3
InChI
InChIKey=QJGVXJYGDBSPSJ-UHFFFAOYSA-N
InChI=1S/C18H24N4O4/c1-4-19-18(23)26-13-5-7-22(8-6-13)17-14-10-16(25-3)15(24-2)9-12(14)11-20-21-17/h9-11,13H,4-8H2,1-3H3,(H,19,23)
Carbazeran is a potent PDE-II and PDE-III inhibitor. Potently inhibits cAMP hydrolysis. Shows chronotropic and inotropic effect in vivo (EC50 = 100 μM, ionotropic effects, independent of adrenergic mechanisms). Carbazeran is a potent cardiac stimulant. Phosphodiesterase inhibition and elevation of intracellular cyclic AMP concentration may be involved, at least in part, in carbazeran`s cardiac effect.
Approval Year
PubMed
Patents
Sample Use Guides
When administered orally to the dog at a dose level of 5mg/kg the compound elicits a marked inotropic response, causing a 60% increase in the maximum rate of pressure change during systole measured via an indwelling pressure transducer in the left ventricle. When administered by i.v. infusion to human subjects at
dose levels up to 1.28 mg/kg a dose-related increase in myocardial contractility was observed, judged from changes in systolic time intervals. However, when human volunteers received single oral doses of up to 350mg (i.e.
approximately 5 mg/kg) no effects on the heart or circulation were observed.
Route of Administration:
Other
ACTIVE MOIETY
METABOLITE (PARENT)
