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Details

Stereochemistry ACHIRAL
Molecular Formula C20H29N5O3
Molecular Weight 387.476
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUQUINERAN

SMILES

CCCCNC(=O)NC1CCN(CC1)C2=C3C=C(OC)C(OC)=CC3=NC=N2

InChI

InChIKey=CPZHDDGPHQRMEJ-UHFFFAOYSA-N
InChI=1S/C20H29N5O3/c1-4-5-8-21-20(26)24-14-6-9-25(10-7-14)19-15-11-17(27-2)18(28-3)12-16(15)22-13-23-19/h11-14H,4-10H2,1-3H3,(H2,21,24,26)

HIDE SMILES / InChI

Description

Buquineran (UK14275), an inotropic compound, is a coronary vasolidator agent. It has been shown to exert a powerful inotropic effect with minimal effect on heart rate in dogs. Buquineran is a phosphodiesterase inhibitor. It acted as potent inhibitor of cyclic AMP hydrolysis catalysed by both PDE-II and PDE-III enzymes.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
7.6 µM [IC50]

PubMed

Sample Use Guides

In Vivo Use Guide
Electrophysiological and haemodynamic measurements were made in six dogs over successive 30 min periods under control conditions and during infusion of Buquineran at 50, 100 and 250 ug/kg per min (infusion rates 0.91, 1.82 and 4.55 ml/min), respectively.
Route of Administration: Intravenous
In Vitro Use Guide
Buquineran inhibited PDE-II and PDE-III activity with IC50 value of 7.6 uM and 8.6 uM, respectively.