NO donors. Part 18: Bioactive metabolites of GTN and PETN--synthesis and vasorelaxant properties.

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Citation

Lange K, Koenig A, Roegler C, Seeling A, Lehmann J

NO donors. Part 18: Bioactive metabolites of GTN and PETN--synthesis and vasorelaxant properties.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3141-4. doi: 10.1016/j.bmcl.2008.04.057. Epub 2008 Apr 26.

PubMed ID
19406636 [ View in PubMed
]
Abstract

The vasodilators glyceryl trinitrate (GTN) and pentaerythrityl tetranitrate (PETN) are supposed to be degraded in vivo to the lower nitrates PETriN, PEDN, PEMN, 1,2-GDN, 1,3-GDN, 1-GMN, and 2-GMN. We synthesized these bioactive metabolites as reference compounds for pharmacokinetic studies. The use of HPLC-methods for monitoring the stepwise reduction of PETN to lower nitrates and the syntheses of the glyceryl dinitrates proved advantageous. Furthermore, we measured the vasorelaxant properties of all metabolites by performing organ bath experiments with porcine pulmonary arteries. In general, the vasodilator potency increases with the number of nitrate moieties in the compound.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Erythrityl tetranitrateAtrial natriuretic peptide receptor 2ProteinHumans
Yes
Agonist
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