NO donors. Part 18: Bioactive metabolites of GTN and PETN--synthesis and vasorelaxant properties.
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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
Drug Target Kind Organism Pharmacological Action Actions Erythrityl tetranitrate Atrial natriuretic peptide receptor 2 Protein Humans YesAgonistDetails