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Restrict the search for
glycerol phenylbutyrate
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Glyceryl 2-nitrate (G-2-N) is the major metabolite of glyceryl trinitrate. Strips of rat aorta contracted with potassium chloride or with norepinephrine were relaxed by G-2-N. After oral administration to the anaesthetized rat or to the conscious dog G-2-N exhibited antianginal and hypotensive activity. The hypotensive and also cardiovascular activity of G-2-N lasted much longer than that of glyceryl trinitrate.
Glyceryl 1-nitrate (G-1-N) is an intermediate metabolic product in the stepwise de-esterification of glyceryl trinitrate (GTN) in animals and humans. It belongs to the group of orally effective longacting antianginal nitrates. In anesthetized rabbits, intravenous (L) G-1-N reduced the blood pressure slightly more than (D) G-1-N, while in the conscious dog the blood pressure lowering effect of (D) G-1-N was greater and had a much longer duration (4-6 versus 2 h) than that of (L)G-1-N. The differences in dogs are probably explained by enantiospecific pharmacokinetics: (D) G-1-N had higher plasma levels and showed a longer half-life of elimination than (L) G-1-N. From the pharmacokinetic point of view, the drug offers clear advantage over glyceryl trinitrate in clinical use: G-1-N is orally available - owing to its relatively low clearance it stays much longer in the body than GTN - kinetic parameters are predictable with low coefficients of variation - and the denitration products of G-1-N are expected to be pharmacologically neutral.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Glyceryl 1-phosphate,(S)- or glycerol-1-phosphate is a glycerophosphate backbone of the archeal ether lipids. It results from the reduction of dihydroxyacetone phosphate using NADH (or NADPH) and divalent ions as cofactors. Two different enzymes carry out the condensation of the isoprenoid chains to the glycerophosphate backbone in archea. The first ether linkage that brings together glycerol-1-phosphate and geranylgeranyl diphosphate is catalyzed by a cytoplasmic protein geranylgeranylglyceryl diphosphate (GGGP) synthase.
