Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H22ClN3O4 |
Molecular Weight | 355.817 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(OC1=CC=C(Cl)C=C1)C(=O)NC(=O)NCN2CCOCC2
InChI
InChIKey=DDDQVDIPBFGVIG-UHFFFAOYSA-N
InChI=1S/C16H22ClN3O4/c1-16(2,24-13-5-3-12(17)4-6-13)14(21)19-15(22)18-11-20-7-9-23-10-8-20/h3-6H,7-11H2,1-2H3,(H2,18,19,21,22)
Plafibride is an acyl derivative of morpholinomethylurea (MMU) with clofibric acid. Plafibride is hypolipemic, platelet aggregation inhibiting agent. Plafibride did not act on the arachidonic acid metabolism. Plafibride inhibited the activity of 3',5'-cyclic AMP-phosphodiesterase, which is one of the principal mechanisms of inhibition of platelet aggregation. In the rat, plafibride inhibited significantly the spontaneously formed circulating platelet aggregates. In vitro plafibride appeared as an effective antiaggregant agent although less powerful than morpholinomethylurea, one of its presumed metabolites. The most evident secondary effects of plafibride were: a certain sedation, as a light tranquilizing agent, a hypothermic effect when it was administered at high doses, a certain beta-blocking and antiarrhythmic activity probably due to its local anesthetic action. All the side effects appeared at high doses, much higher than the therapeutic ones.
Approval Year
PubMed
Title | Date | PubMed |
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Bioavailability of plafibride in healthy volunteers. | 1981 |
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Plafibride tolerance trial at increasing doses in healthy volunteers. | 1981 |
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Toxicological studies of plafibride. Part 1: Acute toxicity and its determination after several administrations of plafibride. | 1981 |
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Clinical research into the hypolipemic and platelet antiaggregant activity of plafibride, Carried out in double-blind conditions and in comparison with clofibrate. | 1981 |
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Double-blind study on the activity of plafibride in the treatment of type IV hyperlipoproteinemia. | 1981 |
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Plafibride: clinical trial of a new platelet antiaggregating agent. | 1981 |
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Bacterial mutation test on plafibride. | 1981 |
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Synthesis and pharmacological evaluation of N'-morpholinomethylurea derivatives with platelet antiaggregant activity. | 1981 |
Patents
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NCI_THESAURUS |
C98150
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ACTIVE MOIETY