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)
| Molecular Formula | C16H22ClN3O4 |
| Molecular Weight | 355.817 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|---|---|---|
| Activity of plafibride on erythrocyte deformability. | 1983 |
|
| Bioavailability of plafibride in healthy volunteers. | 1981 |
|
| Plafibride tolerance trial in healthy volunteers. | 1981 |
|
| Plafibride tolerance trial at increasing doses in healthy volunteers. | 1981 |
|
| Toxicological studies of plafibride. Part 4: Interaction of plafibride with other drugs. | 1981 |
|
| Toxicological studies of plafibride. Part 3: Study of teratogenic activity in rats and rabbits. | 1981 |
|
| Toxicological studies of plafibride. Part 2: Subacute and subchronic toxicity in rats and chronic toxicity in dogs. | 1981 |
|
| Toxicological studies of plafibride. Part 1: Acute toxicity and its determination after several administrations of plafibride. | 1981 |
|
| Pharmacokinetic approach of plafibride in rat. | 1981 |
|
| Clinical research into the hypolipemic and platelet antiaggregant activity of plafibride, Carried out in double-blind conditions and in comparison with clofibrate. | 1981 |
|
| Double-blind study on the activity of plafibride in the treatment of type IV hyperlipoproteinemia. | 1981 |
|
| Plafibride: clinical trial of a new platelet antiaggregating agent. | 1981 |
|
| Bacterial mutation test on plafibride. | 1981 |
|
| Pharmacological activities and side effects of plafibride. | 1981 |
|
| Platelet antiaggregant activity of plafibride ex vivo in rat, dog and rabbit. | 1981 |
|
| Synthesis and pharmacological evaluation of N'-morpholinomethylurea derivatives with platelet antiaggregant activity. | 1981 |
|
| Influence of plafibride, an antiplatelet and hypolipemic agent, on prostacyclin and thromboxane synthesis, 3',5'-cyclic AMP phosphodiesterase activity and serum clearance of a lipid emulsion. | 1981 |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:04:08 GMT 2025
by
admin
on
Mon Mar 31 18:04:08 GMT 2025
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| Record UNII |
5J7C4JZ564
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| Record Status |
Validated (UNII)
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| Record Version |
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NCI_THESAURUS |
C98150
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100000081911
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m8900
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CHEMBL2107129
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C66444
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ACTIVE MOIETY |