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Biomedical subjects

J Couquelet

Publications and source records attributed to J Couquelet.

At least 55 records · Page 3Linked to original sources
PubMed1985

Enhanced prostacyclin biosynthesis and decreased thromboxane formation by 3-dimethylamino 5-(2',6'-dichlorobenzylidene) 6-methyl (4H)-pyridazine (PC 89).

The effects of 3-dimethylamino 5-(2',6'-dichlorobenzylidene) 6-methyl (4H)-pyridazine (PC 89) on the biosynthesis of PG I2 and TX A2 using horse aorta and horse platelet microsomes as sources of enzymes and arachidonic acid as substrate, were investigated. PC 89 (1.10(-6) M- 1.10(-3) M) dose-dependently - enhanced the biosynthesis of PG I2: the AD50 was 6.8 X 10(-6) M +/- 1.2 X 10(-9) M, the Vmax did not vary significantly with concentrations: PC 89 increased the affinity of enzyme for substrate - but inhibited TX A2 biosynthesis (ID50 = 3.31 X 10(-3) M +/- 4.8 X 10(-7) M): this inhibiting action was not of competitive type. Owing to this dual activity of preventing TX A2 formation and stimulating PG I2 biosynthesis, PC 89 could be a valuable drug for myocardial ischemia and atherosclerosis therapeutics.

Animals↗
PubMed1985

[Synthesis and pharmacologic study of 6-(amino-2 ethyl) benzoxazolinones].

Reaction of various amines on 6-(2-bromoethyl)benzoxazolinone or its N-methylated derivative provided eleven new 6-substituted aminoalkyl analogues. In a pharmacological evaluation, several compounds bearing an arylpiperazinic moiety were found to possess significant effects on arterial blood pressure and on the central nervous system; two of them showed interesting analgesic activity.

Analgesics↗
PubMed1981

Comparative blood level of dihydroergotoxine (DHET) after administration of two oral forms (solution & tablet): a preliminary study.

In this preliminary study, using a radioimmunoassay, we demonstrate that the DHET blood levels observed after administration of an oral solution to human subjects, were different from those obtained after administration of a slow-release table. After administration of the oral solution, the DHET blood levels rose quickly, reached a peak between 1 and 2 hours and the decrease rapidly. On the contrary, after ingestion of a slow-release tablet of DHET, the plasma levels took 6 hours to reach the maximum due to the slow release of the drug from this dosage form. In both cases, the areas under the curves were very similar but the relative bioavailability of DHET in these two forms is very different if one considers the two components of availability extent and rate. The equality of the areas under the curves indicated that the extent of DHET available was the same, but time-course of the plasma levels showed that the rate at which DHET became available was significantly slower. Therefore the tablet form has given the desired "slow-release" availability for which it was designed.

Administration, Oral↗
PubMedDate not supplied

[Synthesis and evaluation of the aldose reductase inhibitory activity of new diaryl pyridazine-3-ones].

It has been possible to prepare from 4,6-diaryl pyridazinones a series of derivatives substituted in the 2-position by chains of various lengths bearing a carboxylic acid function. Pig lens aldose reductase inhibitory activity was evaluated for all compounds. N-acetic acid derivative 3c with a chlorine atom on the phenyl nucleus at the 6-position on the pyridazin ring was the most active pyridazinone with an IC50 value of 1.2 x 10(-5) M. Furthermore, it has been shown that lipophilicity and spatial configuration of the synthesized compounds took a prominent part on enzymatic activity.

Aldehyde Reductase↗
PubMedDate not supplied

Synthesis of 6-[(4-imidazol-1-yl)-phenyl]-4-phenyl 4,5-dihydro-2H-pyridazin-3-one: a potential blood platelet aggregation inhibitor.

A new 4,5 diaryl pyridazin-3-one, an analogue of imazodan and Cl-930 was prepared starting from conveniently available chalcone. The resulting derivative was tested in order to determine the area of pharmacological activity. This compound was devoid of positive inotropic effects but showed an important inhibition of PAF-acether induced blood platelet aggregation in vitro with a Cl50 value of 3,4 microM. Ex vivo, anti-aggregating effect against PAF-acether was less important with a DE50 value of 63 mg/kg per os.

Animals↗