Biomedical subjects
Publications and source records attributed to M Leinot.
The synthesis of various 6-(4-arylpiperazino-butyryl)-3-methyl-benzoxazolinones and their reduction products, 6-(4-arylpiperazino-1-hydroxy-butyl)-3-methyl-benzoxazolinones and 6-(4-arylpiperazino-butyl)-3 methyl-benzoxzolinones, is described. These compounds were tested for psychotropic and analgesic activities.
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Acute myocardial ischemia was produced by ligature of the anterior descending coronary artery on 658 dogs in 3 separate laboratories. Overall, 12% of the dogs died within the first hour (instantaneous death) and 25% within the first 24 hours (sudden death). The sudden death rate was significantly related to the logarithm of the weight of the dogs in the range studied. It varied widely if values from small series, comprising the same number of dogs, were considered. Values became less dispersed as the size of the series increased. In series of 10 dogs, sudden death rates ranged from 0 to 70%, whereas in series of 100 dogs the range was 14 to 36%. Stable values were obtained for 50 to 60 dogs per series. Accordingly, reliable assessment of preventive measures can be made only with experimental series of at least this size.
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.
The effects of bepridil, nifedipine, verapamil, lignocaïne and amiodarone on the atrial effective refractory period were investigated in the guinea-pig. The observed results permitted elucidation of a remarkable activity by both nifedipine and verapamil, and by bepridil and lignocaïne. In contrast, in the experimental conditions, no activity was detected with amiodarone up to concentrations of 10(-4) M. The efficacity rating of the test compounds is not reflected by their anti-arrhythmic efficacity as demonstrated in vivo in the animal, nor by their therapeutic anti-arrhythmic efficacity as reported in the clinical literature. However, this efficacity rating may be related to the interaction of the compounds with the transmembrane sodium or calcium movements.
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Preparation of the N-(2-diethylaminoethyl) derivatives of lactam (II) and of the N-(3-dimethylaminopropyl) derivative of lactam (XI) is described. Synthesis of the N-[4-(2-hydroxyethyl)piperazinylacetyl]- and 1-carbothiamide derivatives of azepine (I) and of the n-(chloroformyl)- and N-(carbamoyl) derivatives of azepine (XII) are also described. Some pharmacological results indicate a partial tranquilizing activity.
A method for frequent sampling of blood and injections of fluids in undisturbed rats is described. The right external jugular vein and the left carotid artery are cannulated without completely blood stream interruption in the vessel. Injection or perfusion can be performed during several weeks. Blood was collected for at least 15 post-operative days. The technique appears suitable for pituitary kinetics studies which can be carried out several times in rats bearing indwelling catheters.
Rats with permanent intra-jugular cannula are submitted to an alimentary operant reinforcement schedule with fixed ratio type FR 1, FR5, then FR 20. As a result, the animals are self administering (together with the alimentary inducer) a slow (about 5 sec) intravenous infusion of morphine (0.05 mg/kg). 20 per cent only of the experimental population exhibit a psychogenic dependance afterward. On the other hand, the animals for which morphine self-administration has been substituted to the alimentary reinforcement without respecting a transitory period combining both types of reinforcement have never shown any tendancy toward morphine self-administration. The lack of positive results could be related to the marked duration of the self-injection.
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