epsilon-Aminocaproylcholine: chemical synthesis, biological properties, and interactions with receptor molecules.
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Biomedical subjects
Publications and source records attributed to C Marchand.
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An acyl-CoA-L-alpha-glycerophosphate acyltransferase system has been found in the fat body of the locust Schistocerca gregaria (Forskäl). After homogenization and differential centrifugation the enzyme system has been localized in two distinct particulate fractions. In both fractions phosphatidic acid was the main reaction product. The 10 000 g -30 000 g particulate fraction was further studied. The enzyme system is very sensitive to pH and Mg2+ concentration. An apparent Km of 0.3-0.5 mM for glycerophosphate was measured. The substrate concentration curve for palmitoyl-CoA is influenced by the protein concentration in the assay medium. This effect would partly explain the non-lineariy of the acylation reactions with respect to enzyme concentration. These observations are correlated with physiological phenomena.
A new method is proposed in order to appreciate the potency of some volatile anaesthetics and toxics in vapour phase. The method is founded upon the classical concept of thermodynamic activity and on the reversible inhibition of bacterioluminescence tested in vapour phase. Deprived of all experimental inertia the method allows very precise kinetic studies of the various types of inhibition.
1 During the first 90 min following oral administration of sulphacetamide, there was a rapid decline in plasma drug concentration in control mice whereas a progressive increase in sulphacetamide concentration was observed in leukaemic mice. 2 Similar changes in the kinetics of sulphacetamide distribution were observed in the liver, spleen and muscle. 3 While the concentration of sulphacetamide remained quite constant in the brain and fat tissue of control mice, a progressive increase in drug concentration was observed in the brain and fat tissue of leukaemic mice. 4 Some of these changes in the kinetics of sulphacetamide tissue distribution are compatible with delay in gastrointestinal absorption of the drug and its accumulation in the ascitic fluid.
Among 142 high-risk-newborns, 111 could be regularly followed-up to 3 years of age. 79 (71%) are normal, 6 (5.5%) have minor neurological sequels, 9 (8.1%) have major neurological sequels, associated in 4 cases with mental deficiency, 16 (14.5%) have developmental abnormalities (speech delay, behavioral problems, perceptual-motor and praxis disturbances), and one mental deficiency without neurological sequels. Neonatal cerebral distress proved to be the most dangerous clinical situation with regard to the ultimate neurodevelopmental prognosis (73.6% of neurological sequels or developmental abnormalities). The presence of transient abnormalities of tone in the course of the first year of life was associated with ultimate developmental abnormalities in 33.3% of the cases. Social and cultural status seemed to play a role in the intellectual, linguistic and perceptual-motor performance of this group of infants. In spite of these encouraging results, the need for a systematic long term follow-up of high risk newborns is stressed, since neurological sequels and developmental abnormalities are approximately 4 times more frequent in this group than in a normal infantile population.
The history of 90 full-term infants with neonatal cerebral distress was examined. Informations concerning pregnancy, delivery, neonatal status, clinical and laboratory evolution were compared with final outcome in each case. It was then possible to distinguish certain clinical features significantly associated with poor prognosis. After statistical analysis, different adverse criteria were selected, such as severe neonatal asphyxia, associated respiratory disorders, acute anemia, and especially neurological signs with regard to their chronology. This part of the study has resulted in a classification of the neurological signs and has permitted the description of both malignant and benign cerebral distress syndromes.
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1. Administration of 2-diethylaminoethyl-2,2-diphenylvalerate hydrochloride (SKF 525-A), 40 mg/kg, i.p., simultaneously or 40 min before sulphacetamide sodium, 100 mg/kg, i.p., was associated with a three-fold increase in sulphacetamide plasma concentration of rats. This effect was no longer evident after 30 minutes.2. The augmentation in sulphacetamide plasma concentration was associated with parallel increases in the muscle, kidney and brain tissue. The stomach was the only organ that contained less sulphacetamide.3. When sulphacetamide was administered i.v., a similar phenomenon was observed but the differences were less marked.4. Pretreatment with SKF 525-A was associated with decreased excretion of sulphacetamide by the kidney.5. It is concluded that SKF 525-A may alter the distribution and excretion of drugs as well as inhibiting drug metabolizing enzymes.
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