Cimetidine competition with androgens for binding to human sex skin fibroblasts androgen receptors.
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Biomedical subjects
Publications and source records attributed to B Descomps.
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The fractional clearance K1 of bromsulphthalein was measured in twelve surgical patients at an interval of a least 48 hours. The first measurement was performed pre-operatively and the second postoperatively 24 hours after the operation, whilst the patients were receiving analgesia by the epidural injection of lignocaine at a constant flow rate. Between the two determinations there was a fall in BSP clearance of 25 +/- 11 p. 100 (range: -8 and -40 p. 100) P less than or equal to 0.0001. The clinical implications are discussed on the basis of concrete examples.
Prolactin and somatotrophin were measured during the postoperative period in two series of 15 patients after gynaecological surgery. Samples were collected for four days at the same times during the 24 hours period. The anesthetic given in the first group was a neuroleptanalgesia of dextromoramide-droperidol type followed by postoperative analagesia using a noramidopyrine compound. In the second group, epidural anaesthesia was given, followed postoperatively by the injection of lidocain at constant rate interrupted between the final two samples. In the neuroleptanalgesia group, from a basal levels of 11 micrograms.l-1, prolactin rose to 22 micrograms.l-1 on the evening after surgery (p less than 0.001) to subsequently stay on a plateau between 6 and 8 micrograms.l-1 (p less than 0.025 to p less than 0.005). From a basal level of 2.8 micrograms.l-1, somatotrophin rose to 9 micrograms.l-1 (p less than 0.05) then fell progressively from 7.5 to 2 micrograms.l-1 (NS on D1, D2, D3). In the epidural group, from a basal level of 13.5 micrograms.l-1, prolactin rose to 23 micrograms.l-1 on the evening after surgery (NS) to fall sharply on D1 to 5.6 micrograms.l-1 (p less than 0.01) and then follow a plateau on D2 and D3 of the order of 11 to 12 micrograms.l-1 (NS). From a basal level of 1.9 micrograms.l-1, somatotrophin rose to 10 micrograms.l-1 (p less than 0.001) to fall again to 4.5 micrograms.l-1 on D1 (p less than 0.01) and to 2 micrograms.l-1 on D2 and D3 (NS). Comparison of these two groups showed a difference only on D2 with regard to somatotrophin (p less than 0.05) and on D2 and D3 with regard to prolactin (p less than 0.025 and p less than 0.05). These results are discussed. They do not indicate any fundamental difference in the endocrine response to aggression in relation to the two types of anaesthetic studies.
The effect of DHT on skin fibroblasts proliferation was investigated by measurements of DNA concentrations and of 3H-thymidine incorporation variations. 1 nM DHT did not stimulate fibroblasts growth in either genital nor non genital skin fibroblasts. At higher concentrations, DHT inhibited cell proliferation. It can be concluded that in cell culture, fibroblasts growth is not dependent from androgen receptor content.
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Urinary estrone and estradiol levels have been measured using an enzymatic method during the late lutheal phase in 17 female volunteers trying for a pregnancy and in 10 patients having a treatment for stimulation of ovulation. The profile of urinary estrogenic excretion appears to be different if a pregnancy started or not during the studied cycle. These patterns allow a good diagnostic presumption before the following missing menses, which can be useful when dealing with women treated for infertility and when plasmatic dosage of hCG or beta hCG cannot be rapidly available.
Plasma prolactin was measured in six normal boys, during night sleep, with simultaneous recording of EEG for determination of the various stages of sleep. Peaks of prolactin appear clearly during cycles of rapid sleep: in prepuberty, the average of night peaks of prolactin is higher than that in post-puberty subjects. These results suggest indirectly, a participation of prolactin in prepuberty adrenal maturation.
Secretions of GH and of PRL studied over a period of 24 hours in 6 untreated Parkinson's patients showed slight changes. The normal secretion of PRL in the female shows no nocturnal increase in the male. The secretion of GH linked to sleep is identified in the male and not in the female. These variations related to sex are interpreted as an increase in those normally found in the adult and facilitated by age. Bromocriptine given continuously at a dose of 10 to 20 mg/day for periods of 20 days to 6 months, results in suppression or a marked decrease in the 24-hour secretion of PRL. It has virtually no effect upon the secretion of GH. These results show that the dopaminergic regulation of PRL is preserved in Parkinson's disease.
3-Chloroacetylpyridine--adenine dinucleotide phosphate is both active as a hydride acceptor and inactivates estradiol 17 beta-dehydrogenase. This coenzyme analogue behaves like an affinity label. The inactivation kinetics are discussed in relation to those observed with 3-chloroacetylpyridine--adenine dinucleotide. The pH dependence of the rate of inactivation, in combination with determination of the number of reactive cysteine residues, pointed to the alkylation of one cysteine residue/subunit. The stoichiometry was one molecule of dinucleotide per subunit and no cooperativity was detected. When 14C-labeled dinucleotide was used, the 14C label was found mainly in one peptide, accounting for 90% of the incorporated radioactivity, whereas in previous work it had been shown that 3-chloroacetylpyridine--adenine dinucleotide is an affinity reagent which labels three peptides.
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Plasma and urine estradiol and estrone can be determined using the transhydrogenase function of the estradiol dehydrogenase of human placenta: in the conditions described the transhydrogenase activity which is directly related to the estrogen concentration is measured by spectrophotometry. Estrone and estradiol can be determined together or separately if estrone is previously reacted with hydrazine with a limit of sensitivity of 10 picograms in the sample. On urine samples the assay is performed directly without extraction, a simplification which makes the method highly suitable for numerous routine determinations.
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154 surgical patients were given post-operative analgesia by peridural injection at a constant flow in the post-operative period after obstetric or gynecological surgery. These patients received 536.2 +/- 105.3 mu mol.h-1 (145.2 +/- 28.5 mg.h-1) of lignocaine for 46.97 +/- 15.56 h through a catheter omserted between L1-L2. The drug was given in concentrations which varied between: 27.7 to 18.5 m mol.l-1 (0.75 to 0.50 p. 100) depending on the age; and the volume varied between 17.5 to 30 ml.h-1 depending on the height. Satisfactory analgesia in 87 p. 100 of cases allowed all supplementary analgesia to be stopped. The only significant hemodynamic effect was a slight tachycardia (+ 15 p. 100). Two undesirable side effects were noted: a transitory but well-defined (type 2 or 3) motor paralysis, and an accumulation of plasma lignocaine (40 mu mol.l-1 (1.1 microgram.ml-1) at 48 h).
Before dialysis, acetate levels in hemodialyzed patients (0.27--1.1 mmol/1) were more dispersed than in normal subjects (0.20--0.65 mmol/l) and the mean value of plasma acetate was slightly higher (0.52 mmol/l versus 0.31 mmol/l). Though dialysis conditions were almost identical, the acetate kinetics during hemodialysis were very different: in most subjects, plasma acetate concentrations reached a "plateau" (mean value 5.6 mmol/l) whereas in others a continuous rise was observed, suggesting that with patients having chronic renal failure there were important individual or occasional differences in the ability to metabolize acetate. The acetate loads per minute (or mass transfers) were calculated from the blood compartment with plasma values (plasma flow and concentrations), rather than from the dialysate and using the combined calculations (plasma and whole blood values). The results ranged between 2.4 and 4.1 mmol/min. A very important and rapid fall in arterial acetate concentrations occurs in the first 20 min after the end of the dialysis and proves the rapid turnover of the acetate in man.