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Biomedical subjects

C Lemaire

Publications and source records attributed to C Lemaire.

14 recordsLinked to original sources
PubMed1992

2- and 4-[18F]fluorotropapride, two specific D2 receptor ligands for positron emission tomography: N.C.A. syntheses and animal studies.

Tropapride, (exo)-2,3-dimethoxy-N-[8-(phenylmethyl)-8- azabicyclo[3.2.1]oct-3-yl]benzamide hydrochloride, has been labeled with fluorine-18 at the 2- and 4-positions of its benzylic group. Two synthetic pathways were investigated: the first one required the alkylation of the norbenzyl precursor with 2- or 4-[18F]fluorobenzyl bromide (radiochemical yield of 5% EOB, 180 min); the second method consisted of a reductive amination of norbenzyl tropapride with 2- or 4-[18F]fluorobenzaldehyde (20% EOB, 110 min). In both cases, the specific activity was found to be greater than 1 Ci/mumol (EOS). Animal studies in rats showed the percentage of the injected dose localizing in the whole brain to be 0.6 +/- 0.09 and 0.2 +/- 0.03 at 2 h post injection for the para- and the ortho-[18F]fluoro analogs of tropapride respectively. Cerebral biodistribution studies showed at 4 h a striatum uptake of 5 +/- 0.7% of the injected dose per gram of striatum for the para derivative with a low fixation into the frontal cortex and the cerebellum (% ID/g FC < 0.4 and % ID/g Cb < 0.3). The selectivity of 4-[18F]fluorotropapride for D2 dopaminergic sites was demonstrated through blocking experiments with ketanserin, spiperone and halopemide. The saturability was confirmed by the use of variable specific activities. These preliminary results showed that 4-[18F]fluorotropapride can be considered as a potent radiopharmaceutical for the study of the dopaminergic system with PET.

Animals↗
PubMed1992

Amino acids for the measurement of protein synthesis in vivo by PET.

In principle, PET in combination with amino acids labelled with positron-emitting radionuclides and kinetic metabolic models, can quantify local protein synthesis rates in tissue in vivo. These PET measurements have clinical potential in, for example, oncology, neurology and psychiatry. An optimal positron-emitting amino acid for the measurement of PSR has a high protein incorporation, can easily be prepared by automated equipment and has minimal non-protein radioactive metabolites. Presently L-[methyl-11C]methionine, L-[1-11C]leucine, L-[1-11C]tyrosine, L-[1-11C]phenylalanine, L-[1-11C]methionine and L-[2-18F]fluorotyrosine are under evaluation in normal volunteers and/or in patients. Several other amino acids are suggested. No comparison of the clinical usefulness of the different amino acids in man is yet available. Because of the longer half life of 18F compared to 11C, [18F]fluoro amino acids may have advantages over [11C]amino acids for the investigation of tissue with relative slow protein synthesis, such as brain, and for application in institutions with an off site, but nearby cyclotron. The half life of [13N]amino acids is considered to be too short for flexible clinical application. As yet no metabolic compartmental model has been investigated for [13N]amino acids. For routine application reliable preparation of the radiopharmaceutical is essential. Of all the amino acids under evaluation, a reliable, high yield, easy to automate production procedure is available for L-[methyl-11C]methionine only. It is however unlikely that this tracer can accurately measure PSR because of its non-protein metabolism. For the other amino acids the main problems in production are associated with complex multistep syntheses and/or low radiochemical yields, complex purification methods and the need to isolate the L-enantiomer. The kinetic metabolic models under investigation, consist of 4 or 5 compartments depending on the necessity to compensate for labelled metabolites. The metabolic profile of the amino acids is mainly extracted from animal experiments. Because of the number and amount of labelled metabolites in plasma, [11C]carboxylic labelled amino acids are preferred to amino acids with carbon-11 in another position. As yet no recommendation can be given on the optimal labelled amino acid(s) for PSR measurement in vivo nor on the methods to prepare the amino acids reported for this purpose.

Amino Acids↗
PubMed1992

Ligands and tracers for PET studies of the 5-HT system--current status.

The status of the radiochemical development and biological evaluation of radioligands and tracers for PET studies of the serotonergic system is reviewed, indicating those agents with present value and those with future potential. Practical recommendations are given for the preparation of two useful radioligands for PET studies of central 5-HT2 receptors, namely [18F]setoperone and [18F]altanserin. Though, it has not proved possible to recommend tracers or radioligands for the study of other aspects of serotonergic system, prospects for future radiochemical development are indicated, especially for developing radioligands for the 5-HT re-uptake site, and for the 5-HT1 and 5-HT3 receptors.

Animals↗
PubMed1992

Concentration dependence of fluorine impurity spin-lattice relaxation rate in bone mineral.

The concentration dependence of the fluoride ion spin-lattice relaxation rate has been observed by nuclear magnetic resonance experiments on samples of defatted and dried bone. The 19F spin-lattice relaxation rates increased linearly with the bone fluoride concentration. Different results were obtained from trabecular than from cortical bone. For the same macroscopic fluoride content per gram of bone calcium, the relaxation rate is significantly faster in cortical bone. Relaxation rates in cortical bone samples prepared from both rats and dogs were apparently controlled by the same species-independent processes. For samples from beagle dogs, the bulk fluoride concentrations measured by neutron activation analysis were 3.1 +/- 0.3 times greater in trabecular bone than in the corresponding cortical bone. The beagle spin-lattice relaxation data suggest that the microscopic fluoride concentrations in bone mineral were 1.8 +/- 0.4 times greater in trabecular bone than in cortical bone. It is concluded that the accumulation of fluoride impurities in bone mineral is non-uniform.

Animals↗
PubMed1992

Evaluation of the integrity of the blood-brain barrier after meningeal trauma.

RATIONALE AND OBJECTIVES: The authors used magnetic resonance imaging (MRI) techniques to examine the effect of meningeal trauma produced by cisterna magna puncture on the integrity of the blood-cerebrospinal fluid barrier (BCB) in a rat model. METHODS: Intravenous gadolinium-DTPA (Gd-DTPA), a relaxation rate modifier which normally does not cross the BCB, was used as a probe to follow leakage of fluid across the BCB. After Gd-DTPA injection, cerebrospinal fluid (CSF) serial samples were obtained through the needle used to create the experimental trauma. These samples were subsequently examined in vitro by MRI to obtain their T1 relaxation rates and assayed by mass spectrometry for gadolinium and elemental iron concentrations. RESULTS: The iron levels reflected the severity of puncture-related subarachnoid hemorrhage. Rats with ongoing meningeal damage showed significantly higher CSF levels of gadolinium and significantly higher CSF T1 relaxation rates than controls at all samples times over 1 hour after the puncture. Blood in the CSF could not explain these changes because the CSF iron levels did not significantly differ from control levels. CONCLUSIONS: Intravenously administered Gd-DTPA can gain access to the subarachnoid space through minor defects in the BCB and cause significant increases in CSF T1 relaxation rates.

Animals↗
PubMed1992

High-resolution magnetic resonance imaging of experimental spinal cord injury in the rat.

The ability of magnetic resonance imaging (MRI) to display the anatomic changes after spinal cord injury in the rat were examined in postmortem specimens. With the clip compression technique, acute spinal cord injuries of three grades of severity were produced in adult male rats. One hour after injury, during which time physiological parameters were measured and maintained within the normal range, the rats were killed by transcardiac perfusion of formalin. The vertebral column containing the cervical and upper thoracic segments was excised and, after further formalin fixation, 20 contiguous MRI scans centered on the injury site were obtained using a spin-echo imaging sequence. The volume of signal acquisition for each image was 15 x 15 x 1.0 mm thick. The spinal cords were then removed from the vertebral column, sectioned, and stained for histological examination. Ten-micrometer serial sections of each cord were examined microscopically. MRI scans and microscopic sections at comparable levels were examined to determine the quality of anatomical detail and spatial resolution of the MRI scans. MRI scans with resolution of about 75 microns per pixel edge were obtained. At the site of injury, there was disruption of the normally well demarcated gray-white interface and variable areas of low signal intensity. Because of the resolution achieved, it was possible to determine that these low signal intensity areas were post-traumatic hemorrhages. Indeed, hemorrhages with dimensions of the order of 100 microns were detected on the MRI scans. Furthermore, by examining the serial sections of the cord, the extent of the injury along the cord could be determined.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1991

Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats.

No-carrier-added [18F]altanserin was synthesized by nucleophilic substitution of the corresponding nitro compound with [18F]fluoride in the presence of kryptofix 222 and K2CO3. After purification by preparative HPLC, [18F]altanserin was produced in less than 2 hr with a radiochemical yield of 10% (EOS) and a specific activity of 0.8-1.3 Ci/mumol. In rats, the tracer localized rapidly in the whole brain (0.5% ID/g organ) with a high binding to the frontal cortex. The frontal cortex/cerebellum ratio increased with time and reached a plateau of 11 at 2 hr postinjection. This uptake in S2 receptor regions was saturable and could be blocked by pretreatment with various S2 antagonists. This radiopharmaceutical appears to be more selective for S2 receptor sites than other ligands available today and allows the study of S2 receptors under in vivo conditions.

Animals↗
PubMed1991

Decrease of frontal metabolism demonstrated by positron emission tomography in a population of healthy elderly volunteers.

Frontal metabolism measured with positron emission tomography is shown to be decreased relatively to that in other cortical or sub-cortical areas, in a population of healthy elderly compared to young volunteers. Cortical atrophy or neuronal depopulation are unlikely to entirely explain this physiological phenomenon, and sub-cortico-cortical deactivation should play a role, analogous to that proposed in subcortical diseases.

Aged↗
PubMed1978

Quantifying fatigue in working divers.

Thirty professional divers involved in training, bounce dives, working saturations, and deep experimental saturations were observed over a 1-month period. The subjects themselves performed simple twice-daily measurements of oral temperature, heart rate, breathhold time, handgrip strength, length and quality of sleep, and a subjective estimation of fatigue. The data were analysed with respect to the type of work done by the diver, separating diving from nondiving days. The results showed that subjective estimation of fatigue corresponded to the increment of evening oral temperature and heart rate over morning values. Both inspiratory and expiratory breathhold times decreased from morning to evening in those situations deemed most tiring by the divers. Sleep was generally of average duration and quality; however, diving during the daytime was associated with a decreased amount of sleep in the 24-h period including the following night. Sleep was also of poorer quality during periods of saturation diving. In addition to such group variations, individual divers showed significant performance changes on the various tests, demonstrating the value of this approach to the practical question of deciding when a man is too tired to dive safely. Extension of this method can, we hope, aid in the definition of safe working rotations for professional divers.

Adult↗
PubMed1977

Heart rate and core temperature as indicators of heat stress during deep underwater activity.

In hyperbaric environments, comfortable ambient temperatures are necessarily higher than normal room temperature, and high levels of humidity are also common. These conditions are stressful and even hazardous for an exercising diver. We monitored the heart rates and core temperatures of divers participating in deep experimental dives to pressures up to 300 msw. Accelerated heart rates (100 to 180 beats/min) and elevated core temperatures (+0.4 to 0.9 degrees C) were registered. The increase in heart rate can be explained by the rise in core temperature. Formulas are presented for the relationships between heart rate and duration of activity, between core temperature and duration of activity, and between heart rate and core temperature. These formulas allow the estimation of core temperature from the diver's pulse, and serve to prevent excessive heat stress which could lead to an accident.

Body Temperature↗
PubMed1976

Longitudinal study of performance after deep compressions with heliox and He-N2-O2.

This study concerns three hyperbaric experiments. During SAGITTAIRE iv, compression to 610 msw was accomplished in 11 days with an atmosphere of helium-oxygen. For the two CORAZ experiments, compression to 300 msw was done in 4 hours with He-N2-O2 trimix, varying nitrogen concentration from CORAZI (2.8 ATA N2 =9%) to CORAZ II (1.4 ATA N2=4.5%). Oxygen partial pressure was always maintained at 0.4 ATA except during decompression. The same two subjects participated in all three experiments and underwent the following psychometric tests: manual dexterity, visual choice-reaction time, and number ordination. Results show a large decrement in performance at 610 msw after slow compression (-50% and -47% on the number ordination test, -34% and -24% on the visual choice-reaction time). Test performance was less affected after the rapid compressions to 300 msw, and recuperation to control values occurred within 1 day at 300 msw. Our data show that 1.4 ATA N2 is less detrimental to performance than 2.8 ATA N2 for trimix compressions to 300 msw in 4 hours.

Adaptation, Physiological↗