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Christian Foged Christer Halldin Christian Loc’h Bernard Mazière Stefan Pauli Mariannick Maziére Holger C. Hansen Tetsuya Suhara Carl-Gunnar Swahn Per Karlsson Lars Farde 《European journal of nuclear medicine and molecular imaging》1997,24(10):1261-1267
NNC 13-8241 has recently been labelled with iodine-123 and developed as a metabolically stable benzodiazepine receptor ligand
for single-photon emission computed tomography (SPECT) in monkeys and man. NNC 13-8199 is a bromo-analogue of NNC 13-8241.
This partial agonist binds selectively and with subnanomolar affinity to the benzodiazepine receptors. We prepared 76Br labelled NNC 13-8199 from the trimethyltin precursor by the chloramine-T method. Carbon-11 labelled NNC 13-8199 was synthesised
by N-alkylation of the nitrogen of the amide group with [11C]methyl iodide. Positron emission tomography (PET) examination with the two radioligands in monkeys demonstrated a high uptake
of radioactivity in the occipital, temporal and frontal cortex. In the study with [76Br]NNC 13-8199, the monkey brain uptake continued to increase until the time of displacement with flumazenil at 215 min after
injection. For both radioligands the radioactivity in the cortical brain regions was markedly reduced after displacement with
flumazenil. More than 98% of the radioactivity in monkey plasma represented unchanged radioligand 40 min after injection.
The low degree of metabolism indicates that NNC 13-8199 is metabolically much more stable than hitherto developed PET radioligands
for imaging of benzodiazepine receptors in the primate brain. [76Br]NNC 13-8199 has potential as a radioligand in human PET studies using models where a slow metabolism is an advantage.
Received 19 April and in revised form 10 June 1997 相似文献
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Familial lipoprotein disorders are seen frequently in subjects with premature coronary artery disease. The genetic basis for
several dyslipoproteinemias has been elucidated in the past two decades. The majority of lipoprotein disorders result from
a combination of polygenic predisposition and poor lifestyle habits, including physical inactivity, increased visceral adipose
tissue, increased caloric intake, and cigarette smoking. Monogenic disorders are seen in approximately 5% of premature coronary
artery disease cases, and this prevalence is higher in populations with the Founder effect. Unraveling the genetic basis of
many lipoprotein disorders has allowed fundamental discoveries in molecular cellular physiology and has paved the way for
novel therapeutic approaches. 相似文献
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Grenon SM Lachapelle K Marcil M Omeroglu A Genest J de Varennes B 《The Canadian journal of cardiology》2007,23(14):1159-1161
Homozygous familial hypercholesterolemia (HzFH) is a rare genetic defect caused predominantly by mutations at the low-density lipoprotein receptor. Until recent advances in the management of this complex disorder, patients affected by HzFH rarely survived beyond 30 years of age. Two patients with HzFH who survived to adulthood and developed cardiovascular complications requiring surgery are reported. In these patients, a porcelain aorta complicated surgical management. Lipid profile, mutational analysis and pathological assessment of the aorta were performed in two patients referred for cardiac surgery. The first patient was a 46-year-old man with a history of coronary artery bypass grafting (CABG) and recurrent severe angina who, because of a heavily calcified ascending aorta, required a complex repeat CABG. The second patient was a 42-year-old woman who underwent CAGB at 28 years of age and presented 13 years later with aortic stenosis. The extensive calcifications of the whole aortic root required performance of a modified Cabrol procedure. A porcelain aorta appears to be a feature of HzFH. This has an important impact on surgical planning and management and on possible pathophysiological processes related to the cardiovascular complications of HzFH. 相似文献
7.
Indeterminate genotypes of hepatitis C virus by the Abbott RealTime HCV Genotype II assay in Morocco. About eight cases resolved by a sequencing method
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8.
Seven monoclonal antibodies (MAbs) selected from a large panel of human IgG-specific murine MAbs were characterized serologically and studied for their ability to cooperate in routine antihuman globulin agglutination tests. In binding inhibition experiments, three of these MAbs were shown to bind simultaneously to immobilized human IgG molecules. Cooperation among these MAbs increased significantly the capacity of the individual MAbs to agglutinate red cells sensitized with weak blood group antibodies. These results demonstrate the usefulness of selected MAb blending for the preparation of potent antihuman IgG reagents from murine monoclonal antibodies. 相似文献
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A number of factors were evaluated as predictors of field dependence (Embedded-Figures Test score) in alcoholics. In our sample, duration of excessive drinking and symptomatology of alcohol dependence were significantly related to the level of field dependence. These results fail to corroborate earlier findings and suggest that heightened field dependence in alcoholics is, at least partly, a consequence of alcohol misuse. In addition, a strong relationship was detected between the alcoholics' degree of anxiety and their degree of alcohol dependence. Possible bases for such a relationship are discussed. 相似文献