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Biomedical subjects

K Yanai

Publications and source records attributed to K Yanai.

At least 127 records · Page 7Linked to original sources

Biodistribution and radiation absorbed dose of (N-methyl[11C])pyrilamine: a histamine H-1 receptor radiotracer.

The in vivo biodistribution for (N-methyl[11C])pyrilamine in mice is reported for various times after i.v. bolus injection, together with estimates of the radiation absorbed dose for the same radiotracer in man. More than 60% of the injected dose was excreted via the kidneys in urine after 90 min post injection. The brain regional distribution in mice showed a favorable hypothalamus-to-cerebellum ratio, indicative of H-1 receptor binding, encouraging in vivo histamine H-1 receptor imaging studies in man.

Aminopyridines↗

Adrenergic projection from the caudal part of the nucleus of the tractus solitarius to the parabrachial nucleus in the rat: immunocytochemical study combined with a retrograde tracing method.

The presence of an adrenergic projection from the nucleus of the tractus solitarius (NTS) to the parabrachial nucleus (PB) was demonstrated by the immunocytochemistry combined with a retrograde tracing method. Numerous neurons containing both phenylethanolamine N-methyltransferase, a marker for adrenaline, and wheat germ agglutinin-conjugated horseradish peroxidase, a retrograde tracer, were detected in the dorsolateral part of the NTS at the level of the area postrema after injection of the tracer into the dorsal PB.

Adrenergic Fibers↗

Isolation and identification of beta-nitrostyrene from smoked chicken.

Extraction and identification of beta-nitrostyrene from smoked chicken is described. Commercially obtained smoked chicken was homogenised and extracted with chloroform-methanol (2:1). The extracts were fractioned by silicic acid column chromatography. The purified extract using thin-layer chromatography was identified by a colour reaction (this qualitative method for some nitrated compounds is developed this time), high pressure liquid chromatography and gas chromatography/mass spectrometry. The concentration of beta-nitrostyrene in the smoked chicken was 94 ppb. The average recovery of added beta-nitrostyrene was 107%. However, the toxicity of this material was not tested in the present paper.

Journal Article↗

Synthesis and biodistribution of [11C]fludiazepam for imaging benzodiazepine receptors.

As a tracer for in vivo studies on benzodiazepine receptors, 7-chloro-1,3-dihydro-5-(2-fluorophenyl)-1-[11C]methyl-2H-1,4- benzodiazepin-2-one, [11C]fludiazepam, was synthesized by the methylation of nor-derivative with [11C]CH3I, and purified by high-performance liquid chromatography. Within 60 min [11C]fludiazepam was obtained for injection in high radiochemical yields and in high radiochemical purity with a specific activity of up to 230 mCi/mumol. After i.v. injection of [11C]fludiazepam in rats the radioactivity was rapidly incorporated into many tissues and the blood clearance of the radioactivity was very rapid. The brain uptake was high and decreased gradually. The adrenal uptake was the highest and decreased with high loading doses. The effect of the loading dose on the uptake was also found in the heart and lungs. By autoradiography using [11C]fludiazepam, a higher accumulation was visualized in the cortex and thalamus than in other regions.

Animals↗

(N-methyl-[11C])pyrilamine, a radiotracer for histamine H-1 receptors: radiochemical synthesis and biodistribution study in mice.

The histamine H-1 receptor antagonist, pyrilamine (N-((4-methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethaned i ami ne) was labeled with carbon-11 by N-alkylation of desmethylpyrilamine with [11C]iodomethane, and purified by preparative high performance liquid chromatography. The chemically and radiochemically pure labeled pyrilamine was obtained with specific activity of approximately 2500 mCi/mumol (EOS). In vivo distribution studies in mice suggest that the distribution of this compound parallels the known histamine H-1 receptor density in the brain.

Aminopyridines↗

Primary structure of a base non-specific ribonuclease from Rhizopus niveus.

The primary structure of a base non-specific ribonuclease from Rhizopus niveus (RNase Rh) was determined by nucleotide sequence analysis of the DNA fragment encoding RNase Rh gene including signal peptide sequence, and amino acid sequence analysis of the peptide obtained from RNase Rh and RNase Rh' (a protease-modified RNase Rh created during the course of purification). The sequence determined was: MKAVLALATLIGSTLASSCSSTA LSCSNSANSDTCCSPEYGLVVLNMQWAPGYGPANAFTLHGLWPDKCSGAYAPSGGCDSN RASSSIASVIKSKDSSLYNSMLTYWPSNQGNNNVFWSHEWSKHGTCVSTYDPDCYDNYE EGEDIVDYFQKAMDLRSQYNVYKAFSSNGITPGGTYTATEMQSAIESYFGAKAKIDCSSG TLSDVALYFYVRGRDTYVITDALSTGSCSGDVEYPTK (the sequence of signal peptide is underlined). The sequence indicates that the homology with the sequence of RNase T2 from A. oryzae with the same base specificity is about 42% and that the sequences around the two histidine residues which are supposed to be involved in the active site are fairly conserved.

Amino Acid Sequence↗

Isolation and sequencing of a genomic clone encoding aspartic proteinase of Rhizopus niveus.

A gene encoding Rhizopus niveus aspartic proteinase was isolated from an R. niveus genomic library by using oligonucleotides probes corresponding to its partial amino acid sequence, and its nucleotide sequence was determined. By comparing its deduced amino acid sequence with the amino acid sequence of rhizopuspepsin (5, 26), we concluded that the R. niveus aspartic proteinase gene has an intron within its coding region and that it has a preproenzyme sequence of 66 amino acids upstream of the mature enzyme of 323 amino acids.

Amino Acid Sequence↗

Cerebral glucose utilization in pediatric neurological disorders determined by positron emission tomography.

We measured local cerebral glucose utilization in 19 patients with Lennox-Gastaut syndrome (LG), partial seizures (PS), atypical and classical phenylketonuria (PKU), Leigh disease, and subacute sclerosing panencephalitis (SSPE), using positron emission tomography (PET). The mean values of regional glucose utilization in interictal scans of LG were significantly reduced in all brain regions when compared with that of PS (P less than 0.005). PET studies of glucose utilization in LG revealed more widespread hypometabolism than in PS. Two siblings with dihydropteridine reductase deficiency, a patient with classical PKU, and a boy with cytochrome c oxidase deficiency showed reduced glucose utilization in the caudate and putamen. A marked decrease in glucose utilization was found in the cortical gray matter of a patient with rapidly progressive SSPE, despite relatively preserved utilization in the caudate and putamen. The PET study of a patient with slowly progressive SSPE revealed patterns and values of glucose utilization similar to those of the control. Thus, PET provided a useful clue toward understanding brain dysfunction in LG, PS, PKU, Leigh disease, and SSPE.

Adolescent↗

Regional cerebral metabolic rate for glucose in subacute sclerosing panencephalitis.

Regional cerebral metabolic rates for glucose (rCMRglc) were measured in two cases of subacute sclerosing panencephalitis (SSPE) with different clinical courses. A marked decrease in rCMRglc was found in the cortical gray matter of a patient with rapidly developing SSPE (3.6-4.2 mg/100 g brain tissue per min). However, the rCMRglc was preserved in the caudate and lenticular nuclei of the patient (7.7 mg/100 g per min). The rCMRglc in a patient with slowly developing SSPE revealed patterns and values similar to those of the control. The rCMRglc correlated better with the neurological and psychological status of SSPE.

Adolescent↗

Regional cerebral metabolic rate for glucose and cerebrospinal fluid monoamine metabolites in subacute sclerosing panencephalitis.

Regional cerebral metabolic rate for glucose (rCMRglu) and cerebrospinal fluid monoamine metabolites were measured in two cases of subacute sclerosing panencephalitis (SSPE) with different clinical courses. A marked decrease in rCMRglu was found in the cortical gray matter of a patient with rapidly developing SSPE (3.6-4.2 mg/100 g brain tissue/min). However, the rCMRglu was preserved in the caudate and lenticular nuclei of the patient (7.7 mg/100 g/min). The rCMRglu in a patient with slowly developing SSPE revealed patterns and values similar to those of the control. Cerebrospinal fluid monoamine metabolites; homovanilic acid and 5-hydroxyindoleacetic acid, were decreased in both rapidly and slowly developing SSPE. These data indicated that rCMRglu correlated better with the neurological and psychological status and that dopaminergic and serotonergic abnormalities have been implicated in pathophysiology of SSPE.

Adolescent↗

Characteristics of specific in vivo labeling of neuroleptic binding sites with 3-N-[11C]methylspiperone.

In vivo binding of 3-N-[11C]methylspiperone ([11C]NMSP) was saturable in the rat forebrain, but not in the cerebellum. Nonspecific binding was almost equivalent in all brain regions except for the white matter. [11C]NMSP binding was localized to receptor-rich fractions when low doses were administered (less than 20 nmol/kg body weight). The striatum-to-cerebellum ratio was a function of time after injection and administered dose. This ratio remained constant in low doses of under 30 nmol/kg. The radioactivity curve of the cerebellum in a control positron-emission tomographic study almost equaled that of the striatum in the dog pretreated with spiperone (2 mg). This indicates that the amount of binding in the cerebellum might be considered a nonspecific binding and unbound pool. The data obtained by the pretreatment study was different from that of displacement, which suggested that displaceable [11C]NMSP in the specific binding sites of the striatum was not completely cleared from the brain tissue by a large amount of unlabeled spiperone.

Animals↗

Simplified enzymatic synthesis and biodistribution of 11C-S-adenosyl-L-methionine.

11C-S-Adenosyl-L-methionine (11C-SAM) was synthesized enzymatically from 11C-L-methionine using rat-liver extract [40%-50% saturated (NH4)2SO4 fraction] as the enzyme source. In biodistribution studies in rats, the highest uptake of 11C-SAM was found in the kidneys. 11C-SAM was also accumulated in the small intestine, pancreas, adrenal gland, liver, and spleen. The uptake of 11C-SAM in the brain increased with time, but remained low. At 30 min after injection, about 50%-60% of the 11C radioactivity was present in the acid-insoluble fraction of the kidneys and liver. When a high loading dose of 11C-SAM was administered, the kidney uptake was enhanced, but the proportion of the radioactivity present in the acid-insoluble fraction was lower. In a study of one rabbit, the kidney uptake was of 11-SAM clearly visualized using positron-emission tomography.

Animals↗

In vivo kinetics and displacement study of a carbon-11-labeled hallucinogen, N,N-[11C]dimethyltryptamine.

The endogenous hallucinogen, N,N-dimethyltryptamine (DMT), was labeled with carbon-11 and its regional distribution in rat brain studied. [11C]DMT showed higher accumulation in the cerebral cortex, caudate putamen, and amygdaloid nuclei. Studies of the subcellular distribution of [11C]DMT revealed the specific localization in the fractions enriched with serotonin receptors only when a very low dose was injected into rats. The proportions of the radioactivity in receptor-rich fractions were greatly enhanced by pretreatment with the monoamine oxidase inhibitor, pargyline. Specific binding of [11C]DMT to serotonin receptors in dog brain was demonstrated by a positron emission tomographic study in which 5-methoxy-N,N-dimethyltryptamine caused approximately 20% displacement of the radioligand from the receptors.

Animals↗

[An anatomo-clinical case of sequelae of acute encephalopathy. Infantile spasm with hypsarrhythmia].

Clinico-pathological studies of West syndrome are rather rare. A case of sequelae of acute encephalopathy which involved a nine-month-old boy with post-mortem data is reported. Birth and postnatal development had been normal until the onset of illness. Laboratory examinations ruled out bacterial or viral meningo-encephalitis and metabolic disorders. After the recovery from a coma lasting several days, spastic quadriplegia, severe mental retardation and intractable epileptic attacks were present. The latter were made of tonic spasms and myoclonic seizures. EEG records showed hypsarrhythmia. Neuropathological examination revealed almost symmetrical bilateral cystic cavities in the pontine tegmentum and lateral nuclei of both thalami. The corpus callosum was very thin. No finding suggested a congenital anomaly. In a search of the pathological basis for infantile spasms, this case was compared with the published data. It would appear that the lesions of the pontine tegmentum play a significant role in the pathogenesis of hypsarrhythmia or infantile spasms.

Acute Disease↗

11C-coenzyme Q10: a new myocardial imaging tracer for positron emission tomography.

Coenzyme Q10 (CoQ10) is a co-factor of the mitochondrial electron-transfer system. 11C-Labeled CoQ10 was synthesized and its biodistribution in rats was examined comparing two kinds of preparation methods using different emulsifiers as a basic study for application of positron emission tomography. 11C-CoQ10 emulsified in saline with polyoxyethylene hydrogenated castor oil was present in the highest concentration in the blood at 30 min. On the other hand, the 11C-CoQ10 emulsified with phospholipids was rapidly cleared from the blood. The liver and spleen uptakes were high probably due to endocytosis, reflecting the characteristics of liposomes. The myocardial uptake was also high just after administration, and the heart-to-blood concentration ratio was over 10 after 5 min. These results suggest that 11C-CoQ10 prepared with liposomes may be a myocardial imaging tracer.

Aging↗

11C-labeling of indolealkylamine alkaloids and the comparative study of their tissue distributions.

Five indolealkylamines (N,N-dimethyltryptamine, N-methyltryptamine, bufotenine, O-methylbufotenine, N,N,N-trimethyltryptamine iodide) were labeled with 11C by use of 11CH3I. The labeled compounds were synthesized with a radiochemical yield of 2-50% (based on trapped 11CH3I) in 20-35 min with radiochemical purities of more than 92%. The tissue distributions of these labeled compounds were investigated in rats. In all cases, the accumulations in the liver, lung and small intestine were high. [11C]DMT and [11C]OMB also accumulated to a large extent in the brain, where their accumulation was retained. Brain uptake of three other radiopharmaceuticals was low. [11C]DMT is the radiopharmaceutical of choice for the study of the serotonin action mechanism in the brain, because it has the highest radiochemical yield and the highest brain uptake of these 11C-labeled compounds.

Animals↗