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Iganidipine, a new water-soluble Ca2+ antagonist: ocular and periocular penetration after instillation.

PURPOSE: To evaluate the potential of topical iganidipine ophthalmic solution to exert Ca(2+)-antagonistic activity in the posterior parts o … posterior retina. Fourth, periocular penetration of iganidipine was studied by means of whole-head autoradiography after a single instillation of (14)C-iganidipine (0.09%, 30 microL; n = 5). RESULTS: Penetration of topically applied iganidipine to the cornea or aqueous humor was high and estimated to be at least 10 times higher than that reported for timolol or …

Exploration of (R)-[11C]YH168 as a PET tracer for imaging monoacylglycerol lipase in the brain: from mice to non-human primates.

PURPOSE: The monoacylglycerol lipase (MAGL) plays a pivotal role in modulating the endocannabinoid system and is considered an attractive th … as accomplished by 11C-methylation via Suzuki cross-coupling of a pinacol boron precursor. In vitro autoradiography was performed using brain tissues from MAGL knockout and the corresponding wild-type mice. The metabolic stability of (R)-[11C]YH168 in mouse brain and plasma was assessed 5 min after injection. Dynamic PET scans were conducted on anesthetized mice …

Noninvasive Detection of HER2 Expression in Gastric Cancer by 64Cu-NOTA-Trastuzumab in PDX Mouse Model and in Patients.

The purpose of this study was to establish the quality control and quantify the novel 64Cu-NOTA-Trastuzumab in gastric cancer patient-derive … r and main organs was quantified by region of interested (ROI) analysis of the micro-PET images and autoradiography. Finally, gastric cancer patients were enrolled in preliminary 64Cu-NOTA-Trastuzumab PET/CT scans. NOTA-Trastuzumab was efficiently radiolabeled with 64Cu over a 99% radiochemical purity and 17.5 GBq/μmol specific activity. The immune activity was p …

Radiosynthesis and Evaluation of 18F‑Labeled Deuterated Radioligand for Positron Emission Tomography Imaging of Cholesterol 24-Hydroxylase.

Brain cholesterol homeostasis is critical for neuronal function and primarily regulated by cholesterol 24-hydroxylase (CYP46A1). Dysregulati … 8F]5 in 31.5 ± 1.5% non-decay-corrected radiochemical yield and high molar activity (>95 GBq/μmol). Autoradiography and PET imaging in mice demonstrated robust brain uptake, heterogeneous regional distribution, and specific target engagement. Radiometabolite analysis confirmed that brain radioactivity was mainly attributable to intact [18F]5, with a pharmacokinet …

Oxytocin and vasopressin 1a receptor alterations in the superior temporal sulcus and hypothalamus in schizophrenia.

Schizophrenia is a severe psychiatric condition marked by social impairments. Given that social cognitive functioning strongly predicts life outcomes in schizophrenia, understanding its neurobiological basis is crucial. This study used receptor autoradiography to measure vasopressin 1a (AVPR1a) and oxytocin receptor (OXTR) densities in postmortem brain tissue from individuals with schizophrenia (N = 23) and matched controls (N = 18). We focused on the superior temporal sulcus, a region involved in social perception and often impaired in schizophrenia. AVPR1a binding densities exceeded those of…

Development of 18F-Labeled Radiotracers for PET Imaging of the Adenosine A2A Receptor: Synthesis, Radiolabeling and Preliminary Biological Evaluation.

The adenosine A2A receptor (A2AR) represents a potential therapeutic target for neurodegenerative diseases. Aiming at the development of a p … ivity in the brain. Specific binding of [18F]PPY2 on mice brain slices was demonstrated by in vitro autoradiography. In vivo PET/magnetic resonance imaging (MRI) studies in CD-1 mice revealed a reasonable high initial brain uptake for both radiotracers, followed by a fast clearance.

The DYT1 carrier state increases energy demand in the olivocerebellar network.

DYT1 dystonia is caused by a GAG deletion in TOR1A, the gene which encodes torsinA. Gene expression studies in rodents and functional imaging studies in humans suggest that DYT1 dystonia may be a network disorder of neurodevelopmental origin. To generate high resolution metabolic maps of DYT1 dystonia and pinpoint dysregulated network elements, we performed 2-deoxyglucose autoradiography and cytochrome oxidase (CO) histochemistry in transgenic mice expressing human mutant (hMT1) torsinA and wild-type littermates. In comparison with controls, hMT1 mice showed increased glucose utilization (GU) …

Gestational age and dose influence on placental transfer of 63Ni in rats.

The effects of gestational age and dose of nickel exposure on regulating and influencing placental transfer were investigated. Pregnant rats on gestational day (GD) 12, 15 or 20 were injected intraperitoneally with saline, 64,320 or 640 kBq/kg body weight of (63)Ni. Twenty-four hours after administration, samples were harvested from each for measurement of radioactivity by liquid scintillation counting and for autoradiography. In placenta, amniotic fluid and fetal membrane, (63)Ni concentrations increased with increasing doses and gestational age. In fetus, (63)Ni concentrations reached a maxi…

Evaluation of a rat knee mono-arthritis using microPET.

AIM: Assessing the activity of synovitis, which is characterized by an increase in cell metabolism, is important for the prediction of futur … 2, 3 and 7 after arthritis induction. The subjects (n=2/time) were subsequently subjected to macro-autoradiography, and ¹⁸F-FDG accumulation was compared with histological findings. RESULTS: ¹⁸F-FDG PET images depicted swollen joints, and ¹⁸F-FDG accumulation increased with the progression of arthritis. Histologically, increased ¹⁸F-FDG accumulation correlated …

Пептид, похожий на инсулина, регулирует созревание яиц и метаболизм в комаре Aedes aegypti.

Поглощение позвоночной крови имеет важное значение для созревания яиц и передачи паразитов, вызывающих заболевания, женскими комарами. Предварительные исследования с желтой лихорадкой комаров Эйдес аегипти показали, что кормление крови стимулирует производство яиц путем высвобождения гормонов из медиальных нейросекретарских клеток в мозге комаров. Способность говяжьего инсулина стимулировать аналогичную реакцию также свидетельствует о том, что этот спусковой механизм представляет собой эндогенный инсулиновый песптид (ИЛП). A. aegypti кодирует восемь прогнозируемых ILP. Здесь мы сообщаем, что с

Совпадение в аннотации оригинала
Ingestion of vertebrate blood is essential for egg maturation and transmission of disease-causing parasites by female mosquitoes. Prior stud … ranes indicated that ILP3 had an IC(50) value of 5.9 nM that was poorly competed by bovine insulin. Autoradiography and immunoblotting studies suggested that ILP3 binds the mosquito insulin receptor (MIR), whereas loss-of-function experiments showed that ILP3 activity requires MIR expression. Overall, our results identify ILP3 as a critical regulator of egg produ …

Stimulation of mesothelial cell proliferation by exudate macrophages enhances serosal wound healing in a murine model.

Examination of thermally induced serosal lesions in mice displayed collections of inflammatory cells, predominantly macrophages, on and surr … e. In vivo assessment of mesothelial cell proliferation using tritiated thymidine incorporation and autoradiography demonstrated that peritoneal exudate cells stimulated mesothelial cell proliferation (12.44 +/- 1.63% labeling index, compared with controls in which medium only was used 4.48 +/- 0.71%). The mesothelial proliferation was predominantly because of ma …

Regional differences in the interaction of the excitotoxins domoate and L-beta-oxalyl-amino-alanine with [3H]kainate binding sites in human hippocampus.

The excitotoxic amino acid domoate causes anterograde amnesia and memory deficits while the excitotoxin L-beta-oxalyl-amino-alanine (L-BOAA) is considered the causative agent of the motoneurone disorder, neurolathyrism. Employing quantitative autoradiography we investigated the potency of domoate and L-BOAA to inhibit [3H]kainate binding in human hippocampus. Domoate inhibited binding of [3H]kainate with inhibition constants between 5.8 +/- 2.8 nM (deep layers of gyrus parahippocampalis) and 200.9 +/- 247.8 nM (CA1 region of hippocampus). It was about a thousandfold more potent than L-BOAA wit…

GLP-1 stimulates secretion of macromolecules from airways and relaxes pulmonary artery.

Recent data revealed the existence of specific receptors for glucagon-like peptide-1(7-36)amide (GLP-1) on rat lung membranes. Utilizing slide-mount autoradiography of fresh frozen lung tissue sections, we have localized binding sites for GLP-1 on mucous glands in the trachea and on vascular smooth muscle of the pulmonary artery. When tracheas were incubated in a modified Ussing chamber, the addition of GLP-1 to the submucosal side increased 35S-sulfate-labeled macromolecule secretion (191 +/- 12% above basal, P < 0.005). The optimal secretory response elicited by GLP-1 was approximately 23% o…

Detection of specific serum IgE in clonorchiasis cases and analysis of Clonorchis sinensis allergens.

Specific serum IgE levels of Clonorchis sinensis in infected humans were measured by avidin-biotin ELISA, and allergens from C. sinensis were identified by immunoblot and autoradiography. Then, allergens fractionated by Sephadex G-200 gel filtration were analyzed, and cross-reactive allergenic components of C. sinensis reacted with paragonimiasis sera were revealed. Fourteen out of 15 C. sinensis egg-positives were found to be serum IgE positive (absorbance > 0.27). Of 14 IgE-reacting allergen bands visualized, major allergens of 66, 61.5, 45, 37, 28.5, 23.5 and 15.5 KD were recognized by more…

Distribution and cellular localization of mRNA coding for 5-HT1A receptor in the rat brain: correlation with receptor binding.

In order to localize the cells expressing 5-HT1A receptors in the rat brain, we used in situ hybridization histochemistry to visualize the distribution of the mRNA coding for 5-HT1A receptors. Oligonucleotides derived from different parts of the coding region of the rat 5-HT1A receptor gene were used as hybridization probes. 5-HT1A binding sites were visualized on consecutive sections by receptor autoradiography using 3H-8-hydroxy-2-(di-n-propylamino)tetralin as ligand. The highest levels of hybridization were observed in the dorsal raphe nucleus, septum, hippocampus, entorhinal cortex, and in…

Assignment of a Chinese xeroderma pigmentosum patient from Taiwan to complementation group C.

A 2 years and 7 months-old Chinese boy with severe skin symptoms was diagnosed as xeroderma pigmentosum (XP) at Chang Gung Memorial Hospital in Taipei, Taiwan. Skin fibroblasts derived from the patient (patient identification number, XP1CTA) were used for genetic complementation analysis by the conventional cell-fusion technique followed by measurement of ultraviolet light (UV)-induced unscheduled DNA synthesis (UDS). The level of UDS in XP1CTA cells measured by autoradiography was about 20% of that in normal cells. When XP1CTA cells were fused with cells of a representative strain from each o…

A comparative autoradiographic study demonstrating differential intratumor localization of monoclonal antibodies to cell surface (Lym-1) and intracellular (TNT-1) antigens.

Autoradiography was utilized to explore the patterns of distribution of two different monoclonal antibodies (Lym-1 and TNT-1) in tumor-bearing nude mice. Lym-1 is an antibody against a cell surface B-cell antigen. In comparison, TNT-1 represents a novel approach and is an antibody against an intracellular (nuclear) antigen that is selectively revealed in degenerating tumor cells. Experimentally iodine-125-(125I) labeled Lym-1 or TNT-1 was injected intravenously into nude mice bearing either the Raji lymphoma or the ME-180 human cervical carcinoma. Qualitative autoradiographic analyses performe…

Induction of endogenous arachidonic acid metabolism in human neutrophils with snake venom phospholipase A2, immune complexes, and A23187.

The stimuli responsible for eicosanoid secretion of phagocytes in chronic inflammatory disorders like rheumatoid arthritis and chronic infla … oactive eicosanoids released were extracted and separated by thin layer chromatography, followed by autoradiography and quantitative laser densitometry. Stimulation with PLA2, immune complexes, or A23187 resulted in LTB4 formation of 0%, 1.8%, and 5.3%, respectively, of total released radioactivity. In conclusion, Russelli vipera PLA2 does not stimulate AA-releas …

Fate of attenuated schistosomula administered to mice by different routes, relative to the immunity induced against Schistosoma mansoni.

Newly transformed schistosomula and day 8 lung parasites, derived from optimally irradiated cercariae, were used to immunize groups of C57Bl … ed attenuated lung schistosomula, injected via the various routes, was examined by compressed organ autoradiography. After intradermal vaccination, a proportion of parasites migrated from the site of injection to the draining lymph node and lungs. Conversely, schistosomula administered via the other 3 routes persisted to varying degrees at the injection site, but …

Pathogenesis of shigella diarrhea: evidence for a developmentally regulated glycolipid receptor for shigella toxin involved in the fluid secretory response of rabbit small intestine.

Shigella toxin reproduces the major manifestations of shigellosis in ligated intestinal loops from adult rabbits and binds to a microvillus … d in animals greater than or equal to 16 d of age by high-performance thin-layer chromatography and autoradiography. Fluid secretion in response to shigella toxin in ligated small bowel loops occurred in temporal relation to the appearance of Gb3, a result thus indicating the involvement of Gb3 in mediating the toxin effects.