Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0432222 (SEM)
 47,337 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Changes in substance P (SP) receptor concentration have been implicated in neuropsychiatric disorders, Parkinson's disease, arthritis, inflammatory bowel disease and asthma. Since, SP and peptide analogs are rapidly metabolized and do not penetrate into the CNS, they are not useful for PET. Recently, a non-peptide SP antagonist, (+)-(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine (CP-99,994) was developed. As a prelude to PET studies, this compound was radiolabeled with 11C and biodistribution was determined in hamsters. CP-99,994 was radiolabeled by methylation of tert-Boc, desmethyl CP-99,994 with 11CH3I followed by deprotection and HPLC purification. The time required for the synthesis was 40 min from the end of bombardment. Radiochemical purity of the final product was > 95% and specific activity was routinely > 1000 mCi/mumol [EOS]. The biodistribution of 11C-CP-99,994 was determined in groups of six Syrian hamsters at 5 and 30 min after injection. The results of these studies demonstrated that significant concentrations (%ID/g +/- SEM) of CP-99,994 accumulate in most tissues of the hamster. The highest levels of drug were detected in the lung: 21.04 +/- 1.26 (5 min) and 13.49 +/- 1.71 (30 min). Brain accumulation was: 1.44 +/- 0.06 (5 min), 1.32 +/- 0.05 (30 min). These results indicate that 11C-CP-99,994 can be prepared in high purity and specific activity. This new radiopharmaceutical may be useful for studying both central and peripheral SP receptors by PET.
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PMID:Synthesis of a 11C-labeled NK1 receptor ligand for PET studies. 773 67

[11C]Dapoxetine.HCl, S-(+)-N,N-dimethyl-a-[2-(naphthalenyloxy)ethyl] benzenemethanamine hydrochloride, a potent serotonin re-uptake inhibitor was prepared from its mono-methyl precursor, S-(+)-N-methyl-a-[2-(naphthalenyloxy)ethyl]benzene methanamine hydrochloride. Biodistribution was determined in rats at 5, 30 and 60 min after injection and preliminary PET studies were performed in a Rhesus monkey. 11CH3I was bubbled into a solution of S-(+)-N-methyl-alpha-[2-(naphthalenyloxy)ethyl]benzene methanamine hydrochloride (3.0 mg in DMSO) and the mixture was heated at 110 degrees C for 8 min. [11C]Dapoxetine.HCl was purified by HPLC on a C18 cartridge eluted with MeOH:phosphate buffer, pH 7,2 (75:25) with a 10% yield (end of synthesis). The time required for the synthesis was 40 min, from the end of bombardment. Radiochemical purity of the final product was > 99% and specific activity was routinely > 400 mCi/mumol [EOS]. In the biodistribution studies the highest concentration (%ID/g +/- SEM) of dapoxetine.HCl was detected in lung: 4.56 +/- 0.27 (5 min), 1.28 +/- 0.18 (30 min) and 0.67 +/- 0.04 (60 min). Brain accumulation was 0.76 +/- 0.02 (5 min), 0.46 +/- 0.04 (30 min) and 0.27 +/- 0.01 (60 min). Preliminary PET studies demonstrated significant displaceable binding in the cerebral cortex and subcortical grey matter. These results demonstrate that [11C]dapoxetine.HCl can be prepared in high purity and may be useful for the in vivo evaluation of serotonin re-uptake mechanisms.
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PMID:Synthesis of [11C]dapoxetine.HCl, a serotonin re-uptake inhibitor: biodistribution in rat and preliminary PET imaging in the monkey. 923 26

The male of Pardosa jeniseica, collected in the East-Kazakhstan Area, was first illustrated in Eskov Marusik (1995). The authorship of the species was given as "Zyuzin, 1991", because A.A. Zyuzin informed the authors in 1990 that a description of the species was in press. Because no such description ever appeared the authorship was given to Eskov Marusik, and a single male specimen from East-Kazakhstan is now considered to be the holotype. It is kept in Zoological Museum of the Moscow State University. Esyunin et al. (1999) illustrated and described a female from the Urals thought to be conspecific with P. jeniseica. Conspecifity of the illustrated specimen with P. jeniseica was doubted by Marusik et al. (2000). Kronestedt (2013) was the first to illustrate the epigyne of P. jeniseica and Azarkina Trilikauskas (2013) provided both verbal and illustrated descriptions of the female, and its epigyne and endogyne. Both sexes taken from one locality were never depicted, nor was peculiar pubescence of the male's leg I. Therefore, I decided to provide detailed illustrations and a verbal description of this species based on specimens from the place considered to be the type locality.Specimens were photographed at the Zoological Museum (University of Turku, Finland) with a Canon EOS 7D camera attached to an Olympus SZX16 stereomicroscope and a SEM JEOL JSM-5200 scanning microscope. Digital images were montaged using Helicon focus 3.10 image stacking software. All measurements are given in millimeters. The following abbreviations are used for leg segments: Fe femur, Pa patella, Ti tibia, Mt metatarsus, Ta tarsus; leg spination abbreviations: d dorsal, p prolateral, r retrolateral, v ventral. Material used in this study is deposited in the Moscow State University (ZMMU) and Zoological Museum of the University of Turku (ZMUT). I thank Seppo Koponen (Turku, Finland) for providing museum facilities and Don Buckle (Saskatoon, Canada) for editing English in the earlier draft of the manuscript.
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PMID:Redescription of the Siberian species Pardosa jeniseica (Araneae: Lycosidae). 3031 70

Mineralized tissues, such as bone and teeth, have extraordinary mechanical properties of both strength and toughness. This mechanical behavior originates from deformation and fracture resistance mechanisms in their multi-scale structure. The term quality describes the matrix composition, multi-scale structure, remodeling dynamics, water content, and micro-damage accumulation in the tissue. Aging and disease result in changes in the tissue quality that may reduce strength and toughness and lead to elevated fracture risk. Therefore, the capability to measure the quality of mineralized tissues provides critical information on disease progression and mechanical integrity. Here, we provide an overview of clinical and laboratory-based techniques to assess the quality of mineralized tissues in health and disease. Current techniques used in clinical settings include radiography-based (radiographs, dual energy x-ray absorptiometry, EOS) and x-ray tomography-based methods (high resolution peripheral quantitative computed tomography, cone beam computed tomography). In the laboratory, tissue quality can be investigated in ex vivo samples with x-ray imaging (micro and nano-computed tomography, x-ray microscopy), electron microscopy (scanning/transmission electron imaging (SEM/STEM), backscattered scanning electron microscopy, Focused Ion Beam-SEM), light microscopy, spectroscopy (Raman spectroscopy and Fourier transform infrared spectroscopy) and assessment of mechanical behavior (mechanical testing, fracture mechanics and reference point indentation). It is important for clinicians and basic science researchers to be aware of the techniques available in different types of research. While x-ray imaging techniques translated to the clinic have provided exceptional advancements in patient care, the future challenge will be to incorporate high-resolution laboratory-based bone quality measurements into clinical settings to broaden the depth of information available to clinicians during diagnostics, treatment and management of mineralized tissue pathologies.
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PMID:Breaking new ground in mineralized tissue: Assessing tissue quality in clinical and laboratory studies. 3315 23