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Lee, Hong-Shick,Nash, J. Frank,Meltzer, Herbert Y. The Korean Society of Pharmacology 1992 대한약리학잡지 Vol.28 No.1
Nonbenzodiazepine계 항불안제인 buspirone을 이용하여 건강한 8명의 남자를 대상으로 prolactin과 cortisol분비를 측정하였다. Buspirone는 $Dopamine_2$ 수용체 antagonist 성질 뿐 아니라 $5-HT_{1A}$ partial agonist 효과가 있는 것으로 보고되고 있다. Buspirone 30mg 경구투여시 혈청 prolactin 농도는 유의한 증가를 보였으나 혈청 cortisol 농도의 변화는 차이가 없었다. beta adrenoreceptor antagonist이면서 $5-HT_{1A}$ 수용체 antagonist로 알려진 pindolol (30mg)을 경구 투여한 결과 기초 혈청 prolactin이나 cortisol 농도는 유의한 차이가 없었다. Pinodlol을 전처치한 경우 buspirone-induced prolaction 분비의 유의한 억제효과는 없었다. 이상의 성적은 buspirone-induced prolactin 분비증가는 아마도 $5-HT_{1A}$ 수용체 활성과 관련되지 않음을 시사하는 것으로 사료된다. The effect of the nonbenzodiazepine anxiolytic, buspirone $(Buspar^R)$, a serotonin $(5-HT)_{1A}$ partial agonist, which also has dopamine $(DA)_2$ receptor antagonist properties, on prolactin and cortisol secretion was examined in eight normal male volunteers. The oral administration of buspirone (30 mg) significantly increased plasma prolactin concentrations but did not significantly increase plasma cortisol concentrations in this study. The oral administration of pindolol (30 mg), a beta adrenoceptor antagonist which is also a $5-HT_{1A}$ receptor antagonist, had no significant effect on basal prolactin or cortisol levels. Moreover, pretreatment with pindolol did not significantly inhibit the buspirone-induced increase in prolactin secretion. These preliminary data are suggestive that buspirone-induced prolactin secretion is not mediated via $5-HT_{1A}$ receptor activation.
Evidence for Enhanced Telomerase Activity in Barrett's Esophagus with Dysplasia and Adenocarcinoma
Merchant, Nipun B.,Dutta, Sudhir K.,Girotra, Mohit,Arora, Manish,Meltzer, Stephen J. Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.2
Background: Dysplasia and adenocarcinoma developing in Barrett's esophagus (BE) are not always endoscopically identifiable. Molecular markers are needed for early recognition of these focal lesions and to identify patients at increased risk of developing adenocarcinoma. The aim of the current study was to correlate increased telomerase activity (TA) with dysplasia and adenocarcinoma occurring in the setting of BE. Materials and Methods: Esophageal mucosal biopsies were obtained from patients (N=62) who had pathologically verified BE at esophagogastroduodenoscopy (EGD). Mucosal biopsies were also obtained from the gastric fundus as controls. Based on histopathology, patients were divided into three groups: 1) BE without dysplasia (n=24); 2) BE with dysplasia (both high grade and low grade, n=13); and 3) BE with adenocarcinoma (n=25). TA was measured by a PCR-based assay (TRAPeze$^{(R)}$ ELISA Telomerase Detection Kit). Statistical analyses were performed using one-way ANOVA and post-hoc Bonferroni testing. Results: TA was significantly higher in biopsies of BE with dyplasia and BE with adenocarcinoma than in BE without dysplasia. Subgroup analyses did not reveal any significant correlations between TA and patient age, length of BE, or presence of gastritis. Conclusions: Telomerase activity in esophageal mucosal biopsies of BE may constitute a useful biomarker for the early detection of esophageal dysplasia and adenocarcinoma.
Clozapine, but Not Haloperidol, Increases Hippocampal Dopamine and Acetylcholine Release
Young-Chul Chung,In-Seong Park,Zhu Li,Jin Dai,Herbert Y. Meltzer,Junji Ichikawa 대한정신약물학회 2003 CLINICAL PSYCHOPHARMACOLOGY AND NEUROSCIENCE Vol.1 No.1
Atypical antipsychotics (APDs) such as clozapine, but not the typical APD haloperidol, produce greater increases in dopamine and acetylcholine release in rat medial prefrontal cortex (mPFC), compared to the nucleus accumbens (NAC) or striatum (STR), a mechanism postulated to lead to improvements of negative symptoms and neurocognitive deficits in patients with schizophrenia. The present study determined whether typical and atypical APDs modulate dopamine and acetylcholine release in the ventral hippocampus (vHIP) as well as mPFC, both of which are important to neurocognitive functions in schizophrenia. Clozapine (3 and 10 mg/kg) produced comparable increases in dopamine release in the mPFC and vHIP. Clozapine (3 and 10 mg/kg) also increased acetylcholine release in both regions, without significant effect at 3 mg/kg in the mPFC. The perfusion of tetrodotoxin(1 μM) into the vHIP eliminated clozapine-induced dopamine and acetylcholine release in that region. Haloperidol (0.1, but not 1 mg/kg) only increased dopamine release in the mPFC, without an effect of all the doses on either release in either region. These results suggest that clozapine, but not haloperidol, increases dopamine and acetylcholine release in the vHIP as well as in the mPFC. This may further indicate that clozapine and perhaps related atypical APDs may differ from the typical APDs such as haloperidol in enhancing dopamine and acetylcholine transmission in the hippocampal-PFC pathway that may be responsible for neurocognitive deficits in schizophrenia.
Buspirone-induced Prolaction 분비와 5-HT<sub>1A</sub> 수용체: Pindolol 전처치 효과
이홍식(Hong Shick Lee),J. Frank Nash,Herbert Y. Meltzer 대한약리학회 1992 대한약리학잡지 Vol.28 No.1
Nonbenzodiazepine계 항불안제인 buspirone을 이용하여 건강한 8명의 남자를 대상으로 prolactin과 cortisol분비를 측정하였다. Buspirone는 DopaminE<sub>2</sub> 수용체 antagonist 성질 뿐 아니라 5-HT<sub>1A</sub> partial agonist 효과가 있는 것으로 보고되고 있다. Buspirone 30mg 경구투여시 혈청 prolactin 농도는 유의한 증가를 보였으나 혈청 cortisol 농도의 변화는 차이가 없었다. beta adrenoreceptor antagonist이면서 5-HT<sub>1A</sub> 수용체 antagonist로 알려진 pindolol (30mg)을 경구 투여한 결과 기초 혈청 prolactin이나 cortisol 농도는 유의한 차이가 없었다. Pinodlol을 전처치한 경우 buspirone-induced prolaction 분비의 유의한 억제효과는 없었다. 이상의 성적은 buspirone-induced prolactin 분비증가는 아마도 5-HT<sub>1A</sub> 수용체 활성과 관련되지 않음을 시사하는 것으로 사료된다. The effect of the nonbenzodiazepine anxiolytic, buspirone (Buspar<sup>R</sup>), a serotonin (5-HT)<sub>1A</sub> partial agonist, which also has dopamine (DA)<sub>2</sub> receptor antagonist properties, on prolactin and cortisol secretion was examined in eight normal male volunteers. The oral administration of buspirone (30 mg) significantly increased plasma prolactin concentrations but did not significantly increase plasma cortisol concentrations in this study. The oral administration of pindolol (30mg), a beta adrenoceptor antagonist which is also a 5-HT<sub>1A</sub> receptor antagonist, had no significant effect on basal prolactin or cortisol levels. Moreover, pretreatment with pindolol did not significantly inhibit the buspirone-induced increase in prolactin secretion. These preliminary data are suggestive that buspirone-induced prolactin secretion is not mediated via 5-HT<sub>1A</sub> receptor activation.
Maria Demeter,Ion Călina,Cătălin Vancea,Murat Şen,Mădălina Georgiana Albu Kaya,Elena Mănăilă,Marius Dumitru,Viorica Meltzer 한국고분자학회 2019 Macromolecular Research Vol.27 No.3
Collagen (C)-poly(N-vinyl-2-pyrrolidone) (PVP) double-network superabsorbent hydrogels were synthesized by e-beam (electron beam) radiation processing, both with the addition of water-soluble cross-linking agents (CA), as well as without CA. The aim of the study was to develop a hydrogel for future application as wound dressings via e-beam radiation cross-linking of two biocompatible polymers. The formation of C-PVP hydrogels was confirmed by Fourier transform infrared (FTIR) spectroscopy and their performance was determined from morphological and rheological experiments, such as sol-gel analysis, swelling capacity, storage (G') and viscous (G'') moduli, cross-linking density, and pore size. Sol-gel analysis was performed in order to determine the gel properties as function of absorbed dose and it was found that the degradation density (p0)/cross-linking density (q0) ratio indicates a negligible contribution of chain scission processes. The rheological data confirmed that the elastic properties were predominant: G' moduli were larger than G'' moduli, as is specific to elastic solids and indicate the formation of a permanent hydrogel network were cross-links are present. Moreover, the swelling studies indicated that the hydrogels have good stability both in deionized water and phosphate-buffered saline (PBS) solution at 37 oC, and superabsorbent properties. The hydrogels network parameters obtained with lower content of CA, could be controlled by changing the absorbed dose.
Sohn, Young Chang,Goo, Young-Wha,Kim, Dae-Hwan,Kim, Seung-Whan,Kang, Min-Jung,Nickolai A. Barlev,Shelley L. Berger,Vincent T. Chow,Suh, Pan-Gil,David O. Azorsa,Paul S. Meltzer,Lee, Kong-Ju,Lee, Young- 이화여자대학교 세포신호전달연구센터 2002 고사리 세포신호전달 심포지움 Vol. No.4
Activating signal cointegrator-2(ASC-2), also reported as AIB3, TRBP, RAP250, NRC and PRIP, directly binds to and functions as a coactivator molecule of nuclear receptors and many other transcription factors. In particular, our previous results from microinjection of anti-ASC2 antibody demonstrated that ASC-2 is required for transactivation by nuclear receptors and AP-1 in vivo. Here we show that ASC-2 belongs to a steady-state complex of approximately 2 MDa(ASCOM for ASC-2 complex) in HeLa nuclei, which contains mammalian homologues of Drosophila Trithorax group(Trx-G) proteins ALR-1, ALR-2, HALR and ASH2. ALR-1/2 and HALR contain a SET domain that specifically methylates histone H3 lysine 4(K4). We further demonstrate that retinoic acid receptor(RAR) transactivation requires retinoid-dependent recruitment of ASCOM to DNA-bound RAR in vivo. Thus, ASCOM represents the first mammalian coactivator complex with H3/K4-methylase activity, directly recruited to nuclear receptors.