• 제목/요약/키워드: H3 subtype

검색결과 86건 처리시간 0.029초

Effects of Age on Selective Antagonist Binding to Muscarinic Receptors in Rat Striatum

  • Kim, Hwa-Jung;Lee, Sun-Hyoung;Molly H. Weiler
    • Biomolecules & Therapeutics
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    • 제6권4호
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    • pp.337-344
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    • 1998
  • The objective of the present study was to investigate the effect of senescence on the binding properties of muscarinic receptors in the neostriatum of young (3 months), middle-aged (18 months) and aged (33 months) male Fischer 344 x Brown Norway hybrid rats by employing direct binding of selective radiolabeled antagonists. Using the selective M, muscarinic receptor antagonist, $[^3H]$AF-DX384, as the ligand, no significant difference in the maximal receptor density (Bmax) was observed in the neostriatum among any age-groups. In contrast, with the selective M, receptor antagonist, $[^3H]$4-DAMP, a significant increase in the number of muscarinic receptors was observed in neostriatal membrane fractions prepared from the aged animals relative to that observed in the young rats. For each ligand there was no age-related change in its affinity (Kd) for the muscarinic receptors. These results indicate that the observed age-related changes in the muscarinic receptor density may not be necessarily decremuntal and depend upon the muscarinic receptor subtype examined.

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수종 생약추출물의 muscarin성$(M_1\;type)$ acetylcholine 수용체$(mAChR-M_1)$에 대한 친화력 검색 (Binding affinity of some herbal extracts on the muscarinic acetylcholine receptor subtype 1 $(mAChR-M_1)$)

  • 김영섭;김정섭;김성기;허정희;이병의;유시용
    • 생약학회지
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    • 제32권3호통권126호
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    • pp.219-225
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    • 2001
  • The water extracts of 82 Korean medicinal herbs were examined for the binding affinity on the recombinant human muscarinic acetylcholine receptor subtype 1 $(mAChR-M_1)$ produced from the CHO (Chinese Hamster Ovary) cell line. Of those tested, the extracts of Coptidis Rhizoma, Phellodendri Cortex, Hedyotis Herba and of Terminariae Fructus were found to exhibit a significant competition with $[^3H]$ N-methyl-scopolamine for the specific binding to $mAChR-M_1$ in a dose dependent manner, respectively.

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서울지역 급성호흡기 환자들로부터 분리한 인플루엔자 바이러스의 유행양상 (2010-2012) (Epidemiological Characterization of Influenza Viruses detected from Acute Respiratory Patients in Seoul during 2010-2012)

  • 함희진;장정임;최성선;오세아;조석주;최성민;박선일
    • 한국환경보건학회지
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    • 제39권3호
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    • pp.230-238
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    • 2013
  • Objectives: For our survey of the incidence of influenza viruses among respiratory viral infections in Seoul, we evaluated their prevalence among infectious acute respiratory viral patients in Seoul from 2010 to 2012 through regular surveillance. Methods: For influenza virus detection, we conducted real-time PCR analyses on 2,544 throat specimens collected from patients with respiratory viral infections in Seoul between 2010 and 2012. They were collected and then tested for the presence of influenza viruses through reverse transcription (RT) - polymerase chain reaction (PCR). Results: 19.1% (486/2,544) of the throat specimens were determined to be positive for influenza viruses. The incidences of influenza viral infection in the case of respiratory viral infections through regular surveillance in Seoul were 23.0% (212/923) in 2010, 6.4% (47/738) in 2011, and 25.7% (227/883) in 2012, and 10.8% (275/2,544) of type A, and 8.3% (211/2,544) type B influenza viruses. In addition, the greatest prevalence was in the 20-49 age group (51.6% ), which shows that influenza viruses constituted a major causative agent of acute respiratory viral infections. Conclusions: The distributions of influenza viruses and the epidemiologic patterns of the viral pathogen in acute respiratory viral infectious patients may provide potentially effective data for epidemiological studies in Seoul, Korea.

소 부신수질 Muscarine 수용체의 성질 (Properties of Muscarinic Receptor in Bovine Adrenal Medulla)

  • 이신웅;이해태
    • Biomolecules & Therapeutics
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    • 제2권4호
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    • pp.361-368
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    • 1994
  • The nature of the muscarinic receptors in bovine adrenal medulla was investigated in this study. [$^3$H]Quinuclidinyl benzilate(QNB) specifically bound to a single class of muscarinic receptor with a $K_{D}$ value of about 70 pM in bovine adrenal medullary, cardiac ventricular and ileal homogenates. Pirenzepine inhibition curves of [$^3$H]QNB binding to cardiac ventricular and ileal homogenates were steep, indicating the presence of a single class of binding site for pirenzepine with a Ki value of 990 nM and 508 nM, respectively. However, pirenzepine/[$^3$H]QNB competition binding curves in adrenal medulla suggested the presence of two binding sites (Hill coefficient=0.59) with a high( $M_1$) and a low( $M_2$) affinity. Respective Ki values for pirenfepine were 16 nM and 633 nM, with 44% of total sites having a high affinity( $M_1$). Gallamine, which is selective to cardiac $M_2$-receptor, inhibited [$^3$H]QNB binding to adrenal medullary, cardiac ventricular and ileal homogenates with Ki values of 12 $\mu$M, 6 $\mu$M and 13 $\mu$M, respectively. Thus, the binding affinities of pirenzepine and gallamine for $M_2$-receptor in adrenal medulla were similar to those in ileum, which contains the $M_3$-receptor. These results indicate that the $M_1$- and $M_3$- muscarinic receptor subtypes coexist in the bovine adrenal medulla.a.

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Differential Expression of Protein Kinase C Subtypes during Ginsenoside Rh2-Induced Apoptosis in SK-N-BE(2) and C6Bu-1 Cells

  • Kim, Young-Sook;Jin, Sung-Ha;Lee, You-Hiu;Park, Jong-Dae;Kim, Shin-Il
    • Archives of Pharmacal Research
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    • 제23권5호
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    • pp.518-524
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    • 2000
  • We examined the modulation of protein kinase C (PKC) subtypes during apoptosis induced by ginsenoside Rh2 (G-Rh2) in human neuroblastoma SK-N-Bl(2) and rat glioma C6Bu-1 cells. Apoptosis induced by C-Rh2 in both cell lines was confirmed, as indicated by DNA fragmentation and in situ strand breaks, and characteristic morphological changes. During apoptosis induced by G-Rh2 in SK-N-BE(2) cells, PKC subtypes $\alpha$, $\beta$ and $\gamma$ were progressively increased with prolonged treatment, whereas PKC $\delta$ increased transiently at 3 and 6 h and PKC $\varepsilon$ was gradually down-regulated after 6 h following the treatment. On the other hand, PKC subtype $\beta$ markedly increased at 24 h when maximal apoptosis was achieved. In C6Bu-l cells, no significant changes in PKC subtypes $\alpha$, $\gamma$, $\delta$, $\varepsilon$ and $\beta$ were observed during apoptosis induced by G-Rh2. These results suggest the evidence for a possible role of PKC subtype in apoptosis induced by G-Rh2 in SK-N-BE(2) cells but not in C6Bu-1 cells, and raise the possibility that G-Rh2 may induce apoptosis via different pathways interacting with or without PKC in different cell types.

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일 지역 보건계열 대학생의 신종인플루엔자 A (H1N1) 예방접종 실태 및 영향 요인 (Status of and Factors Influencing Vaccination against the Pandemic (H1N1) 2009 Virus among University Students from the Fields of Nursing and Allied Health)

  • 김옥선
    • 대한간호학회지
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    • 제41권3호
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    • pp.403-410
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    • 2011
  • Purpose: This study was to identify the current status of vaccination against the pandemic (H1N1) 2009 virus among university students from the fields of nursing and allied health from a local community and verify factors influencing vaccination. Methods: The study included 227 students in the fields of nursing and allied health from a provincial university. Data were obtained from these participants between May 31 and June 11, 2010 by using self-report questionnaires. Results: The rate of vaccination against the pandemic (H1N1) 2009 virus for these participants was 14.5%. No difference was observed in this regard between majors and school year. Factors that influence vaccination against this virus included previous vaccination against seasonal influenza and participants’ attitudes toward general vaccination. Conclusion: The results suggest that for effective pandemic (H1N1) 2009 vaccination of university students from the fields of nursing and allied health, students who have not been vaccinated should be intensively managed. Developing a vaccination program that encourages a positive attitude toward vaccination is recommended.

Selectivity of Oxomemazine for the $M_1$ Muscarinic Receptors

  • Lee, Shin-Woong;Woo, Chang-Woo;Kim, Jeung-Gu
    • Archives of Pharmacal Research
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    • 제17권6호
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    • pp.443-451
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    • 1994
  • The binding characteristics of pirenzepine and oxomemazine to muscarinic receptor were studied to evaluate the selectivity of oxomemazine for the muscarinic receptor subtypes in rat cerebral microsomes. Equililbrium dissociation constant $(K_D){\;}of{\;}(-)[^3H]$quinuclidinyl benzilate$([^3H)QNB)$ determined from saturation isotherms was 64-pM. Analysis of the pirenzepine inghibition curve of [$^3H$]QNB binding to cerebral microsome indicatd the presence of two receptor subtypes with high $(K_1 = 16 nM, M_1 receptor)$two receptor subypes with about 20-fold difference in the affinity for high $(k_1 = 84nM, {\;} O_H receptor){\;} and {\;}low{\;} (K_1{\;} ={\;} 1.65\muM, {\;} O_L receptor$) affinity sites. The percentage populations of $M_1{\;} and M_3$, /TEX> receptors to the total receptors were 61 : 39, and those of $O_H{\;} and{\;} O_L$ receptors 39 : 61, resepectively. Both pirenzepine and oxomemazine increaed the $K_D$ value for $[^3H]QNB$ without affecting the binding site concentrations and Hii coefficient for the $[^3H]QNB$ without affecting the binding site concentractions and Hill coefficient for the [$^{3}$H]QNB binding. Oxomemazine had a 10-fold higher affinity at $M_1$ receptors than at $M_3$ receptors, and pirenzepine a 8-fold higher affinity at $O_H$ receptors were of $O_H$ receptors and 71% of $M_3$ receptors. However, $M_3$for oxomemazine and $O_H$for pirenzepine were composed of a uniform population. These results suggest that oxomemazine could be classified as a selective drug for $M_1$ receptors and also demonstrate that rat cerebral microsomes contain three different subtypes of $M_1{\;} M_3$ and the other site which is different from $M_1, {\;} M_2$, /TEX> receptors.

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Construction of a Transcriptome-Driven Network at the Early Stage of Infection with Influenza A H1N1 in Human Lung Alveolar Epithelial Cells

  • Chung, Myungguen;Cho, Soo Young;Lee, Young Seek
    • Biomolecules & Therapeutics
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    • 제26권3호
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    • pp.290-297
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    • 2018
  • We aimed to understand the molecular changes in host cells that accompany infection by the seasonal influenza A H1N1 virus because the initial response rapidly changes owing to the fact that the virus has a robust initial propagation phase. Human epithelial alveolar A549 cells were infected and total RNA was extracted at 30 min, 1 h, 2 h, 4 h, 8 h, 24 h, and 48 h post infection (h.p.i.). The differentially expressed host genes were clustered into two distinct sets of genes as the infection progressed over time. The patterns of expression were significantly different at the early stages of infection. One of the responses showed roles similar to those associated with the enrichment gene sets to known 'gp120 pathway in HIV.' This gene set contains genes known to play roles in preventing the progress of apoptosis, which infected cells undergo as a response to viral infection. The other gene set showed enrichment of 'Drug Metabolism Enzymes (DMEs).' The identification of two distinct gene sets indicates that the virus regulates the cell's mechanisms to create a favorable environment for its stable replication and protection of gene metabolites within 8 h.

Molecular Characterization of an H5N3 Influenza Virus Isolated from Spot-Billed Duck

  • Lee, Jin Hwa;Kwon, Hyuk Moo;Sung, Haan Woo
    • 한국가금학회지
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    • 제40권3호
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    • pp.243-252
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    • 2013
  • Among the 16 hemagglutinin (HA) subtypes of avian influenza virus (AIV), only the H5 and H7 subtypes have caused highly pathogenic avian influenza (HPAI) in poultry. However, most H5 or H7 subtype viruses are categorized as low pathogenic avian influenza (LPAI). Some AIVs, including the H5 and H7 HPAI viruses, have shown the ability to infect humans directly. In this study, we describe the biological and molecular characterization of an H5N3 AIV (SBD/KR/KNU SYG06/06) isolated from spot-billed duck (Anas poecilorhyncha) in Korea. A phylogenetic analysis of the eight viral genes showed that the SBD/KR/KNU SYG06/06 isolate belongs to the Eurasian lineage and that the SBD/KR/KNU SYG06/06 isolate was clearly different from HPAI H5N1 strains, including human isolates and the Italian HPAI H5N2 strains. Additionally, no relationship was found between SBD/KR/KNU SYG06/06 and the Korean HPAI H5N1 isolates. The SBD/KR/ KNU SYG06/06 isolate had avian specific receptor binding site residues in the HA protein and the four C-terminal amino acids in the NS1 protein. The HA protein of the SBD/KR/KNU SYG06/06 isolate exhibited the typical LPAI motif at the cleavage site and this virus produced no cytopathic effects in MDCK cells without trypsin. Given these results, we suggest that the H5N3 AIV isolated from the spot-billed duck should be considered an LPAI virus and should have no pathogenic effect in humans.

간기능 검사 이상이 동반된 대유행 인플루엔자(H1N1 2009)와 쯔쯔가무시병 동시감염 1예 (A Case of Coinfection with Pandemic (H1N1) 2009 Influenza and Scrub Typhus with Abnormal Liver Function Test)

  • 안용철;황윤우;김유석;김주희;조오현;임채만;우준희
    • Tuberculosis and Respiratory Diseases
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    • 제70권3호
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    • pp.247-250
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    • 2011
  • The pandemic (H1N1) 2009 influenza outbreak coincided with the typical Scrub typhus season, which can lead to diagnostic difficulties due to their similar and non-specific symptoms. Here we describe a case of laboratory confirmed co-infection of Pandemic (H1N1) 2009 influenza and Scrub typhus and discuss the difficulties in distinguishing the two illnesses clinically.