• 제목/요약/키워드: Beta-endorphin

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LIGAND BINDING CHARACTERISTICS OF $K_2$- OPIOID RECEPTOR AND ITS ROLE IN REGULATION OF 〔$^3$H〕HISTAMINE RELEASE IN FRONTAL CORTEX OF THE RAT

  • Kim, Kee-Won-;Park, Kyu--Cho
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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    • pp.305-305
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    • 1994
  • It has been shown that there are several subtypes of $\kappa$ opioid receptor, We have evaluated the properties of non-${\mu}$, non-$\delta$ binding of 〔$^3$H〕DIP, a nonselective opioid antagonist, in rat cortex membranes. Binding to ${\mu}$ and $\delta$ sites was inhibited by the use of an excess of competing selective agonists (DAMGO, DPDPE) for these sites. (-)Ethylketocyclazocine(EKC) inhibited 〔$^3$H〕DIP binding with Ki. of 70 nM. However, arylacetamides (U69593 and U50488H) gave little inhibition. Also, we have examined the opioid modulation of K$\^$+/(30 mM)-induced histamine release in rat frontal cortex slices labeled with 1-〔$^3$H〕histidine. The 〔$^3$H〕histamine release from cortex slices was inhibited by EKC, a $\kappa$$_1$-and $\kappa$$_2$-agonist, in a concentration-dependent manner(10 to 10,000 nM). The IC$\sub$50/ of EKC was 107 ${\pm}$ 6 nM. However, the $\delta$ receptor selective agonists, DPDPE and deltorphine II, ${\mu}$ receptor agonists, DAMGO and TAPS, $\kappa$$_1$-agonists, U69593 and U50488H, and $\varepsilon$-agonist, ${\beta}$-endorphin, did not inhibit histamine release even in micromoiar dose, indicating that ${\mu}$, $\delta$ or $\kappa$$_1$ receptors are not involved. The concentration-response curve of EKC was shifted to right in the presence of naloxone (300 nM), a ${\mu}$ preferential antagonist, norbinaltorphimine(300 nM), a $\kappa$$_1$ preferential antagonist and bremazocine(1 nM), a $\kappa$$_1$-agonist and $\kappa$$_2$-antagonist. These results suggest that $\kappa$$_2$ opioid receptor regulates histamine release in the frontal cortex of the rat.

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The Clinical Effect of Bosingunyang-tang on Chronic Non-bacterial Prostatitis/Chronic Pelvic Pain Syndrome : Randomized Double-blind, Placebo-controlled Clinical Trial

  • ;;;;;;이병철
    • 대한한방내과학회지
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    • 제29권3호
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    • pp.800-809
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    • 2008
  • Objective : Although chronic prostatitis/chronic pelvic pain syndrcme(CP/CPPS) is a common disease, there is no consensus on the etiology or pathology and treatment. This was a double-blinded, placebo-controlled, randomized clinical trial, investigating the therapeutic effects of the traditional Korean medicine, Bosingunyang-tang(BSGYT). Method : Participants who met US National Institutes of Health (NIH) consensus criteria for CP/CPPS were entered after applying inclusion/exclusion criteria. They were randomized to the BSGYT or placebo group. and treated three times a day for 6 weeks. NIH-Chronic Prostatitis Symptom Index (NIH-CPSI) was used to estimate the clinical symptoms of CP/CPPS. Prostaglandin E2 and ${\beta}$-endorphin in prostatic fluid, collected by 2-glass pre-massage and post-massage test, were analyzed as factors associated with pain and inflammation. Result : The mean decrease in NIH-CPSI total score of the BSGYT group was 11.0 points, which is 5.7 points more than the placebo group. (Mann Whitney test P=0.038) Also the BSGYT group showed three times higher response rate than the placebo group in NIH-CPSI pain subscale score. (Fisher's exact test P=0.027) In those responders, prostaglandin E2 decreased significantly. (Wilcoxon's signed-ranks test P=0.037). No specific side effects were observed. Conclusion : After a 6-week treatment period, BSGYT improved clinical symptoms of CP/CPPS patients by decreasing PGE2 level in prostatic fluid.

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전침이 자연살해세포 활성에 미치는 유전자 발현 profile에 대한 연구 (Genes profile related to modulation of natural killer cell activity induced by electroacupuncture)

  • 최기순;노삼웅;오상덕;배현수;안현종;하윤문;김강호;민병일
    • Journal of Acupuncture Research
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    • 제19권6호
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    • pp.111-124
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    • 2002
  • A line of study reported that electroacupuncture(EA) modulate natural killer cell(NK Cell) activities. One report suggested that EA enhanced splenic interferon-gamma($IFN-{\gamma}$), interleukin-2(IL-2), and NK cell activity in Sprague-Dawley rats. Another study suggested that $IFN-{\gamma}$ mediates the up-regulation of NK cell activity, and endogenous ${\beta}$-endorphin secretion also play a role in the up-regulation of NK cell activity induced by EA stimulation. In order to better understand the molecular regulation underlying the activation of NK cell induced by EA, we have utilized cDNA microarray to elucidate how EA alters program of gene expression of spleen in rats. First, we divided three groups, group I was EA group treated with EA in restriction holder, group II was sham group with only holder stress, and last group III was control group with no treatment. We measured NK cell activity after EA stimulation three times for 2 days using $^{51}Cr$ release assay. Second, Biotin-labeled cDNA probes synthesized from EA group and sham group, were competitively hybridized to the microarray that contained variable genes. Such high-throughput screening has identified a number of EA-responsive gene candidates. Of these, we found that EA induced a subset of genes of genes that functionally could modulatory effects on NK cell activity. Genes(vascular cell adhesion molecule-1, protein-tyrosine kinase, CD94 mRNA) related to boost NK cell activity, were increased by EA And, genes(protein-tyrosine-phospatase mRNA, protein-tyrosine phosphatase(SHP-1) mRNA) related to inhibit NK cell activity, were decreased by EA. These EA-responsive genes may provide key insights from which to understand mechanisms of activation of NK cell induced by EA.

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익지인(益智仁), 두충(杜沖), 백강잠(白殭蠶) 혼합추출물이 남성갱년기 증상 개선에 미치는 영향 (Effects of Fructus Amomi Amari, Eucommiae Cortex, Bombyx Batryticatus Extract on Improving Symptoms of Late-onset Hypogonadism)

  • 박선영;안상현;김호현
    • 동의생리병리학회지
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    • 제33권2호
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    • pp.89-101
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    • 2019
  • In recent times, the number of men with late-onset hypogonadism has increased, and interest on this topic has also increased. This study was conducted to investigate effects of the mixture extract of Fructus amomi Amari, Eucommiae cortex, Bombyx batryticatus on improve late-onset hypogonadism. The experimental subjects consisted of three groups: a control group consisting of 8-week-old male ICR mice that had undergone no treatment, an aging-elicited group (AE group) consisting of 50-week-old ICR male mice that had undergone no treatment, and a Mixed herbal extract treatment group (MT group) consisting of 50-week-old ICR male mice that had undergone the mixture extract of Fructus amomi Amari, Eucommiae cortex, Bombyx batryticatus treatment (0.1 g/kg/day) for 6 months. After the experiment, the mice from all the experimental groups were dissected, and they were analyzed through histochemical and immunohistochemical methods. The mixture extract of Fructus amomi Amari, Eucommiae cortex, Bombyx batryticatus reduces aging-induced cell damage and oxidative stress and increases the secretion of serotonin and B-endorphin in aged mice, and promotes spermatogenesis in seminiferous tubules and reduces apoptosis and oxidative stress, and increases androgen receptor, $17{\beta}-HSD$ and GnRH, increases the ratio of smooth muscle to collagen fibers in the corpus cavernosum, increases eNOS, decreases PDE-5 and oxidative stress in aged mice, so it improves depression, reproductive, sexual problems caused by Late-onset hypogonadism. the mixture extract of Fructus amomi Amari, Eucommiae cortex, Bombyx batryticatus inhibits the induction of osteoporosis by increasing decreased bone matrix distribution due to aging, increasing the activities of OPC and OPN, which are produced in osteoblasts, and decreasing RANKL, MMP-3 activity, increasing OPG activity. It also reduces muscle damage, oxidative stress, inflammation and apoptosis of muscle tissue, and increases Myo-D in the sartorius muscle of aged mice for improving muscle atrophy caused by by Late-onset hypogonadism.

백서 대뇌피질에서 Opioid Kappa수용체의 Histamine 유리조절기능에 관한 연구 (Regulation of Histamine Release by Kappa Opioid Receptor in Rat Cortical Slices)

  • 김기원;조규박
    • 대한약리학회지
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    • 제30권1호
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    • pp.1-9
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    • 1994
  • Opioid 수용체에는 ${\mu},\;{\delta}$ 그리고 ${\kappa}$의 세가지 주된 형이 존재함이 알려져 있는 바, 최근 수용체 동정 기법과 선택적인 약물의 개발로 인해 그 아류들이 존재함이 보고되고 있다. 그러나 Opioid ${\kappa}_{2-}$ 수용체의 기능에 대해서는 이 수용체에 있어서의 선택적인 효현제 또는 길항제가 밝혀져 있지 않으므로써 현재까지 잘 알려져 있지 않다. 본 연구에서는 백서 대뇌피질 세표막표본에 opioid ${\mu}$${\delta}$ 수용체를 과량의 DAMGO와 DPDPE로 봉쇄한 후 수종 ${\kappa}$수용체 결합자의 $[^3H]\;idprenorpnine(DIP)$ 결합억제효과와 이에 대한 sodium과 $GTY{\gamma}S$의 영향을 관찰하여 이를 지표로 각 ligand의 수용체에서의 작용양상을 검토하여 이를 토대로 동일 표본에서 $[^3H]diprenorpnine[^3H]DIP$ 결합은 DIP, ethylketocyclazocine 그리고 bremazocine에 의해 효과적으로 억제되었으나, ${\kappa}_1$, 수용체 효현제인 U69593에 의해서는 억제되지 않았다. Opioid ${\kappa}_1$, 및 ${\kappa}_2$-수용체 효현제인 EKC의 Ki치는 배양액내 NaCl을 NMDG로 알려진 $GTP{\gamma}S\;100{mu}M$ 첨가에 의해 증가되었다. 그러나 Bremazocine과 DIP의 Ki치는 sodium 제거 또는 $GTP{\gamma}S\;100{mu}M$ 첨가에 의해 증가되었다. 그러나 Bremazocine과 DIP의 Ki치는 sodium 제거 또는 $GTP{\gamma}S$ 첨가에 의해 영향받지 않았다. $1-[^3H]\;histidine$을 미리 부하한 대뇌피질 절편에서 $30mM\;K^+$ 에 의한 $[^3H]\;histamine$의 유리는 (-)EKC에 의하여 영향받지 않았다. (-)EKC의 histamine유리 억제효과는 naloxone, norbinaltorpmine 또는 bremazocine에 의하여 각각 억제되었다. 본 실험 성적은 백서 대뇌피질에서 histamine의 유리는 이 부위에 존재하는 opioid ${\kappa}_2$-수용체에 의하여 조절됨을 시사한다.

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