• 제목/요약/키워드: A3 agonist

검색결과 493건 처리시간 0.023초

${\alpha}_1-Adrenoceptor$ Agonist로서의 Oxymetazoline -가토혈압(家兎血壓) 상승작용(上昇作用)- (Oxymetazoline as an ${\alpha}_1-Adrenoceptor$ Agonist -A pressor effect in the rabbit-)

  • 박영태;최수형
    • 대한약리학회지
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    • 제18권2호
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    • pp.59-67
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    • 1982
  • 1) 여러가지 말초(末梢) 조직(組織)에서 ${\alpha}_1-adrenoceptor$의 agonist로 알려져 있는 oxymetazoline의 측뇌실내(側腦室內) 투여(投與)는 urethane마취가토(麻醉家兎)의 혈압상승(血壓上昇)을 일으켰다. 이 상승(上昇)은 guanethidine, chlorisondamine처리(處理)로 거의 영향(影響)을 받지 않았고, phenotolamine, guanethidine과 chlorisondamine 또는 부신결찰(副腎結紮)과 guanethidine처리하(處理下)에서는 억제(抑制)되었다. 2) 측뇌실내(側腦室內) oxymetazoline에 의한 혈압상승(血壓上昇)은 측뇌실내(側腦室內) prazosin투여후(投與後)에는 현저(顯著)히 감약(減弱)되었으나 yohimbine 및 piperoxan의 영향(影響)은 받지 않았다. 3) Reserpine처리(處理) 가토(家兎)에서도 측(側) 뇌실내(腦室內) oxymetazoline은 혈압(血壓) 상승(上昇)을 일으켰으며, 이도 측(側) 뇌실내(腦室內) prazosin투여후(投與後)에는 현저(顯著)히 감약(減弱)되었으나 yohimbine의 영향(影響)은 받지 않았다. 4) 전신마취(全身麻醉) 가토(家兎) 및 척수가토(脊髓家兎)에서 정맥내(靜脈內) oxymetazoline은 혈압상승(血壓上昇)을 일으켰으며 이 상승효과(上昇效果)에 대(對)한 정맥내(靜脈內) ${\alpha}_1-adrenoceptor$ antagonist의 길항능력(拮抗能力)은 prazosin, phentolamine, yohimbine의 순(順)으로 강(强)하였다. 5) 본(本) 실험성적(實驗成績)은 oxymetazoline이 혈압조절(血壓調節)에 관여(關與)하는 가토(家兎) 뇌조직(腦組織) 및 가토(家兎) 혈관근(血管筋)에서는 ${\alpha}_1-adrenoceptor$ agonist로 작용(作用)함을 가리키고 있다.

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랫드에서 TSH와 갑상선 호르몬에 미치는 dopamine계의 영향 (Effects of the dopaminergic system on release of TSH and thyroid hormone in rats)

  • 이상우;김진상;한정희
    • 대한수의학회지
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    • 제32권2호
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    • pp.165-173
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    • 1992
  • The present study was carried out to investigate the effects of dopaminergic drugs and the role of specific dopamine(DA) receptors on the release of TSH, $T_4$ and $T_3$. Serum TSH levels (cold-induced, $4{^{\circ}C}$) were determined using RIA(radioimmunoassay) at 30 min after administration of dopamine agonists and antagonists. Serum $T_4$ and $T_3$ levels were detected after these dopaminergic drugs were administered subcutaneously twice a day for a week. The results of the study are summarized as follows : Apomorphine, a nonspecific DA receptor agonist, produced a dose-depedent decrease in serum TSH, $T_4$ and $T_3$ levels. However, only low doses (0.3, 1.0mg/kg) of SKF38393, a specific $D_1$-receptor agonist, produced a decrease in serum lelvels of TSH. I,Y171555, a specific $D_2$-receptor agonist, produced a dose dependent decrease in serum TSH, $T_4$ and $T_3$ levels. However, SCH23390, a specific $D_1$-receptor antagonist, produced a decrease except in serum T levels which were increased dose dependently. High doses (1.0, 3.0mg/kg) of sulpiride, a specific $D_2$-receptor antagonist, made a increase in the serum levels of TSH and $T_3$. The effects of dopaminergic drugs in serum TSH and $T_4$ levels was potentiated by the pretreatment of apomorphine. The overall results of this study suggest that the regulation of TSH, $T_4$ and $T_3$ secretion were mediated via specific $D_1$ and $D_2$ receptor.

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소(牛)의 제1위 종주근 운동성에 대한 교감신경계 약물의 효과 (Effects of sympathomimetics on motility in the longitudinal muscle of the cattle rumen)

  • 임형주;한호재;한방근
    • 대한수의학회지
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    • 제34권3호
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    • pp.479-486
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    • 1994
  • Effects of catecholamines and the site of receptor of catecholamines were investigated in the longitudinal muscle of the rumen. In order to this experiment, specimens were obtained from 35 Korean Native Cattles, 2-3 years old, in the Kwang-ju area slaughterhouse. Longitudinal muscle strips of rumen were made from sample, and then measured the isometric contraction with physiograph in $37{^{\circ}C}$ organ bath. The results were summarized as follows. 1. 30% of all strips showed rhythmic contraction after short incubation time. 2. Relaxation produced by catecholamines in this preparations increased in a dose-dependant manner. 3. Isoproterenol(${\beta}$-agonist) caused relaxation, but phenylephrine(${\alpha}_1$-agonist) and xylazine(${\alpha}_2$-agonist) were unaffected. 4. The relaxation induced by epinephrine and norepinephrine were not affected by phentolamine(${\alpha}$-blocker) and prazosin(${\alpha}_1$-blocker), yohimbine(${\alpha}_2$-blocker). But propranolol(${\beta}$-antagonist) abolished the effect of catecholamines on relaxation. 5. It is concluded that catecholamines produced relaxation in the longitudinal muscle of rumen via the ${\beta}$-adrenoceptor.

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무릎굽힘근의 신장성에 대한 수축-이완 기술의 효과 (The Effect of Contract-Relax with Agonist Contraction on Hamstring Extensibility in Normal Subjects)

  • 송은지;오성희;이승화;이충휘
    • 한국전문물리치료학회지
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    • 제1권1호
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    • pp.55-60
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    • 1994
  • Thirty healthy adults aged 20 to 29 with no history of musculoskeletal or neurogenic disorder volunteered for this study. The contract-relax with agonist contration(CRAC) was applied to the right hamstring muscles with the subject in the supine position. Each hamstring group was stretched on three sucessive days with several repetitions of the technique lasting 1min, 3min, and 5min. respectively. Hamstring extensibility at the knee(ROM) was measured before and after stretching using on electronic digital inclinometer(EDI). The results, namely the increase in ROM, were analysed using one-way repeated ANOVA at p<0.05. The differences were not significant. Possible factors influencing the results are excessive sensitibility of the measuring instrument, the psychological and physical status of the subjects, and the level of muscle fatigue. The mean increases in ROM were 3.0 at 1min., 2.6 at 3min, and 2.1 at 5min. Inclusion of a control group would have further defined the effects of the stretching technique.

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Dehydrocostus Lactone Suppresses the Expression of iNOS Induced by TLR Agonists

  • Kim, Su Yeon;Heo, Sunghye;Kim, Seung Han;Kwon, Minji;Park, Sin-Aye;Youn, Hyung-Sun
    • 대한의생명과학회지
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    • 제25권3호
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    • pp.267-274
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    • 2019
  • Toll-like receptors (TLRs) are one of the families of pattern recognition receptors (PRR) to recognize pathogen-associated molecular patterns (PAMPs). PAMPs stimulate TLRs to initiate specific immunoactivity. The activation of TLRs signaling leads to the expression of pro-inflammatory gene products such as cytokines and inducible nitric oxide synthase (iNOS). To evaluate the therapeutic potential of dehydrocostus lactone (DHL), which is a natural sesquiterpene lactone derived from various medicinal plants, iNOS expression induced by LPS (TLR4 agonist), MALP-2 (TLR2 and TLR6 agonist), or Poly[I:C] (TLR3 agonist) were examined. DHL suppressed the iNOS expression induced by LPS, MALP-2, or Poly[I:C]. DHL also inhibited nitrite production induced by LPS, MALP-2, or Poly[I:C]. These results suggest that DHL can modulate TLRs signaling pathways resulting in anti-inflammatory effect.

중추성 성조숙증 및 조기 사춘기 여아에서 성선자극호르몬 방출호르몬작용제의 용량에 따른 사춘기 억제 효과 비교 (A comparative study of the puberty suppression effect of gonadotropin-releasing hormone agonist in precocious or early puberty girls)

  • 심계식;배종우;양유정
    • Clinical and Experimental Pediatrics
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    • 제51권6호
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    • pp.634-639
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    • 2008
  • 목 적 : 중추성 성조숙증 또는 조기 사춘기 소아에서 사춘기 진행의 억제를 위하여 사용하는 GnRH agonist의 적절한 용량에 대하여 논란이 많다. 따라서 치료의 표준화가 힘들고 치료에 대한 반응도 다양할 수밖에 없다. 본 연구는 중추성 성조숙증 또는 조기 사춘기 여아에서 GnRH agonist의 용량에 따른 사춘기 억제 효과를 비교하여 적당한 용량을 추정해보고자 하였다. 방 법 : 2006년 6월부터 2007년 5월까지 경희대학교 동서신의학병원 소아청소년과에서 조기 사춘기 혹은 성조숙증으로 진단받고 GnRH agonist를 투여하기로 한 여아 22명을 임의로 3군으로 나눠서 1군은 leuprolide acetate $70{\mu}g/kg$, 2군은 $90{\mu}g/kg$, 3군은 $110{\mu}g/kg$을 투여하였다. 치료 전, 치료 후 6개월에 채혈하여 황체화 호르몬, 난포자극호르몬, 에스트라디올, 프로게스테론을 검사하였고, 신장, 체중, 골 연령, 성성숙도의 변화를 평가하여 modified puberty suppression score를 구하여 억제된 경우는 2점 이하인 경우로 하였다. 각각의 군에서 역연령과 골연령의 평균은 Kruskal-Wallis test로 차이의 유무를 검정하였고, 억제가 된 경우와 되지 않은 경우의 수를 비교하여 two-by-K 교차분석(카이제곱 검정)을 시행하였다. 결 과 : 1군, 2군, 3군의 치료 전 역연령은 각각 $8.7{\pm}0.9$, $8.8{\pm}1.0$, $8.7{\pm}0.8$세, 골 연령은 $11{\pm}0.8$, $11{\pm}0.9$, $11{\pm}0.8$세, 신장표준편차점수는 $1.1{\pm}0.9$, $1.1{\pm}0.9$, $1.2{\pm}0.9$, 예측 성인키의 신장표준편차점수는 $-1.4{\pm}0.8$, $-1.4{\pm}1.1$, $-1.4{\pm}0.6$으로 의미 있는 차이는 없었다. 1군, 2군, 3군의 치료 전 혈중 황체화 호르몬은 각각 $3.0{\pm}2.9$, $3.0{\pm}2.3$, $3.0{\pm}3.4IU/L$, 에스트라디올은 각각 $1.5{\pm}1.0$, $1.4{\pm}0.9$, $1.6{\pm}1.0ng/dL$로 의미 있는 차이는 없었으며, 난포자극호르몬은 각각 $4.1{\pm}2.6$, $6.3{\pm}0.3$, $3.1{\pm}2.5IU/L$, 프로게스테론은 $33.9{\pm}17.1$, $30.6{\pm}14.7$, $35.8{\pm}14.8mg/dL$로 의미 있는 차이가 있었다(P<0.05). 1군, 2군, 3군 각각의 6개월 치료 후 신장표준편차점수의 변화는 $0.3{\pm}0.4$, $0.2{\pm}0.3$, $0.1{\pm}0.1$로서 1군과 2군 간에는 의미 있는 차이가 없었으나 3군과는 의미 있는 차이가 있었다(P<0.05). 1군, 2군, 3군의 치료 후 각각의 황체화 호르몬은 $0.5{\pm}0.3$, $0.4{\pm}0.3$, $0.3{\pm}0.3IU/L$, 난포자극호르몬은 $2.4{\pm}1.8$, $1.9{\pm}1.6$, $1.3{\pm}0.9IU/L$, 에스트라디올은 $0.9{\pm}0.8$, $0.9{\pm}0.8$, $0.9{\pm}0.9ng/dL$, 프로게스테론은 $19.5{\pm}8.7$, $18.0{\pm}7.7$, $16.9{\pm}7.2ng/dL$ 로서 치료 전과 비교하여 세 군에서 모두 의미 있게 감소하였으며 특히 난포자극호르몬과 프로게스테론은 다른 군에 비하여 3군에서 더욱 의미 있게 감소하였다(P<0.05). 사춘기 억제가 된 경우는 1군 7명중 4명, 2군 7명중 5명, 3군 8명중 8명이었고, 억제가 안 된 경우는 1군과 2군에서 각각 2명씩으로 3군에서 의미 있게 억제되는 경우가 많았다(P<0.05). 3군의 2명에서 치료 초기 주사 부위의 경미한 동통 외에 특이한 부작용은 없었다. 결 론 : 조기 사춘기 여아에서 사춘기의 진행을 막기 위해서는 성선 자극 호르몬이 보다 억제 될 수 있도록 고용량의 GnRH agonist의 투여가 필요하며, 적절한 용량에 대한 보다 많은 수의 연구가 필요하다고 사료된다.

Effects of Histamine on Cultured Interstitial Cells of Cajal in Murine Small Intestine

  • Kim, Byung Joo;Kwon, Young Kyu;Kim, Euiyong;So, Insuk
    • The Korean Journal of Physiology and Pharmacology
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    • 제17권2호
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    • pp.149-156
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    • 2013
  • Interstitial cells of Cajal (ICCs) are the pacemaker cells in the gastrointestinal tract, and histamine is known to regulate neuronal activity, control vascular tone, alter endothelial permeability, and modulate gastric acid secretion. However, the action mechanisms of histamine in mouse small intestinal ICCs have not been previously investigated, and thus, in the present study, we investigated the effects of histamine on mouse small intestinal ICCs, and sought to identify the receptors involved. Enzymatic digestions were used to dissociate ICCs from small intestines, and the whole-cell patch-clamp configuration was used to record potentials (in current clamp mode) from cultured ICCs. Histamine was found to depolarize resting membrane potentials concentration dependently, and whereas 2-PEA (a selective H1 receptor agonist) induced membrane depolarizations, Dimaprit (a selective H2-agonist), R-alpha-methylhistamine (R-alpha-MeHa; a selective H3-agonist), and 4-methylhistamine (4-MH; a selective H4-agonist) did not. Pretreatment with $Ca^{2+}$-free solution or thapsigargin (a $Ca^{2+}$-ATPase inhibitor in endoplasmic reticulum) abolished the generation of pacemaker potentials and suppressed histamine-induced membrane depolarization. Furthermore, treatments with U-73122 (a phospholipase C inhibitor) or 5-fluoro-2-indolyl des-chlorohalopemide (FIPI; a phospholipase D inhibitor) blocked histamine-induced membrane depolarizations in ICCs. On the other hand, KT5720 (a protein kinase A inhibitor) did not block histamine-induced membrane depolarization. These results suggest that histamine modulates pacemaker potentials through H1 receptor-mediated pathways via external $Ca^{2+}$ influx and $Ca^{2+}$ release from internal stores in a PLC and PLD dependent manner.

Effects of Alternate Treatment of Estrogen Receptor Antagonist and Agonist on Morphology of Male Reproductive Organs of Adult Mice

  • Choi, Hayana;Seong, Chi Nam;Park, Mi Suk;Cho, Hyun Wook
    • Applied Microscopy
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    • 제43권3호
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    • pp.103-109
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    • 2013
  • ICI 182,780 (ICI) is known as an estrogen receptor antagonist, whereas propyl pyrazole triol (PPT) is an estrogen receptor agonist. In this study, ICI or ICI added with PPT was injected into adult male mice. Body and reproductive organ weights were reduced in the ICI added with PPT group compared to the control group. Further, the ICI and ICI added with PPT groups both showed increases in luminal areas of the seminiferous tubules of the testis, whereas cell heights of efferent ductules and the initial segment of the epididymis were reduced. Sperm count in the caudal epididymis was reduced in the ICI and ICI added with PPT groups. These results show that reproductive tissues were more deeply affected in the ICI added with PPT group. We also demonstrated that treatment with ICI resulted in histological changes in the testis, efferent ductule, and epididymis. Further, alternate treatment with ICI and PPT induced abnormalities in reproductive organs. These results indicate that a high concentration of PPT together with ICI may cause histological abnormalities instead of histological restoration in reproductive organs.

The Differential Effect of Whole-body Irradiation on Morphine- and $\beta$-Endorphin-Induced Antinociceptive Actions in Mice

  • Kim, Kyung-N.;Chung, Ki-M.
    • International Journal of Oral Biology
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    • 제34권3호
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    • pp.137-142
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    • 2009
  • Whole-body $\gamma$-irradiation(WBI), which produces an oxidative stress, is reported to attenuate the acute antinociceptive action of morphine (a $\mu$-opioid receptor agonist), but not DPLPE (a $\delta$-opioid receptor agonist), in mice. Recently, we also reported that antinociceptive effect of morphine, but not $\beta$-endorphin (a novel $\varepsilon$-opioid receptor agonist), was attenuated by oxidative stress. These findings prompted us to investigate the effect of WBI on the antinociception of morphine and $\beta$-endorphin in mice. Mice were exposed to WBI (5 Gy) from a $^{60}Co$ gamma-source and tested 2 hours later for antinociception produced by intracerebroventricular administration of morphine or $\beta$-endorphin using the hot water tail-immersion and the writhing tests. WBI significantly attenuated the antinociception produced by morphine only in the hot water tail-immersion test, whereas the antinociception of $\beta$-endorphin was significantly potentiated by WBI in both tests. These results demonstrate a differential sensitivity of $\mu$- and $\varepsilon$-opioid receptors to WBI, and support the hypothesis that morphine and $\beta$-endorphin administered supraspinally produce antinociception by different neuronal mechanisms.

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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