• 제목/요약/키워드: piperazine

검색결과 91건 처리시간 0.029초

아민 흡수제의 화학구조에 따른 휘발 특성 (Analysis of Amine Absorbents Volatility Based on the Chemical Structure)

  • 이경자;이지현;곽노상;이인영;김준한;엄용석;장경룡;심재구;이용택
    • Korean Chemical Engineering Research
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    • 제50권2호
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    • pp.348-352
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    • 2012
  • 화학흡수법을 이용한 $CO_2$ 포집 공정에서 발생되는 아민계 흡수제의 휘발은 대기 환경에 좋지 않은 영향을 미칠 뿐만 아니라 공정 운용에 있어 흡수제 손실을 보충하기 위한 비용의 증가를 초래하게 되므로 이에 대한 정확한 특성을 파악하는 것이 중요하다. 본 연구에서는 이를 위해 자체 고안한 휘발도 측정 장치를 활용하여 주요 아민 수용액(MEA(monoethanolamine), MDEA(n-methyldiethanolamine), Pz(piperazine), AMP(2-amino-2-methyl-1-propanol), 2-MP(2-methylpiperazine), DGA(diglycolamine))의 휘발도를 측정하고, 가스크로마토그래피 장치를 활용한 정량적인 비교를 통해 다양한 온도 조건과 $CO_2$ 부하 변화에 따른 휘발도의 영향을 분석하였다. 실험결과 MDEA$CO_2$ 부하 조건에 따른 실험에서 휘발도가 매우 낮음을 확인할 수 있었다. 이는 MDEA의 분자 구조 내에 하이드록실기(-OH)가 2개 있어 높은 친수성으로 인하여 휘발이 거의 되지 않았고, 이에 비해 MEA 및 AMP는 하이드록실기(-OH)가 1개이고, AMP의 경우 소수성기인 알킬기($-CH_3$)가 2개 있어 가장 많이 휘발된 것으로 판단된다.

백서의 심방관류모델에서 protein kinase C의 활성화가 atrial natriuretic peptide(ANP) 조절에 미치는 영향 (Effects of activation of protein kinase C on the regulation of atrial natriuretic peptide(ANP) by isolated perfused left atria)

  • 강창원;강형섭;이호일
    • 대한수의학회지
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    • 제37권4호
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    • pp.735-744
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    • 1997
  • 심방근 세포는 심방이뇨호르몬을 합성, 저장 그리고 분비하며, 세포내외 이온의 농도, 수분균형 및 혈압 등을 조절하는 것으로 알려져 있다. 또한 심방근의 인장자극에는 Atrial Natriuretic Peptide(ANP)를 2단계(분비, 유리)의 과정으로 이루어져 있으며, 이에 따른 심방이뇨호르몬의 분비 조절기전에 대하여서는 명확히 알려져 있지 않다. 따라서 본 연구는 백서의 심방근 적출관류 모델을 이용하여 protein kinase C와 ANP 조절의 상관관계를 밝히고 분비와 유리의 과정중 어떠한 과정을 이용하여 분비자극에 영향을 주는지를 관찰하기 위하여 본 실험을 실시하였다. PKC 활성제인 PMA(phorbol 12-mystrate 13-acetate)는 ANP의 유리를 현저하게 증가시켰으며, PKC 억제제인 H-7(1-(5-isoquinoline sulfonyl)-2-methyl piperazine dihydrochlo-ride)에 의해 유리를 억제시켰다. PMA와 H-7을 동시에 처리한 경우 PMA에 의하여 증가된 ANP의 유리가 H-7에 의하여 차단됨을 관찰할 수 있었다. 따라서 백서의 관류 심방에서의 ANP 분비 증가는 PKC 활성화에 의하여 이루어지며, ANP분비의 2단계중 ANP 유리에 영향을 줌을 알 수 있었다.

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5-$HT_{1A}$수용체작용약의 검색

  • 성연희
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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    • pp.282-282
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    • 1994
  • Radioligand결합실험에 의하여 7가지 이상의 5-hydroxytryptamine serotonin, 5-HT)수용체 subtype가 규명되어 있고, 1983년 5-HT agonist로 알려져 있던 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT)가 〔$^3$H〕5-HT수용체에 대한 결합만을 선택적으로 억제하며, 본 수용체를 직접 표식함이 알려진 이래, 본 수용체의 기능에 대한 연구가 계속되어 오고있다. 특히 항불안약으로 임상에 사용되어 왔던 benzodiazepines이 5-HT neuron의 활성을 억제한다는 사실이 보고되면서 5-HT neuron과 불안과의 관련에 관한 연구가 계속되고 있는 가운데, 새로운 항불안약으로 주목을 받고 있던 buspirone이 5-$HT_{1A}$ 수용체에 높은 친화성을 가짐이 확인되었다. 그 외에도 5-$HT_{1A}$ 수용체작용약이 항우울약, 항고혈압약으로서의 응용가능성 이 시사되면서 본 수용체작용약의 개발 및 그 기능해명이 주목을 받고 있다. 본 연구에서는, 5-$HT_{1A}$ 수용체작용약인 8-OH-DPAT와 항불안약을 개발할 목적으로 합성된 화합물인 1-[3-(3,4-methylenedioxyphenoxy)propy〕-4-phenyl piperazine (8P-554)을 이용하여, 화합물의 5-HT$_{1A}$수용체에 대한 친화성을 검토하는 방법과. 본 수용체를 통하여 나타난다고 알려져 있는 5-HT의 약리작용을 검토하는 방법을 기술하므로서, 여러가지 임상적 응용을 위하여 새롭게 합성되는 화합물의 5-$HT_{1A}$ 수용체와의 상호작용을 검색하는 방법을 제시하고자 한다.다.

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신경약리학적 방법에 의한 $5HT_{1A}$ Receptor agonist의 평가

  • 김학성;성연희
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1992년도 제1회 신약개발 연구발표회 초록집
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    • pp.39-39
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    • 1992
  • 5-Hydroxytryptamine(serotonin, 5-HT)은 중추신경의 신경 전달물질로서 조울병, 불안신경증 등의 정신병태생리에 중요한 역할을 한다. Radioligand 결합실험에 의하여 5-$HT_{1A}$, 5-$HT_{1B}$, 5-$HT_{1C}$, 5-$HT_{1D}$, 5-$HT_{2}$, 5-$HT_3$의 5-HT receptor subtypes의 존재가 확인되어 있고, 그 중에서도 5-$HT_{1A}$ receptor는 중추작용 증 정 도의 조절에 관계가 깊은 raphe nuclei 및 해마에 주로 존재하여 약리학적으로는 체온강하, 혈압 강하, 과식작용, corticosterone 분비 등과 관련되어 있음이 알려져 있다. 따라서 본 수용체 agonist가 항불안약, 항우울약 또는 항고혈압약으로서의 응용이 가능해지면서 5-$HT_{1A}$ 수용체 기능의 해명 및 그 agonist의 개발이 주목받고 있는 가운데, 본 연구에 있어서, 항불안약 개발목적으로 합성된 일련의 화합물 중 1-<3-(3,4-methylene-dioxyphenoxy)propyl> 4-phenyl piperazine (DP-554)이 5-HT 수용체에 특이적이고 선택적으로 높은 친화성을 가지며, rat 해마의 막분획에서 adenylate cyclase 활성을 억제하고, 뇌내 5-HT turnover rate를 감소시키는 둥의 약리학적 작용을 나타내어, 이 화합물이 5-$HT_{1A}$ receptor agonist로서 작용함을 밝혔다. Mouse vas deferens (MVD)를 이용한 실험에서 5-$HT_{1A}$ receptor가 MVD의 교감신경 말단에 존재하여 그 neurotransmission을 억제함이 시사되었으며, 이 조직에서 또한 5-$HT_2$와 5-$HT_3$ 수용체의 존재를 확인하고 각각의 기능을 분명히 했다.

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Pharmacological Screening of Dikamali Resin Extract

  • Sridhar, S.K.;Ramachandran, S.;Anbalagan, N.;Leonard, J. Thomas;Joanofarc, J.;Kumar, S. Sadish
    • Natural Product Sciences
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    • 제9권1호
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    • pp.10-12
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    • 2003
  • In the present study, dikamali resin (obtained from the leaf buds and the young shoots of Gardenia gummifera Linn.) was extracted with diethyl ether and the extract was vacuum dried. Qualitative tests confirmed the presence of flavonoids and free phenolic compounds in the extract. The antioxidant property (qualitative) of the extract was performed by TLC method $({\beta}-carotene-linoleate method)$. The $LD_{50}$ of the extract was found to be 2227 mg/kg by Karber's arithmetic method. The extract was screened for analgesic, anti-inflammatory, antipyretic (100, 200 and 400 mg/kg) and anthelmintic (0.1,0.2 and 0.5%w/v) activities by standard methods. The extract exhibited antioxidant property and prevented oxidation of ${\beta}-carotene$. The extract exhibited significant graded dose response for analgesic, anti-inflammatory, antipyretic and anthelmintic activities. The extract caused the death of earthworms in all experimental concentration whereas the standard drug (piperazine) only effected paralysis. The present study proved the claims of dikamali resin mentioned in the Indian system of medicine.

Acute Cyclosporin A-Treatment Impairs the Cytosolic Guanylate Cyclase-Mediated Vasodilatation in Rat Thoracic Aorta

  • Kook, Hyun
    • The Korean Journal of Physiology and Pharmacology
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    • 제2권4호
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    • pp.471-477
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    • 1998
  • Cyclosporin A (CsA), a widely used immunosuppressant, is well known to cause nephrotoxicity and hypertension as major side effects. The present study was aimed at investigating the effects of CsA-pretreatment on the activities of cytosolic guanylate cyclase (cGC) in relation to the alteration of relaxant responses in the rat thoracic aorta. CsA $(10\;{\mu}M)-preincubation$ for 90 min significantly attenuated the vasodilatation induced by sodium nitroprusside (SNP), a cytosolic guanylate cyclase activator, shifting the dose-response curve to the right. The increase in cGMP contents induced by SNP was markedly attenuated by CsA. SNP ($1\;{\mu}M{\sim}\;mM$) increased the cGC activity dose-dependently, and the increase was completely abolished by CsA. CsA attenuated the SNP-induced cGC activation dose-dependently. The abolishing effect of CsA-pretreatment on the SNP-induced cGC activation was not affected by washing the preparation, suggesting that the inhibition is irreversible. When CsA was added simultaneously with SNP, cGC activation was not attenuated. 1-(5-isoquinolinylsulfonyl)-2-methyl piperazine (H-7), a protein kinase C (PKC) inhibitor, decreased SNP-induced cGC activation and blocked the CsA-attenuation of cGC activation. These results suggest that CsA directly inhibits cGC participating in the CsA-induced impairment of vasodilatation, and that PKC is involved in the inhibitory action of CsA on cGC.

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Lactobacillus acidophilus 88의 Protoplast 형성 및 재생에 관한 연구 (Studies on the Protoplast Formation and Regeneration of Lactobacillus acidophilus 88)

  • 전홍기;허경;조영배;백형석
    • 한국미생물·생명공학회지
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    • 제22권2호
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    • pp.143-151
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    • 1994
  • In the course of the study on strain inprovement by protoplast fusion, Lactobacillus acidophilus 88 protoplasts production and regeneration conditions were investigated. This strain produced a bacteriocin that revealed strong inhibitory activity against various indicator strains, especially L. helveticus CNRZ 1096. Protoplasts of L. acidophilus 88 strains were very efficiently obtained by treatment with 125 $\mu $g/ml lysozyme in a protoplast forming buffer containing 20 mM N-2 hydroxy-ethtl-piperazine-N'-2-ethane-sulfonic acid(HEPES, pH 7.0) and 1M sucrose at 37$\circ $C for 30 min. Hovever, treatment with mutanolysin was not effective for the production of L. acidophilus 88 protoplasts under the same conditions. High protoplast yield was obtained form the cells at the middle to late logarithmic growth phase in the de Man, Rogosa and Sharpe(MRS) medium. Regeneration was efficiently accomplished with the MRS medium containing 10% sucrose.

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Spectral, Electrochemical, Fluorescence, Kinetic and Anti-microbial Studies of Acyclic Schiff-base Gadolinium(III) Complexes

  • Vijayaraj, A.;Prabu, R.;Suresh, R.;Kumari, R. Sangeetha;Kaviyarasan, V.;Narayanan, V.
    • Bulletin of the Korean Chemical Society
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    • 제33권11호
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    • pp.3581-3588
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    • 2012
  • A new series of acyclic mononuclear gadolinium(III) complexes have been prepared by Schiff-base condensation derived from 5-methylsalicylaldehyde, diethylenetriamine, tris(2-aminoethyl) amine, triethylenetetramine, N,N-bis(3-aminopropyl)ethylene diamine, N,N-bis(aminopropyl) piperazine, and gadolinium nitrate. All the complexes were characterized by elemental and spectral analyses. Electronic spectra of the complexes show azomethine (CH=N) within the range of 410-420 nm. The fluorescence efficiency of Gd(III) ion in the cavity was completely quenched by the higher chain length ligands. Electrochemical studies of the complexes show irreversible one electron reduction process around -2.15 to -1.60 V The reduction potential of gadolinium(III) complexes shifts towards anodic directions respectively upon increasing the chain length. The catalytic activity of the gadolinium(III) complexes on the hydrolysis of 4-nitrophenylphosphate was determined. All gadolinium(III) complexes were screened for antibacterial activity.

Analysis of Diethylcarbamazine and Diethylcarbamazine-N-oxide by Gas Chromatography

  • Lee, Suk-Hyang;M.S;Pharm.D
    • Archives of Pharmacal Research
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    • 제19권6호
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    • pp.475-479
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    • 1996
  • Diethylcarbamazine (DEC, 1-diethylcarbamyl-4-methylpiperazine) is an antiparasitic piperazine derivative used in the treatment of lymphatic filariasis caused by Wuchereria bancrofti, Brugia malayi or grugia timori. DEC-N-oxide is a major metabolite in humans and has antifilarial activity. In carrying out pharmacokinetic studies, gas chromatographic analysis of DEC in plasma can be complicated by the presence of the metabolite, since the thermally unstable DEC-N-oxide is converted back to a material which coelutes with DEC under the conditions of the analysis. We now report a method to separate DEC-N-oxide from DEC in plasma using solid phase extraction with subsequent gas chromatographic analysis using a nitrogen specific detector. One-diethylcarbamyl-4-ethylpiperazine (E-DEC) was the internal standard. The standard curve of DEC was linear in the range of 10 to 200 ng/ml as described by Y=0.0350+0.0128X, $R^2=0.999$. The limit of quantitation was 4 ng/mL. Reproducibility at 10, 100 and 200 ng/mL concentration points of the standard curve gave coefficient variations of 6.1%, 7.8% and 1.6%, respectively. The recovery following solid phase extraction was 99.3% for DEC and 94.8% for the internal standard. This sensitive and specific analytical method is suitable for pharmacokinetic studies of DEC.

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Effects of a New Selective Phosphodiesterase Type 5 Inhibitor, KJH-1002, on the Relaxation of Rabbit Corpus Cavernosum Tissue

  • Cho, Eun-Young;Chung, Sung-Hyun;Kim, Joong-Hyup;Kim, Dong-Hyun;Jin, Cang-Bae
    • Biomolecules & Therapeutics
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    • 제11권4호
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    • pp.232-237
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    • 2003
  • The present study examined functional effects of a new selective phosphodiesterase type 5 inhibitor, 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-thioxo-3-propyl-1H-pyrazolo[ 4,3]pyrimidin-5-yl)phenylsulphonyl]-4-methyl piperazine (KJH-1002), in the isolated rabbit corpus cavernosum (RCC). Relaxing effects of KJH-1002 were also compared with those of sildenafil, which is currently used as an oral therapy for penile erectile dysfunction. In the isolated RCC precontracted with phenylephrine, both KJH-1002 and sildenafil in the concentration range of 1 to 1000 nM, produced a comparable potentiation of the electical field stimulation-induced relaxation in a concentration-dependent manner. In the sodium nitroprusside (SNP)-induced relaxation, the $IC_{50}$/ values, concentrations of SNP required to produce a 50% relaxation of the phenylephrine-induced contraction, were significantly decreased to the similar extent by treatments with KJH-1002 and sildenafil. The results suggest that a new selective phosphodiesterase type 5 inhibitor, KJH-1002, has an augmentative effect on penile erection comparable to that of sildenafil and can be useful for the treatment of erectile dysfunction.