• Title/Summary/Keyword: 길항제

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The Neurotransmitter Pathway of Itching (가려움증의 신경전달 경로)

  • Jo, Jeong Won;Kim, Chi-Yeon
    • Journal of Life Science
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    • v.27 no.5
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    • pp.600-610
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    • 2017
  • It was common that the classification of itching was classified into four categories according to the neurophysiological mechanisms of pruritoceptive itching, neuropathic itching, neurogenic itching and psychogenic itching. Recently it was classified by clinical criteria. The neurotransmission pathway of itch is divided into histamine-dependent pathway and histamine-independent pathway. Different receptors and neuropeptides act on each itch mediator. Itch mediators such as histamine, BAM8-22, and chloroquine are transmitted through the histamine-dependent pathway. Cowhage spicule, protease, and TSLP (Thymic stromal lymphopoietin) have been reported to be related to the histamine-independent pathway. These itch mediators, receptors, and neuropeptides are the targets of treatment for itching. Although itching and pain are typical noxious stimuli, and in the past, it was argued that two senses were transmitted through one noxious stimulus receptor. It has recently been shown that itching and pain have an independent neurotransmitter system and both neuronal systems inhibit each other. In addition, the mutual antagonism between itching and pain is explained by various mechanisms. Recently, many new mediators and receptors are being studied. The studies on histamine 4 receptor (H4 receptor) have been actively conducted. And the H4 receptors are expressed in immune cells such as T cells. The therapeutic agent for blocking the H4 receptor can inhibit the inflammatory reaction itself, which is important for the itching and chronicization. Understanding the underlying mechanisms of itching and studying new itch mediators will lead to the development of effective therapies, and this is what I think the itching study will go on.

STUDIES OF GINSENG EXTRACT ON AGE-RELATED ENZYMES (고려인삼 추출물이 노화관련효소에 미치는 영향)

  • Cho Young Dong;Koo Bon Sook;Lee Song Jae
    • Proceedings of the Ginseng society Conference
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    • 1984.09a
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    • pp.37-43
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    • 1984
  • 노화는 모든 다세포 유기물의 특징이다. 노화가 됨에 따라서 효소활성 및 면역반응의 감소와 과산화지질과 지방갈색물질의 축적, 효소와 염색질을 포함하는 단백질 구조의 변화, 호르몬계의 불균형 등이 일어난다. 그렇지만, 노화가 어떻게 일어나는지에 관하여는 현재까지 확실하지 않다. 본 연구진은 노화와 관련된 효소들에 관하여 연구를 하여 왔으며, 노화가 진행되는 동안의 효소의 활성을 유지시켜주거나, 또는 효소의 활성이 감소되는 것을 지연시켜 주는 물질을 찾고자 노력하였다. 그 가운데 하나로서, 고려인삼 추출물을 흰쥐에 기간별로 투여하여 효소활성의 차이, 열에 대한 안정성, 기질에 대한 친화력, 전기 영동 상의 이동성과 면역적인 반응을 대조군과 비교하였다. Glucose-6-phosphate dehydrogenase, 6-phosphog-luconate dehydrogenase, glutathione redutease, glutathion peroxidase와 같은 노화와 관련된 효소들의 활성을 고려인삼 추출물을 1개월간 흰쥐에 ($60{\~}80$g)투여하여 대조군과 비교 조사하였으나, 별 차이가 없었다. 그러나 고려인삼 추출물을 15개월간 투여하였을 때에는 이러한 노화관련 효소들의 활성이 급격히 증가함이 ($70{\~}200\%$) 관찰되었다. 예견된 바와 같이, 효소의 열에 대한 안정성과 기질에 대한 친화력도 증가함이 관찰되었다. 그러나 glucose-6-phosphate dehydrogenase의 경우에서 전기영동상의 차이 및 면역적인 반응은 대조군과 유사하였다. 이상의 결과는 고려인삼 추출물이 노화와 관련된 효소들의 활성이 감소되는 것을 지연시켜줄 수 있으며, 노화를 어느정도 지연시켜 줄 수 있음을 의미한다. 이와 같은 결과를 포함한 실험자료를 국제 인삼심포지움에서 발표할 것이다.$-tocopherol의 항 산화작용을 더욱 효과적으로 촉진 시킬 것으로 생각된다.-L(독성 호르몬-L)의 작용을 억제함으로서 암환자의 체중 감소를 방지하고, 식욕감퇴를 개선할것으로 생각된다.해되었으며, $Rb_{1}$은 장내의 효소와 tetracycline-resistantant bacteria에 의해 Rd와 2 종류의 미확인 물질로 분해되었다.xA_{2}$ synthetase 억제제인 imidazole의 효과와 유사하였다. 4. G-Re는 $1{\times}10^{-5}g/ml$ 이하의 농도에서는 효과가 없으나 $1{\times}10^{-4}g/ml$ 이상의 농도에서 농도의존적으로 유의성 있는 $PGE_{2},\;PGF_{2}{\alpha},\;TXB_{2}$의 생성억제와 함께 6-keto-$PGF_{1}{\alpha}$ 증가를 보였다. 이는 prostacyclin synthetase를 자극하는 serotonin의 효과와 같은 작용으로서 prostacyclin synthetase 억제제인 tranylcypromine에 대하여 길항효과를 보였다. 5. $TxB_{2}$생성억제 작용을 나타내는 ginsenoside들의 효과를 뒷받침하기 위하여 인삼 saponin 성분을 전처치한 patelet rich plasma에서 혈소판 응집시험 결과, ADP로 유도된 혈소판 응집반응에는 모든 인삼 saponin 성분들이 효과가 없었으나 arachidonic acid로 유도된 혈소판 응집반응에는 $G-Rb_{2}$, G-Rc, G-Re의 순으로 농도 의존적인 억제현상을 보였다. 이상의 결과와 같이 인삼 saponin 성분들은 arachidonic acid로부터 cyclooxygenase를

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Effect of Baclofen on the Cholinergic Nerve Stimulation in Isolated Rat Detrusor (흰쥐의 적출배뇨근에서 baclofen의 콜린성신경 억제작용)

  • Lee, Kwang-Youn;Lee, Keun-Mi;Choi, Eun-Mee;Choi, Hyoung-Chul;Ha, Jeoung-Hee;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.12 no.2
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    • pp.246-259
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    • 1995
  • This study aimed to investigate the mechanism of action of baclofen on the detrusor muscle isolated from rat. Rats (Sprague-Dawley) were sacrificed by decapitation and exsanguination. Horizontal muscle strips of $2mm{\times}15mm$ were prepared for isometric myography in isolated muscle chamber bubbled with 95% / 5%-$O_2$ / $CO_2$ at $37^{\circ}C$, and the pH was maintained at 7.4. Detrusor strips contracted responding to the electrical field stimulation (EFS) by 2 Hz, 20 msec, monophasic square wave of 60 VDC. The initial peak of EFS-Induced contraction was tended to be suppresed by ${\alpha},{\beta}$-methylene-adenosine 5'-triphosphate (mATP), a partial agonist of purinergic receptor, and baclofen, a $GABA_B$ receptor agonist (statistically nonsignificant). The late sustained contraction by EFS was suppressed significantly (p < 0.05) by additions of atropione, a cholinergic muscarinic receptor antagonist and baclofen. The adenosine 5'-triphosphate-induced contraction was completely abolished by mA TP but not by baclofen. In the presence of atropine, the subsequent addition of acetylcholine could not contract the muscle strips: but the addition of acetylcholine in the presence of baclofen evoked a contraction to a remarkable extent. These results suggest that in the condition of present study, the cholinergic innervation may play a more important role than the purinergic one, and baclofen suppresses the contractility of rat detrusor by the stimulation of the $GABA_B$ receptors to inhibit the release of neurotransmitter from the cholinergic nerve ending.

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Combined Effect of Afidopyropen, Chlorfenapyr and Cyantraniliprole to Insecticide-resistant Cotton Aphid, Aphis gossypii (Hemiptera: Aphididae) (살충제 저항성 목화진딧물에 대한 afidopyropen과 chlorfenapyr, cyantraniliprole의 혼합효과 평가)

  • Dong-Hyun Kang;Yuno Lee;Ha Hyeon Moon;Se Eun Kim;Hyun-Na Koo;Hyun Kyung Kim;Gil-Hah Kim
    • Korean journal of applied entomology
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    • v.63 no.1
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    • pp.53-61
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    • 2024
  • The susceptibility of Aphis gossypii populations collected from three fields (WJ, CC, and GS) was evaluated to three insecticides (afidopyropen, chlorfenapyr and cyantraniliprole) and three binary mixtures. Three field populations showed resistance ratios of over 100 to all insecticides. The Combination Index (CI), %M(synergism), Co-Toxicity Coefficient (CTC), Wadley Ratio (WR), Synergism Ratio (SR) and Abbott Ratio (AR) were used to evaluate combined effect of the insecticides. Afidopyropen + chlorfenapyr (CI ≤ 0.16; %M(synergism) ≥ 94; CTC ≥ 764.5; WR ≥ 6.4; SR ≥ 6.9 and AR ≥ 1.1) showed a synergism in all filed populations. WJ and CC populations showed a synergism in all binary mixtures of insecticides, but GS population showed an antagonism for chlorfenapyr + cyantraniliprole (CI, 1.63; %M(synergism), 30; CTC, 64.0; WR, 0.6 and AR, 0.54) and afidopyropen + cyantraniliprole (CI, 6.7; %M(synergism), 1; CTC, 19.8; WR, 0.2 and AR ≤ 0.55). All mixtures (afidopyropen + chlorfenapyr, chlorfenapyr + cyantraniliprole and afidopyropen + cyantraniliprole) showed a control value of over 99% after 21 days of treatment in the field. This study highlights that binary mixtures of three insecticides serve as an effective control strategy for A. gossypii.

Effect of Diazepam on the Oxytocin Induced Contraction of the Isolated Rat Uterus (Oxytocin의 자궁수축작용에 미치는 Diazepam의 영향)

  • Park, Yoon-Kee;Lee, Sung-Ho;Kwon, Oh-Cheol;Ha, Jeoung-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.9 no.2
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    • pp.359-381
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    • 1992
  • This study was designed to investigate the effect of diazepam on the spontaneous contraction and oxytocin induced contraction of the isolated rat uterus. Female rat(Sprague-Dawley) pretreated with oophorectomy and 4 days administration of estrogen, weighing about 200 g, was sacrificed by cervical dislocation, and the uteruses were isolated. A longitudinal muscle strip was placed in temperature controlled($37^{\circ}C$) muscle chamber containing Locke's solution and myographied isometrically. Diazepam inhibited the spontaneous contraction and oxytocin induced contraction of the isolated rat uterus in a concentration-dependent manner. GABA, muscimol, a GABA A receptor agonist, bicuculline, a competitive GAGA A receptor antagonist, picrotoxin, a non competitive GABA A receptor antagonist, baclofen, a GABA B receptor agonist, and delta-aminovaleric acid, a GABA B receptor antagonist, did not affect on the spontaneous and oxytocin induced contraction of the isolated rat uterus. The inhibitory actions of diazepam on the spontaneous and oxytocin induced contraction were not affected by all the GABA receptor agonists and antagonists, but exceptionally potentiated by bicuculline. This potentiation-effect by bicuculline was not antagonized by muscimol. In normal calcium PSS, addition of calcium restored the spontaneous contraction preinhibited by diazepam and recovered the contractile of oxytocin preinhibited by diazepam. A23187, a calcium inophore, enhanced the restoration of both the spontaneous and oxytocin induced contraction by addition of calcium. In calcium-free PSS, diazepam suppressed the restoration of spontaneous motility by addition of calcium but allowed the recovery of spontaneous motility to a considerable extent. Diazepam could not inhibit some development of contractility by oxytocin in calcium-free PSS, but inhibited the increase in contractility by subsequent addition of calcium. These results suggest that the inhibitory action of diazepam on the rat uterine motility does not depend on or related to GABA receptors and that diazepam inhibits the extracellular calcium influx to suppress the spontaneous and oxytocin induced contractilities.

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Control effect of the Mixture of Bacillus amyloliquefaciens M27 and Plant Extract against Cucumber Powdery Mildew (Bacillus amyloliquefaciens M27과 식물천연물 혼합제에 의한 오이 흰가루병의 방제 효과)

  • Lee, Sang Yeob;Weon, Hang Yeon;Kim, Jeong Jun;Han, Ji Hee;Kim, Wan Gyu
    • The Korean Journal of Pesticide Science
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    • v.17 no.4
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    • pp.435-439
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    • 2013
  • Bacillus amyloliquefaciens M27 was selected as a control agent for the biological control of cucumber powdery mildew. The new mixture of B.amyloliquefaciens M27 and plant (Eucalytus) extract was developed to improve the control activity of B.amyloliquefaciens M27 against cucumber powdery mildew. The mixed formulation showed the high preventive and curative control effect against cucumber powdery mildew when it was diluted at 500 times and foliar-sprayed. Its control effect was higher in preventive spraying than curative spraying. When 500-fold diluted solution of the formulation was sprayed preventively four times at five-day intervals, three times at seven-day intervals and twice at ten-day intervals, the diseased leaf area was shown to be 4.4%, 8.0%, 27.9%, respectively; Whereas the diseased leaf area in the control plot was 45.4%. When the 500-fold diluted formulation was sprayed curatively four times at five-day intervals, three times at seven-day intervals and twice at ten-day intervals after occurred cucumber powdery mildew, the diseases leaf area was 11.5%, 25.2%, 51.8%, respectively; whereas in the control plot, the diseases leaf area was 64.3%. When the 500-fold diluted formulation was treated four times at five-day intervals in the plastic house, its control effect was higher than that treated three times at seven-day intervals and twice at ten-day intervals. As the results, the mixed formulation of B.amyloliquefaciens M27 and plant extract could be a promising candidate of bio-fungicides for the environment-friendly control of powdery mildew of cucumber.

A Study on the Post-Receptor Mechanism of Adenosine Receptor on Acetylcholine Release in the Rat Hippocampus (흰쥐 해마에서 Acetylcholine 유리에 관여하는 Adenosine Receptor의 Post-Receptor 기전에 관한 연구)

  • Choi, Bong-Kyu;Oh, Jae-Hee
    • The Korean Journal of Pharmacology
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    • v.30 no.3
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    • pp.263-272
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    • 1994
  • Since it was been reported that the depolarization-induced ACh release is inhibited by activation of presynaptic $A_1-adenosine$ heteroreceptor in hippocampus, a large body of experimental data on the post-receptor mechanism of this process has been accumulated. But, the post-receptor mechanism of presynaptic $A_1-adenosine$ receptor on the ACh release has not been clearly elucidated yet. Therefore, it was attempted to clarify the post-receptor mechanisms of the $A_1-adenosine$ receptor-mediated control of ACh release in this study. Slices from rat hippocampus were equilibrated with $^3H-choline$ and the release of the labelled products was evoked by electrical stimulation (3 Hz, 5 $VCm^{-1}$, 2ms, rectangular pulses), and the influence of various agents on the evoked tritium-outflow was investigated. Adenosine, in concentrations ranging from $0.3{\sim}300\;{\mu}M$, decreased the ACh release in a dose-dependent manner, without affecting the basal rate of release. The adenosine effects were significantly inhibited by $DPCPX\;(2\;{\mu}M)$, a selective $A_1-receptor$ antagonist. The responses to N-ethylmaleimide $(10&30{\mu}M)$, a SH-alkylating agent of G-protein, were characterized by increments of the evoked ACh-release and the basal release, and the adenosine effects were completely abolished by NEM pretreatment. PDB $(1{\sim}10\;{\mu}M)$, a specific protein kinase C (PKC) activator, increased, whereas PMB $(0.03{\sim}1\;mg)$, a PKC inhibitor, decreased the evoked ACh-release, and the adenosine effects were not affected by these agents. Nifedipine $(1\;{\mu}M)$, a $Ca^{2+}\;-channel$ blocker of dihydropyridine analogue, significantly inhibited the adenosine effect, but glibenclamide, a $K^+-channel$ blocker, did not. Finally, 8-bromo cyclic AMP $(100\;&\;300{\mu}M)$, a membrane-permeable analogue of cAMP, did not alter the ACh release, but adenosine effects were inhibited by pretreatment with large dose of 8-br-cAMP $(300\;{\mu}M)$. These results indicate that the decrement of the evoked ACh-release by $A_1-adenosine$ receptor is mediated by the G-protein, and nifedipine-sensitive $Ca^{2+}-channel$ and adenylate cyclase system are coupled partly to this effect, and that protein kinase C and glibenclamide-sensitive $K{^+}-channel$ are not involved in this process.

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Involvement of Serotonergic Mechanism in the Nucleus Tractus Solitarius for the Regulation of Blood Pressure and Heart Rate of Rats (흰쥐의 혈압 및 심박동수 조절에 대하여 Nucleus Tractus Solitarius 부위의 Serotonin성 기전의 역할)

  • Lee, Yong-Kyu;Hong, Ki-Whan;Yoon, Jae-Soon
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.1-11
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    • 1989
  • In this study, it was aimed to investigate the role of serotonergic neurotransmission in nucleus tractus solitarius (NTS) for the central regulation of blood pressure and heart rate and its involvement in baroreceptor reflex activation in rats. A microinjection of 5-hydroxytryptamine (5-HT) into the NTS produced decreases in blood pressure and heart rate. Maximal decreases were $34.4{\pm}1.6$ mmHg and $41.7{\pm}10.2$ beats per min by 300 pmol of 5-HT. Microinjections of ${\alpha}-methylnor-adrenaline$ $({\alpha}-MNE)$ and clonidine manifested similar decreases in blood pressure and heart rate. The hypotensive and bradycardial effects of 5-HT were blocked by previous applications of 5-HT antagonists, ritanserin, methysergide and ketanserin into the NTS, respectively. By pretreatment with reserpine and 6-hydroxydopamine (6-OHDA, i.c.v.), both hypotensive and bradycardial effects of 5-HT were significantly attenuated. Pretreatment with 5, 7-dihydroxytryptamine (5,7-DHT, i.c.v.) enhanced the hypotensive and bradycardial effects of 5-HT. Similarly, following pretreatment with 6-OHDA, the effects of clonidine were increased. Pretreatment either with 5,7-DHT or 6-OHDA significantly attenuated the sensitivity of baroreflex produced either by phenylephrine or by sodium nitroprusside. When either 5,7-DHT or 6-OHDA was injected into the NTS $(5,7-DHT;\;8{\mu}g\;6-OHDA;\;10{\mu}g)$, both of the baroreflex sensitivities were impaired. In the immunohistochemical study, the injection of 6-OHDA into the the NTS led to reduction of axon terminal varicosity, however, the injection did not reduce the numbers of catecholaminergic cell bodies. Likewise, when 5,7-DHT was injected into the NTS, the varicosity of serotonergic axon terminals was markedly reduced. Based on these results, it is suggested that (1) stimulation of serotonergic receptors in the NTS leads to decreases in blood pressure and heart rate as observed with the stimulation of catecholaminergic system, (2) both serotonergic and catecholaminergic receptors may be located postsynaptically, and (3) the serotonergic neurons as well as catecholaminergic neurons may have a close relevance for the activation of baroreflex.

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Efficacy of Suppression of Phytophthora Blight of Red Pepper Caused by Phytophthora capsici by Treatment with Antagonistic Trichoderma harzianum DYMC in Greenhouse (온실에서 길항미생물 Trichoderma hazianum DYMC 처리에 의한 고추 역병 억제 효과)

  • Lee, Yong-Se;Chang, Tae-Hyun;Ryu, Yeon-Ju;Park, Jeong-Yong;Lim, Tae-Heon
    • Korean Journal of Environmental Agriculture
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    • v.24 no.4
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    • pp.409-415
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    • 2005
  • To control Phytophthora blight of red pepper biologically caused by Phytophthora capsici, we developed Trichoderma harzianum DYMC for commercial product. DYMC was storage at room temperature and was investigated their population every 3 months for 1 year. For investigating the dynamic population of T. harzianum in the pot soils, we applied powder and suspension applications with DYMC, and then investigated for 95 days. The efficacy of powder and suspension applications of DYMC for control of Phytophthora blight of red pepper and plant growth were investigated for 50 days in greenhouse experiment. The population of T. harzianum was decreased at the room temperature for 1 year but there was not statistically significance. After soil treated in the pot with DYMC, the population of Trichoderma spp. was the highest when DYMC powder at 5 g was applied to mix with pot soil, and the population was deceased significantly among treatment means as time goes by ($R^2=0.76$, F=10.5960, P=<.0001). Incidence of Phytophthora blight of, red pepper was significantly reduced among treatment means on 50th day after treated with DYMC ($R^2=0.82$, P=16.4758, P=<.0001). Disease control value was the highest at 62.5% when DYMC powder at 5 g was applied to mix with pot soil. No significant difference (P=0.05) of effects of plant and root growth showed by treated with DYMC on 60th day, except stem. Mixing the application of DYMC powder with soil to control Phytophthora blight of red pepper was greater than suspension application to dilute with water. DYMC could be used as an effective biocontrol agent to control Phythophthora blight of red pepper.

Automated Synthesis of [$^{18}F$]Fallypride for Routine Clinical Use (자동합성장치를 이용한 [$^{18}F$]Fallypride의 합성)

  • Park, Jun-Hyung;Moon, Byung-Seok;Lee, Hong-Jin;Lee, Hyo-Jun;Lee, In-Won;Lee, Byung-Chul;Kim, Sang-Eun
    • The Korean Journal of Nuclear Medicine Technology
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    • v.14 no.2
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    • pp.104-109
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    • 2010
  • Purpose: $[^{18}F]$Fallypride plays an effective radiotracer for the study of dopamine $D_2/D_3$ receptor occupancy, neuropsychiatric disorders and aging in humans. This tracer has the potential for clinical use, but automated labeling efficiency showed low radiochemical yields about 5~20% with relatively long labelling time of fluorine-18. In present study, we describe an improved automatic synthesis of [$^{18}F$]Fallypride using different base concentration for routine clinical use. Materials and Methods: Fully automated synthetic process of [$^{18}F$]Fallypride was perform using the TracerLab $FX_{FN}$ synthesizer under various labeling conditions and tosyl-fallypride was used as a precursor. [$^{18}F$]Fluoride was extracted with various concentration of $K_{2.2.2.}/K_2CO_3$ from $^{18}O$-enriched water trapped on the ion exchange cartridge. After azeotropic drying, the labeling reaction proceeded in $CH_3CN$ at $100^{\circ}C$ for 10 or 30 min. The reaction mixture was purified by reverse phase HPLC and collected organic solution was exchanged by tc-18 Sep-Pak for the clinically available solution. Results: The optimal labeling condition of [$^{18}F$]Fallypride in the automatic production was that 2 mg of tosyl-fallypride in acetonitrile (1 mL) was incubated at $100^{\circ}C$ for 10 min with $K_{2.2.2.}/K_2CO_3$ (11/0.8 mg). [$^{18}F$]Fallypride was obtained with high radiochemical yield about $66{\pm}1.4%$ (decay-corrected, n=28) within $51{\pm}1.2$ min including HPLC purification and solid-phase purification for the final formulation. Conclusion: [$^{18}F$]Fallypride was prepared with a significantly improved radiochemical yield with high specific activity and shorten synthetic time. In addition, this automated procedure provides the high reproducibility with no synthesis failures (n=28).

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