• Archives of Pharmacal Research
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• 제17권5호
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• pp.304-308
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• 1994

Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the phamacological properties of KR-25018 were compared with those of morphine, capsaicin, and nonsteroidal antiinflammatory drugs (NSAIDs). The analgesic activities were evaluated in several animal models, using different stimuli, such as phenylbenzoquinone(PBQ)-induced weithing test, tail-filck test in mice and adjuvant arthritic flexion test in rat. The relationship of phamacological properties of KR-25018 to that of centrally acting opioids was assessed by the blocking test using naloxone. The analgesic potency of the KR-25018 $(MPED_{50}=0.89{\;}p.o.{\;}in{\;}PBQ-induced{\;}weithing{\;}test, {\;}MPED_{50}$=0.61$ s.c. in tail-flick test in mice0, with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.

• Biomolecules & Therapeutics
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• 제7권2호
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• pp.198-203
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• 1999

Loxoprofen-Na (sodium 2-〔4-(2-oxocyclopentylmethyl)pheny)propionate dihydrate) is a potent analgesic drug. We developed loxoprofen-Na plasters to extend duration time of analgesic activity and to reduce side effect on gastrointestinal tract. Analgesic effect of Loxoprofen-Na plasters was investigated. Loxoprofen-Na plaster had good analgesic effect in rat paw pressure test, Tail-flick latency test and acetic acid-induced writhing test. Also, it had anti-inflammatory effect on carrageenan-induced rat hind paw edema. In pharmacokinetic study of Loxoprofen-Na, plasters dosage form showed that plasma drug concentration was prolonged up to 14 hours. So, we can conclude that loxoprofen-Na plasters, when applied on skin, will be a new type of drug for controlling the various local pain or inflammation.

• Journal of Preventive Medicine and Public Health
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• 제26권2호
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• pp.222-230
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• 1993

본드라고 불리우는 공업용 접착제는 수종의 유기용제를 함유하고 있으므로 본드 흡입은 단일 유기용제 흡입과는 다른 독성을 나타낼 수 있다. 공업용 접착제에서 휘발한 유기용제를 흡입하여 반복적으로 급성 중추신경계 억제증상에 이르렀던 어린 백서가 급성 중독증상이 소실된 후에도 체중증가의 둔화나 중추신경계 기능이상 혹은 만성 비가역적 중추신경계 이상이 유발되는가를 검증하고자 주령이 6주인 어린 웅성 백서 20 마리를, 폭로장치를 이용하여 $40^{\circ}C$의 평판위에서 가열한 30g의 본드에서 발생하는 유기용제 증기에 4주간에 걸쳐서 1회에 30분씩 21회 반복 폭로시켜서 폭로군으로 하였고. 이와 함께 동일한 주령의 백서 20마리를 같은 조건으로 대기에 폭로시켜서 대조군으로 하였다. 그후 6 개월동안 동일한 환경하에서 사육하면서 시간경과에 따라서 체중을 측정하였고 tail flick 검사, hot plate 검사, treadmill 검사를 실시한 다음 뇌를 적출하여 육안과 현미경으로 신경조직의 변화유무를 관찰하였다. 시간의 변화를 고려한 폭로군과 비교군간의 비교에서 체중 증가는 양군간에 유의한 차이를 나타냈으나, tail flick 검사, hot plate 검사, rotarod treadmill검사 등의 결과에서는 양군간의 차이를 발견할 수 없었다. 눈가림법을 적용한 현미경적인 비교에서나, 적출한 대뇌와 소뇌의 크기의 비교에서도 양군간 유의한 차이는 없었다. 이상의 결과에 의하면 본드흡입은 정상발육에 의한 체중증가를 저해하는 것으로 보인다. 한편 본 연구의 결과만으로 본드흡입이 백서나 인체의 신경계에 영구적인 손상을 유발하지 않는다고 결론짓기는 어려우며. 다양한 폭로조건으로 연구를 시행한 후에만 이러한 가설에 대한 평가가 가능할 것으로 생각된다. 철과 Sc척도, Pt척도는 양의 상관 관계를 보이고 있다. 본 연구의 결과로 볼때 비폭력범죄자와 정상 대조군 사이에서 일부 금속원소의 함량 차이가 있는 것으로 보여지며, 금속원소 함량과 MMPI 척도와도 상관관계가 있는 것으로 나타났다. 향후 폭력범과 비폭력범, 폭력범과 일반인과의 차이를 비교하여 볼 필요성을 느낀다.으로 현저히 증가되어 있었다. 이상의 결과로 규폐증에서는 일반적인 건강진단 항목상의 신기능 검사에 이상소견을 보이지 않은 경우라도 신장기능의 변화가 동반될 수 있으며, 요중 NAG 활성치를 분진 폭로 근로자에게 적용하면 산업보건학적 측면에서 근로자의 건강관리를 위하여 매우 유익한 자료가 될 것으로 생각한다.견해를 보였으나 약국의료보험이용은 극히 저조하고 의사의 처방전 발행도 저조한 실정이다. 이에 약국의료보험제도에서 의약분업제도로의 제도적 전환이 고려되어야 할 것으로 생각된다. 둘째, 의사와 약사의 의약분업에 대한 의견이 상이한 점으로 미루어 유추할 수 있지만 의약분업제도 실시의 장애요인으로 의 약사단체 상호간의 업권문제와 의약사간의 갈등이 지적되는 바, 이들 모두를 만족 할 대안을 선택하는 것이 쉬운일 아닐 것이므로 국민의 건강보호차원에서 정부의 중립적 의지가 있어야 할 것으로 생각된다.의 비율이 감소하였으나 본태성고혈압, 당뇨병, 폐결핵, 협심증 둥의 비율이 증가하였다. 일반외과의 경우에는 치핵, 항문열상, 종기 등의 비율이 감소하였고, 위암, 대장암, 담낭암 등의 비율은 증가하였다. 소아과의 경우 급성상기도염, 기관지염, 불명확한 장관감염 등의 비율은 감소하였고, 간질, 폐결핵, 천식, 임파성백혈병 등은 증가하였다. 이상의 결과로 보아 의료전달체계가 실시됨으로써 3차 진료기관의 외래 방문 환자의 건수, 건당 진료기간, 건당 방문횟수, 건당 검사건수, 건당

• Journal of Acupuncture Research
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• 제23권4호
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• pp.149-162
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• 2006

Objectives : The aim of this study is to evaluate the analgesic effect of electroacupuncture on Jogsamni (ST36) in the collagen-induced arthritis rats and investigate the role played by opioid receptor subtypes $({\mu},\;{\delta},\;{\kappa})$ in the antinociceptive effect of electroacupuncture (EA) In the thermal hyper algesia test. Methods : Immunization of male Sprague-Dawley rats with bovine type H collagen emulsified in incomplete Freund's adjuvant, followed by booster injection 2 weeks later induced collagen-induced arthritis (CIA). The thermal hyperalgesia was evaluated weekly with tail flick latency (TFL). In the fourth week after first immunization, EA stimulation (2 Hz, 0.07 mA, 0.3 ms) was delivered into Jogsamni (5736) for 20 minutes. Analgesic effect was evaluated by using the tail flick latency (TFL) after intraperitoneal injection of normal saline, naloxone, naltrindole and nor-binaltorphimine respectively to CIA rats. Results : The results were as follows; 1. The TFL were gradually decreased in CIA as time elapsed after e immunization of arthrogenic collagen and the maximum value was reached between the third to fifth week. 2. EA stimulation on 5736 inhibited chronic inflammatory pain induced by CIA. 3. The analgesic effect of EA was inhibited by pretreatment of ${\mu}-receptor$ antagonist (naloxone),${\delta}-receptor$ antagonist (naltrindole) and ${\kappa}-receptor$ antagonist (nor-binaltorphimine) respectively. Conclusion : Electroacupuncture has an analgesic effect on the CIA rat and has an antinociception mediated by 8, 5, H receptors.

• 약학회지
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• 제43권2호
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• pp.263-273
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• 1999

When glutamate was infected intrathecally, the result is similar to those produced by TPA injected. The involvement of protein kinase C (PKC) in the nociceptive responses in rat dorsal horn neurons of lumbar spinal cord was studied. In test with formalin, a PKC inhibitor (chelerythrine) inhibited dose-dependently the formalin-induced behavior response. Neomycin also inhibited it significantly. But, a PKC activator (12-O-tetradecanoylphorbol-13-ester, TPA) showed reverse effect. When gluatamate was injected intrathecally, we observed the result is smilar to those produced by TPA injection. On the other hand, intrathecal injection of glutamate induced thermal and mechanical hyperalgesia. In Tail-flick test, we examined the involvement of PKC on the glutamate-indeced thermal hyperalgesia. Chelerythrine showed an inhibitory effect and TPA enhanced thermal response. Glutamate decreased the mechanical threshold significantly. A pretreatment of chelerythrine and neomycin inhibited glutamate-induced mechanical hyperalgesia, but the effect of neomycin was not significant. TPA had little effect on the mechanical nociceptive response. These results suggest that the PKC activation through metabotropic receptor at postsynaptic region of spinal cord dorsal horn neurons may influence on the persistent nociception produced by chemical stimulation with formalin, thermal and mechanical hyperalgesia induced by glutamate.

• Advances in Traditional Medicine
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• 제7권5호
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• pp.501-508
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• 2008

Anti-nociceptive and anti-inflammatory effects of Clematidis Radix (CR)-distillates were investigated in three different pain animal models. Highly purified distillate of CR was injected to Zusanli (ST36) acupoint, called CR herb-acupuncture in the Korean traditional medicine. In tail flick latency test, the CR herb-acupuncture treatment did not show a significant effect of relieving acute phasic pain. To investigate the anti-inflammatory effect of CR herb-acupuncture, inflammatory pain was induced by subcutaneous injection of formalin to the plantar tissue or intra-articular injection of carrageenan to the tibio-tarsal joint in the rats. And the medicinal effect of CR herb-acupuncture was evaluated by analyzing pain behavior such as licking or biting behavior, or by measuring weight distribution ratio between two foot and ankle circumference. In the rat formalin test, the analgesic effect of CR herb-acupuncture was more pronounced in the late phase (for 20 min after the early phase) than in the early phase (for the first 10 min post formalin injection). It also significantly alleviated the carrageenan-induced monoarthritis, in terms of weight distribution ratio and ankle edema. These results revealed that CR herb-acupuncture was effective to treat the inflammatory pain and could be used as an analgesic treatment with an antiinflammatory effect.

• The Journal of Korean Physical Therapy
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• 제16권2호
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• pp.181-194
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• 2004

The aim of this study was to investigate the effects of TENS and cold application on secondary thermal hyperalgesia in rats induced by muscle pain. Muscle pain was induced in male Sprague-Dowley rats by intra-muscular injection of gastrocnemius with $3\%$ carrageenan. The paw withdrawal latency(PWL) and tail flick test(TFT) to heat were used to detect secodary thermal hyperalgesia induced by the muscle pain. PWL and TFT were quantified before and 4, 10, and 24 h after induction of muscle pain and after application of TENS(100Hz, $100{\mu}s$, sensory intensity) and cold($4^{\circ}C$). TENS and cold significantly reduced the PWL and TFT to heat stimuli when compared with controls receiving no TENS and cold(p<.05). These results suggested that application of TENS and cold attributed to decrease secodary thermal hyperalgesia in rat induced by muscle pain.

• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.273-278
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• 2000

Several topical preparations containing lidocaine, a widely used local anesthetic agent, have been developed and marketed recently for the treatment of premature ejaculation. In this study, microemulsion(ME)-based hydrogels containing lidocaine were prepared by dispersing ME to hydrogel bases such as Carbopol, sod. alginate, and sod. carboxymethylcellulose. Lidocaine-containing ME was thermodynamically stable over 6 months and had a diameter ranging from 10 to 100 nm. In vitro skin penetration of lidocaine from ME-based hydrogels followed apparent zero-order kinetics. ME-based hydrogel showed higher drug penetration during fifteen minutes after application than alcoholic hydrogel, reference preparation. Tail flick test in rat was introduced to compare in vivo local anesthetic effects of different hydrogels, and the results showed that ME-based hydrogels are superior to other hydrogels. In optical microscopy, recrystallization of lidocaine was observed within 5 min after application of reference hydrogel, but there was no change in ME-based hydrogels even after 30 minnute. These results indicated that ME-based hydrogels had some advantages in skin penetration, anesthetic effect and physical stability compared with alcoholic hydrogels. Finally it is possible to conclude that ME-based hydrogels containing lidocaine is a good topical drug delivery system for the treatment of premature ejaculation.

• 한국임상수의학회지
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• 제27권6호
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• pp.674-678
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• 2010

Medetomdine의 투여가 흰쥐의 진통과 진정효과에 미치는 영향에 대하여 평가하였다. 실험동물은 생리식염수 1 ml/kg 투여군 (group 'Saline'), butorphanol, 2.0 mg/kg 투여군 (group 'BUT'), medetomidine, 0.2, 0.4, 0.8 or 1.6 mg/kg 투여군 (각각 group 'MED0.2', 'MED0.4', 'MED0.8' and 'MED1.6') 등 6개의 실험군으로 나누어졌다. 진통효과는 $50^{\circ}C$ hot-water tail-flick latency test로 측정하였고, 진정효과는 numerical sedation score (NSS)와 정위반사 (righting reflex)로 평가하였다. MED0.2군을 제외한 모든 medetomidine 투여군들이 Saline군에 비해 유의적인 진통효과의 증가를 보였다. MED0.2군과 비교할 때 MED0.4와 MED0.8군은 유의적인 진통효과의 상승을 보였으나, MED1.6군은 유의적인 변화를 보이지 않았다. BUT군과 모든 medetomidine 투여군은 진통효과에서 유의적인 차이를 보이지 않았다. Saline과 butorphanol의 투여는 진정효과와 정위반사의 소실을 유발하지 않았다. Medetomidine의 투여 용량의 증가는 진정효과를 증가시켰다. MED0.2군과 비교할 때 MED0.4, MED0.8과 MED1.6군의 NSS가 유의적으로 증가하였으나, MED0.4군에 비해서는 MED0.8과 MED1.6군이 유의적인 차이를 나타내지 않았다. 정위반사의 소실 시간은 MED0.2군에 비해 MED0.8과 MED1.6군이 유의적으로 감소하였다. 본 실험의 결과로 볼 때, 흰쥐에서 medetomidine 0.4에서 0.8 mg/kg 이내의 용량을 복강내 투여할 때 신뢰할 수 있는 진통효과와 진정효과를 동시에 얻을 수 있으며, 따라서 흰쥐의 진정, 진통 및 화학적 보정 목적에 적절한 용량임을 알 수 있었다.

• Journal of Acupuncture Research
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• 제18권1호
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• pp.76-87
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• 2001

Objective : Zusanli(ST36) and Hoku(Li4) are analgesic acupuncture points frequently used for acupuncture in Oriental medicine. The present study was conducted to see the antinociceptive effects produced by electroacupuncture combined two frequencies(Low, High) and two different acupuncture points(LI4, ST36) in the rat tail flick test. Method : In this study the Rats (Sprague-Dawley, 250-300g) were partially anesthetized with thiopental sodium(40mg/kg, i.p.). The basal reaction time for the tail-flick was 3${\pm}$0.5 sec. Low frequency(3Hz, 5V, biphasic) and high frequency(100Hz, 5V, biphasic) were applied to the inserted needle for the period of insertion(twenty minutes). Experimental groups are divied as follow; a) electroacupuncture stimulation groups at Hoku with or high frequency(L-EA, H-EA), b) electroacupuncture stimulation groups at Zusanli with low or high frequency(1-EA, h-EA), c) low frequency at Hoku and Zusanli(LIEA), d) low frequency at Hoku and high frequency at Zusanli(LhEA), e) high frequency at Hoku and low frequency at Zusanli(HIEA), f) high frequency at Hoku and Zusanli(HhEA) Results : The individual stimulation at either Hoku or Zusanli with low frequency has stronger and longer analgesic effect than high frequency stimulation. In addition, the combined stimulation at Hoku and Zusanli with low frequency has superior effect to individual stimulation with low frequency. LhEA and LIEA have superior effect to other stimulation groups among the combined groups. In order to determine the involvement of opioid system on the different antinociceptive effects, Naloxone, an opioid antagonist, was used in the combined groups. LIEA is the most sensitive when naloxone was administrated among study groups. HhEA is the least sensitive in the administration of naloxone. Conclusion : From results, this study confirmed that the opioid system is involved in analgesic effect of low frequency stimulation of acupuncture point, and we also can suggest the stronger analgesic effect of combining stimulation points is due to the theory of spatial summation in the nervous system.