• The Korean Journal of Pain
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• v.7 no.1
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• pp.1-12
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• 1994

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.70-81
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• 2000

DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag$\varepsilon$nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$st. Pharmacokinetics of DA-50 18 were studied after topical application of ${14}^C$-Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in

• Journal of Veterinary Clinics
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• v.22 no.1
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• pp.6-15
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• 2005

This study was performed to investigate non-invasive behavioral pain assessment of dogs after surgery, and the analgesic effects of butorphanol after intestinal anastomosis in dogs. In this study, five dogs in the Control Group were anesthetized, but did not undergo surgery. Five dogs in the Analgesic Group were undergone intestinal anastomosis and treated with butorphanol. Five dogs in the Non-analgesic Group were also undergone intestinal anastomosis without analgesic treatment. The dogs in the Analgesic Group received butorphanol (0.4 mg/kg, IM) before and immediately after operation, while dogs in Control and Non-analgesic Groups received isovolumetric doses of sterile saline. The behavior of dogs were videotaped for 400 mins after anesthesia, during which time a researcher interacted with the dog once per each 80 mins. At each interaction, the researcher recorded behavioral pain score, using University of Melbourne Pain Scale. Interactive and non-interactive behaviors were observed and quantitated by a single observer using focal continuous sampling method. Vocalizations were obtained during 400 mins after anesthesia, and duration of call, intensity, pitch, 1-4 Formant were analyzed. Surgery affected an increasing of pain score. During interactions with researcher, greeting behaviors were decreased after surgery. Differences between Analgesic group given analgesic or that given a placebo drug were readily understood using quantitative behavioral measurements and vocalization. Significant difference between Analgesic group given butorphanol or that the given placebo drug was apparent(p< 0.05).

• Toxicological Research
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• v.11 no.1
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• pp.63-68
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• 1995

N-methyl-D-aspartate(NMDA) receptor has been well known as an important mediator of several forms of neural and behavioral plasticity. But different results were reported about the effect of MK-801 or dextromethorphan on opioid dependence. The present studies examined whether NMDA receptor antagonists can alter the opioid dependence and tolerance in rodents. Naloxone precipitated withdrawal symptoms and changes of locomotor activities were observed in MK-801 or dextromethorphan pretreated morphine-dependent rats. Tail-flick assay was used for morphine analgesia and tolerance was found after 4 day's consecutive injections (10 mg/kg, s.c., twice/day) of morphine in mice. Locomotor activity was increased and the withdrawal symptoms were decreased by the pretreatment of MK-801 in morphine-dependent rats. But 0.3 mg/kg i.p. of MK-801 intensified the body weight loss and produced severe ataxia and rotation although some withdrawal signs were attenuated. Morphine induced analgesic tolerance was inhibited by the pretreatment of MK-801 and dextromethorphan. Dextromethorphan was more potent than MK-801 in inhibiting the development of the analgesic tolerance in mice. These results suggest that NMDA system may be involved in opioid withdrawal and analgesic tolerance but appropriate caution should be requested when MK-801 is used in combination with opioid because of untoward neurologic signs.

• Journal of Oriental Neuropsychiatry
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• v.5 no.1
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• pp.69-79
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• 1994

In order to prove the effectiveness for anticonvulsion and analgesic of Ukgansan, Ukgansan added Jinphi Banha and Ukgansan added Chunma by experiment, experimental animals(mouse) are injected with strychnine, picrotoxin and caffeine to cause convulsion and ovserved the consumed time from convulsion to death. Comparing data with control group and observation data for frequency of writhing syndrome caused by acetic acid and phenylquinone show the results as follows : 1. Anticonvulsion effect on the convulsion induced by strychnine it was significantly effective in all sample groups. 2. Anticonvulsion effect on the convulsion induced by picrotoxin it was significantly effective in sample A and B. 3. Anticonvulsion effect on the convulsion induced by caffeine it was not recognized in all sample groups. 4. Analgesic effect on the pain induced by acetic acid it was significantly effect in sample A and C. 5. Analgesic effect on the pain induced by phenylquinone it was significantly effective in sample A and C. The results show that Ukgansan can be an effectual cure on anticonvulsion and analgrsic, Ukgansan added Jinphi·Banha on anticonvulsion, and Ukgansan added Chunma on analgesic.

• Advances in Traditional Medicine
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• v.6 no.4
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• pp.319-323
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• 2006

The crude ethanolic extract of the leaves of Clerodendrum viscosum (Family: Verbenaceae) was evaluated for its antioxidant and analgesic activities to investigate the scientific basis of the traditional uses. The antioxidant property of the extract was assessed by 1, 1-diphenyl -2- picryl hydrazyl (DPPH) free radical scavenging assay. The extract showed prominent antioxidant activity ($IC_{50}about{\sim}16{\mu}g/ml$) which was comparable to standard drug ascorbic acid ($IC_{50}about{\sim}15{\mu}g/ml$).The extract produced significant (P<0.001) writhing inhibition in acetic acid induced writhing in mice at the dose of 125 mg, 250 mg and 500 mg/kg body weight respectively, which were comparable to the standard drug diclofenac sodium. The results tend to suggest that the crude leaves extract at the above doses have antioxidant and analgesic activities and indicate that it might possess biologically active constituents having free radical scavenging and analgesic activities respectably.

• Advances in Traditional Medicine
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• v.9 no.4
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• pp.315-319
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• 2009

In present study evaluate the analgesic and anti-inflammatory activity of the compound obtained from the petroleum ether (40 - 60$^{\circ}C$) extract of the fruits from Dregea volubilis in Swiss albino mice and in Wister albino rats respectively. Dried and crushed fruits of Dregea volubilis were extracted by petroleum ether (40 - 60$^{\circ}C$), the proper solvent system was developed by TLC and subjected to column chromatography for obtaining the pure compound/s. IR, MASS, NMR (PMR, C13 NMR and DEPT) spectroscopic analysis were done to elucidate the structure of the compound/s. The petroleum ether (40 - 60$^{\circ}C$) extract of the fruits of Dregea volubilis led to isolation of a pentacyclic triterpenoid designated as taraxerone and characterized as D- friedoolean- 14- en, 3 one. Taraxerone had been screened for analgesic activity in Swiss albino mice and anti-inflammatory activity in Wister albino rats at the dose of 5 mg/kg body weight orally and exhibit significant analgesic and anti-inflammatory properties.

• Herbal Formula Science
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• v.11 no.1
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• pp.161-170
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• 2003

This study was designed to elucidate the analgesic effects of Jakyakgamchotang and Radix paeinia, Radix Glycyrrhiziae which are the component of Jakyakgamchotang in mice. The analgesic effects were measured by the Whittle's method and hot plate method. The results were as follows ; After the administration of Jakyakgamchotang extrace, the frequency of writhing syndrome was significantly inhibited. After the administration of Radix paeinia extract, the frequency of writhing syndrome was significantly inhibited. After the administration of Radix Glycyrrhiziae extract, the frequency of writhing syndrome was significantly inhibited. After the administration of Jakyakgamchotang extrace, paw licking time and escape time were significantly prolonged. After the administration of Radix paeinia extract, paw licking time was significantly prolonged. After the administration of Radix Glycyrrhiziae extract, paw licking time was significantly prolonged. It is concluded that the analgesic effects of Jakyakgamchotang were found to be more effective than Radix paeinia and Radix Glycyrrhiziae.

• Korean Journal of Pharmacognosy
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• v.32 no.3 s.126
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• pp.242-247
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• 2001

The anti-inflammatory activity of water extract of Mahaengeuigam-Tang(MHEGTWE) was examined using the carrageenin and acetic acid induced edema, croton oil induced granuloma pouch, and adjuvant arthritis in rats. In addition, the acute toxicity, analgesic and antipyretic effects of MHEGTWE were investigated by the general experimental methods. In acute toxicity test in mice, MHEGTWE showed 10% mortality at 2400 mg/kg(p.o), but it did not showed at 1200 mg/kg(i.p). It was also showed significant analgesic action on the writhing syndrome induced by 0.7% acetic acid at 600 mg/kg(p.o) and its antipyretic activity was observed in the typhoid vaccine induced fevered rats at 300 mg/kg(p.o). By the oral administration of the MHEGTWE, the significant anti-inflammatory activity was observed on 1% carrageenin induced edema, and it significantly inhibited the granuloma and exudate formation in rats. In the adjuvant arthritis experiment, the MHEGTWE decreased the hind paw edema in rats for 19 days. The results suggest that MHEGTWE has analgesic, anti-inflammatory and antipyretic action.

• YAKHAK HOEJI
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• v.36 no.5
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• pp.474-480
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• 1992

Astilbes rhizoma has been used for headache, arthralgia, chronic bronchitis and stomachalgia in traditional chinese medicine. The analgesic activities and their components of Astilbe chinensis var. davidii Rhizomes were evaluated. The ether and ethylacetate fractions of 70% EtOH extract showed considerable analgesic activities by acetic acid induced writhing method. Compound $1{\sim}5$ were isolated from ethylacetate fraction and identified as gallic acid, (+)-catechin, (+)-gallocatechin, bergenin and 11-O-galloylbergenin on the basis of spectroscopic methods. Among them (+)-gallocatechin showed stronger analgesic activity than that of other compounds.