• Archives of Pharmacal Research
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• v.17 no.5
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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.

• Korean Journal of Pharmacognosy
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• v.17 no.2
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• pp.107-112
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• 1986

The investigation aimed to study the effects of methanol fraction of licorice (FM 100) and glycyrrhizin on prostaglandin synthetase activity, in relation to their analgesic effects. Effects of FM 100 and glycyrrhizin on the activity of prostaglandin synthetase extracted from bull seminal vesicles were examined by the modified method of Takeguchi et al. The analgesic effect of FM 100 was tested in mice by the acetic acid writhing method. FM 100 was administered orally to mice. BSV prostaglandin synthetase activity was inhibited significantly by FM 100 in a dose-dependent manner, whereas the activity was slightly inhibited by glycyrrhizin. Statistically significant analgesic effects were also observed with FM 100. The results suggest that analgesic effect of licorice may be due to the inhibition of prostaglandin synthesis.

• Korean Journal of Pharmacognosy
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• v.17 no.3
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• pp.199-205
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• 1986

It has been known that Magnolia officinalis, Magnolia and Machilus Barks are reputed to be effective in 'Hagi', 'Sanman' and to be analgesic but there was differences of efficacy of these crude drugs against the kinds and habitates. For this reason, this study was conducted to compare the acute toxicities, analgesic effects and motilities of isolated intestine. This results obtained in this work were summarized as follow: 1. In the test of acute toxicies, Machilus bark was found to be more toxic than the others. 2. Both these was found to have analgesic effect. 3. In the effects against the motility of isolated intestine, Magnolia officinalis and Magnolia barks were found to be relaxant, Machilus bark was found to be contractive. From these results, Magnolia officinalis and Magnolia barks might have analgesic effect and relaxant effect of intestine.

• Korean Journal of Pharmacognosy
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• v.30 no.1
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• pp.18-24
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• 1999

This study was investigated on anti-inflammatory and analgesic activity on Gu-Mi-Gang-Hwal-Tang which has been used for the treatment of common cold and headache, arthralgia, fever in oriental medicine. The anti-inflammatory activities of Gu-Mi-Gang-Hwal-Tang water extract (GMGHT) on the carrageenin induced edema, acetic acid induced edema, and corton oil induced granuloma pouch in rats were examined. The analgesic effect of the GMGHT was investigated utilizing acetic acid induced writhing syndrome in mice. The antipyretic activity of the GMGHT was also investigated. The oral administration of GMGHT has been shown the anti-inflammatory activities in 1% carrageenin and acetic acid induced edema in rats. The GMGHT has been shown significant inhibitory effects on glanuloma and exudate formation in rats, especially the GMGHT (450 mg/kg) has the efficacy more than the GMGHT (150 mg/kg). The writhing syndromes induced by acetic acid in mice were inhibited, especially analgesic activity of the GMGHT (450 mg/kg) is similar to that of piroxicam and antipyretic activities were recognized in rats. In the present study, the GMGHT is indicated to have the anti-inflammatory, analgesic and antipyretic activities.

• Archives of Pharmacal Research
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• v.19 no.3
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• pp.246-247
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• 1996

In the previous reports (Park et al., 1991, and 1993), we described the synthesis and analgesic effects of various homovanillic amides as analogs of capsaicin. In the study, we tried to enhance the analgesic actvity of capsaicin by structural modification. Our study has been performed in three directions. First, the amide bond of capsaicin was transposed. Second, a phenyl ring was introduced to replace a double bond of capsaicin. Finally, aminoethylation was performed on 4-hydroxy group of capsaicin to improve oral bioavailability. These studies have led to N-(3-phenylpropyl)homovanillic amide 2 which has high analgesic activity. Our continuing efforts in this area have focused on the introduction of various substituents on the phenyl ring of 2 as well as their pharmacological studies. We report herein the synthesis of homovanillic amide derivatives and their analgesic activity.

• Journal of Acupuncture Research
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• v.33 no.2
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• pp.97-108
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• 2016

Objectives : This study was performed to investigate the analgesic effect of Styrax japonica pharmacopuncture on formalin induced pain in rats and to figure out efficient extraction method. Methods : The subjects were divided into 5 groups ; normal group(treated with normal saline at KI03, and injected normal saline at right hindpaw after 35 minutes), control group(treated with normal saline at KI03, and injected with formalin at right hindpaw after 35 minutes), water group(treated by hot water extraction pharmacopuncture at KI03, and injected with formalin at right hindpaw after 35 minutes), ethanol group(treated with ethanol extraction pharmacopuncture at KI03, and injected with formalin at right hindpaw after 35 minutes), and ultrasound group(treated with ultrasound extraction pharmacacupuncture and injected with fromalin formalin at right hindpaw after 35 minutes). We conducted a formalin test with ultrasonic vocalization( USV), and after the test checked for substance P, Aspartate aminotransferase(AST), and Alanine aminotransferase(ALT) concentration in the blood for each of the groups. Results : There was a significant analgesic effect of Styrax japonica pharmacopuncture in the early phase of the formalin test, and pharmacopuncture made with an ultrasound extracting method was observed to have a better analgesic effect than other extracting methods in early phases. The substance P concentration decreased significantly in the Styrax japonica pharmacopuncture treated group and no difference was found in the AST and ALT concentration of each group. Conclusion : These results demonstrated that Styrax japonica pharmacopuncture had analgesic effects in noxious nociceptors stimulation. Also pharmacopuncture made with an ultrasound extracting method had a better analgesic effect than others.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.87-93
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• 1997

DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

• Journal of Acupuncture Research
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• v.20 no.3
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• pp.117-130
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• 2003

To study the analgesic and effect and its mechanism of eletroacupunture(EA) on the chronic inflammatory pain 50 rats were induced with arthralgesia by injecting complete freund's adjuvant(CFA). Two weeks after the injection of CFA, EA stimulation(2Hz, 0.07mA, 0.3ms) was delivered to Jogsamni($ST_{36}$) for 20 minutes. Analgesic effect was evaluated by using the tail flick latency(TFL) and the analgesic mechanism was observed by applying TFL with the pretreatment with naloxone and yohimbine. The results were as follows ; 1. TFL level for the model of adjuvant-induced arthritis decreased as time went by and it induced the hyperalgesia. 2. EA stimulation delivered to Jogsamni($ST_{36}$) for 20 minutes in the rat model of adjuvant-induced arthritis brought analgesic effect and its effect had lasted for 40 minutes after the stimulation. 3. The analgesic effect of Jogsamni($ST_{36}$) EA in the rat model of adjuvant-induced arthritis was blocked by pretreatment with naloxone(2mg/kg,i.p). This result suggests that the EA effect on the chronic inflammatory pain can be related to the endogenous opioid mechanism. 4. The analgesic effect of Jogsamni($ST_{36}$) EA in the rat model of adjuvant-induced arthritis was blocked by pretreatment with naloxone(2mg/kg,i.p). This result suggests that the EA effect on the chronic inflammatory pain can be related to the ${\alpha}_2$-adrenergic mechanism.

• Journal of Acupuncture Research
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• v.21 no.6
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• pp.51-62
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• 2004

Objective: To investigate the analgesic effect and its serotonergic mechanism, especially related with 5-HTI and 5-HT2 receptor, of electroacupuncture(EA) in the rat model of collagen-induced arthritis(CIA). Methods : Immunization of male Sprague-Dawley rats with bovine type II (C II) collagen emulsified in Freund's incomplete adjuvant, followed by a booster injection 14 days later, leads to development of arthritis in more than 70% of rats by 21 days postinjection. After three weeks of first immunization, EA stimulation(2 Hz, 0.07 mA, 0.3 ms) was delivered into Jogsamni($ST_{36}$) for 30 minutes. Analgesic effect was evaluated by tail flick latency(TFL). We compared the analgesic effect of EA with TFLs between pretreatment of normal saline and pretreatment of spiroxatrine (5-HT1 receptor antagonist, 1mg/kg, intraperitoneal) and spiperone (5-HT2 receptor antagonist, 1 mg/kg, intraperitoneal) in CIA. Results : 1. TFLs were gradually decreased in CIA as increasing severity of arthritis. 2. Jogsamni($ST_{36}$) EA stimulation in CIA increased TFLs and the effect lasted for 60 minutes. 3. Increased TFLs with Jogsamni($ST_{36}$) EA stimulation were inhibited by pretreatment of spiroxatrine and spiperone in CIA. Conclusions : Jogsamni($ST_{36}$) EA showed analgesic effects in CIA The analgesic effects of Jogsamni($ST_{36}$) EA were inhibited by spiroxatrine and spiperone pretreatment. These observations suggest that 5-HT1 and 5-HT2 serotonergic receptor, which involve the release of serotonin neurotransmitter, play an important roles in analgesic mechanism of EA stimulation.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.34 no.6
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• pp.449-454
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• 2012

Purpose: Intravenous sedation with midazolam is common in contemporary dentistry. That is effective for anxious patients, but additional analgesic agent needs to be used, because midazolam alone doesn't have an analgesic effect. This study was performed to select an analgesic agent between an opioid agent, and nonsteroidal anti-inflammatory drugs as adjunctives in intravenous sedation with midazolam. Methods: The subjects were 60 patients who visited the Department of Oral and Maxillofacial Surgery, Sacred Heart Hospital, Hallym University, between August 2009 and February 2010. Conscious sedation was performed on 20 patients of 3 groups (control group, ketorolac group, and fentanyl group), who were divided randomly. The analgesic agent was administrated preoperatively. For sedation, vital signs were recorded. After sedation and operation, subjective questionnaires of the patient and operator were implemented. Results: All of the $SPO_2$, blood pressure, and heart rates stayed within the normal range for sedation. The sedation depth and analgesic effect of the ketorolac group and fentanyl group were similar. In the case of sedation depth, 12 patients in the ketorolac group and 14 patients in the fentanyl group had no memory of surgery. In the case of analgesic effect, the visual analogue scale of pain scored 2~3 in 13 patients in the ketorolac group, and 0~2 in 12 patients in the fentanyl group. The satisfaction of patients and doctors was also similar. Conclusion: Considering the management and complication of an opioid agent, non-steroidal anti-inflammatory drugs is more effective than an opioid agent.