• 생약학회지
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• 제44권2호
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• pp.188-192
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• 2013

Acer tegmentosum which is belongs to Aceraceae has been widely used as a traditional medicine for the treatment of lots of diseases including pain management. In this study, we evaluated the anti-nocicepitve effects of methanolic extract of A. tegmentosum (MAT) in mice using various pain models. MAT presented strong and dose-dependent anti-nociceptive activities on thermal nociception models such as tail-immersion test and hot plate test. Moreover, acetic acid-induced chemical nociception was signigicantly reduced by MAT treatment. We could confirm MAT's central and peripheral analgesic properties by formalin test. We also found that the pre-treatment of opioid receptor antagonist did not alter the MAT's anti-nociception, suggesting opioid receptor is not involved in analgesic activity of MAT. Based on our results, we could conclude that MAT may be possibly used as an anti-nociceptive agent for the treatment of various nociceptive pains.

• Advances in Traditional Medicine
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• 제9권4호
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• pp.326-334
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• 2009

The effect of alcoholic extract of Anthocephalus (A.) Cadamba Roxb. was evaluated in experimental models of pain and ulcer. Hot tail flick test, hot plate test and acetic acid induced writhing test were employed for evaluating the peripheral as well as central analgesic mechanism exerted by the extracts. Gastroprotective activity was examined by HCl and ethanol induced gastric damage test. Test group received crude extract 500 mg/kg showed maximum time needed for the response against thermal stimuli (6.26 ${\pm}$ 0.439 s) which is comparable to diclofenac sodium (6.56 ${\pm}$ 0.381 s) in hot tail flick method. These experimental results also followed the experimental results of hot plate test where crude extract 500 mg/kg showed maximum time needed for the response against thermal stimuli (4.74 ${\pm}$ 0.234 s) which is comparable to diclofenac sodium (5.58 ${\pm}$ 0.585 s). The crude extract at 500 and 250 mg/kg showed significant reduction in acetic acid induced writhing in mice with a maximum effect of 68.026% reduction at 500 mg/kg dose which is comparable to standard diclofenac sodium (79.93%). In gastroprotective study the extract of A. Cadamba (250 and 500 mg/kg) significantly inhibited ulceration induced by both HCl and ethanol dose dependently. Results of the study suggest that the extract possesses both analgesic and gastroprotective activity on mice.

• The Korean Journal of Physiology and Pharmacology
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• 제22권2호
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• pp.173-182
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• 2018

Recent studies have provided several lines of evidence that peripheral administration of oxytocin induces analgesia in human and rodents. However, the exact underlying mechanism of analgesia still remains elusive. In the present study, we aimed to identify which receptor could mediate the analgesic effect of intraperitoneal injection of oxytocin and its cellular mechanisms in thermal pain behavior. We found that oxytocin-induced analgesia could be reversed by $d(CH_2)_5[Tyr(Me)^2,Dab^5]$ AVP, a vasopressin-1a (V1a) receptor antagonist, but not by $desGly-NH_2-d(CH_2)_5[D-Tyr^2,Thr^4]OVT$, an oxytocin receptor antagonist. Single cell RT-PCR analysis revealed that V1a receptor, compared to oxytocin, vasopressin-1b and vasopressin-2 receptors, was more profoundly expressed in dorsal root ganglion (DRG) neurons and the expression of V1a receptor was predominant in transient receptor potential vanilloid 1 (TRPV1)-expressing DRG neurons. Fura-2 based calcium imaging experiments showed that capsaicin-induced calcium transient was significantly inhibited by oxytocin and that such inhibition was reversed by V1a receptor antagonist. Additionally, whole cell patch clamp recording demonstrated that oxytocin significantly increased potassium conductance via V1a receptor in DRG neurons. Taken together, our findings suggest that analgesic effects produced by peripheral administration of oxytocin were attributable to the activation of V1a receptor, resulting in reduction of TRPV1 activity and enhancement of potassium conductance in DRG neurons.

• Journal of Chest Surgery
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• 제29권5호
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• pp.477-486
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• 1996

통각정보나 과탄산증이 내재진통계를 활성화 시켜서 진통효과를 가져온다는 것은 잘 알려져 있다. 이 러한 일련의 과정에서 중추신경세포의-역활에 대한 체계적인 연구가 요구되는 바, 16마리의 성숙한 고 양이를 u-chloralose로 마취한 후 연수 및 좌골신경을 노출시켜, 상부연수의 복외측부(rostral ventrolateral medulla, 이후 RVLM으로 칭함)세포활동이 탄산가스분압의 변동에 어떠한 영향을 받는 지를 관찰하였다. RVLM에서 세포의 기록법으로 그 변화를 관찰한 바, 총 53개의 세포에서 자발적 인 활동을 보였고, 이 중 28개는 심맥관계 세포, 16개는 호흡관련 세포, 2개는 심맥관계-호흡 동시 관련 세포이었으며, 7개는 자발적 활동은 보이나 심 장주기나 호흡주기와 무관 하였다. 28개의 심맥관계 세포중 11개에서는 동맥혈내 탄산가스분압이 상승하였을때 세포 활동이 증가하고, 13개 세포에서는 반대로 감소하였으며, 나머지 4개 에서는 특별한 변화가 없었다. 16개의 호흡관련 세포중 9개에서는 동맥혈내 탄산가스분압이 상승하였을때 활동이 증가하고, 6개에 서는 감소하였으며 1개는 특별한 변화가 없었다 B개의 심맥관계-호흡관련 세포에서는 탄산\ulcorner스 분압의 상승에 큰 영향을 받지 않았다. 심 장 혹은 호흡주기와 무관하였던 7개의 세포중 4개는 동맥 혈 탄산가스 분압이 상승하였을때 세포 활 동이 감소하였고, 2개는 상승하였으며 1개는 큰 영향을 받지 않았다 말초신경 자극과 동시에 탄산가스분압을상승시켰을 때 심먹관계 세포의 A반응은큰 영향이 없었으 나 C반응은 상승하였다. 결론적으로 RVLM에는 동맥혈 탄산가스 분압이 상승하였을 때 활동이 증가하는 세포들이 존재하고, 이때 말초화학 감수기의 영 향보다는 탄산가스가 중추에 직접 작용할 가능성이 크며 과탄산증에 의한 내 재진통작용도 RVLM을 통하지는 않는다고 생각된다.

• 한국식품위생안전성학회지
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• 제9권3호
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• pp.163-168
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• 1994

In the present study we investigated the peripheral function of capsaicin and KR-25018, a newly synthesized capsaicin derivative, which was demonstrated to have a potent analgesic activity through different mechanism from morphine and nonsteroidal antiinflammatory drugs. Capsaicin (10-8~10-5 M) and KR-25018 (10-8~10-5 M) produced concentration-dependent contractions of the isolated guinea pig bronchi. There were no significant differences in the maximum response and the EC50 values (EC50: 0.137$\pm$0.025 $\mu$M and 0.097$\pm$0.031 $\mu$M for capsaicin and KR-25018, respectively, P>0.05). Phosphoramidon (10 $\mu$M) and indomethacin (10 $\mu$M) had no significant effect on contractile response to the submaximal concentration range of capsaicin and KR-25018 (3$\times$10-9~3$\times$10-7 M). The response to KR-25018, like that to capsaicin, was significantly inhibited by ruthenium red with reduction in the maximum response, which is indicative of non-competitive antagonism. A further common feature of the responses to capsaicin and KR-25018 in the guinea pig bronchi was their sensitivity to capsazepine. Capsazepine caused a rightward parallel shift in concentration-response curves obtained by capsaicin and KR-25018. the pA2 values of capsazepine were 5.90 and 5.99 against capsaicin and KR-25018 response, respectively. In conclusion, KR-25018 and capsaicin exert their contractile effects in the isolated guinea pig bronchial muscle by common mechanisms, probably via the activation of a specific receptor.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.252-252
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• 1996

We Investigated the peripheral excitatory effect of capsaicin and KR-25018, a newly synthesized capsaicin derivative which was demonstrated to have a potent analgesic activity. KR-25018 and capsaicin were found to be both potent efficacious contractors of isolated guinea pig bronchial smooth muscle. KR-25018 was equipotent with capsaicin and [Sar$\^$9/,Met(O$_2$)$\^$11/]-substance P, 10-fold more potent than histamine and 10-fold less potent than (${\beta}$ -Ala$\^$8/)-neurokinin A(4-10), and their -log(M)EC$\_$50/ values were 6.94${\pm}$0.08, 6.86${\pm}$0.05, 6.96${\pm}$0.07, 5.64${\pm}$0.04, 7.96${\pm}$0.02, respectively. Contractile responses to KR-25018 and capsaicin were potentiated by phosphoramidon (1 ${\mu}$M), an inhibitor of neuropeptide-inactivating endopeptidase, but completely abolished in a calcium-free medium. These responses to KR-25018 and capsaicin were unaffected by the NK-1 antagonist CP96345 (1${\mu}$M), partially inhibited by the NK-2 antagonist SR48968 (1 ${\mu}$M) but almost completely abolished by a combination of the antagonists. A vanilloid receptor antagonist capsazepine competitively antagonized the responses to both KR-25018 and capsaicin (pA$_2$: aganst KR-25018, 5.98${\pm}$0.47; against capsaicin, 5.80${\pm}$0.31), and a capsaicin-sensitive cation channel antagonist ruthenium red caused significant reduction in the maximum responses to KR-25018 and capsaicin (pD'$_2$: against KR-25018, 4.61${\pm}$0.33; against capsaicin 4.96${\pm}$0.21). In conclusion, the present results suggest that KR-25018 and cpasaicin act on the same vanilloid receptor inducing the influx of calcium through ruthenium red-sensitive cation channel and produce contractile responses via the release of tachykinins that act on both NK-1 and NK-2 receptor subtypes.