• 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.

• Biomolecules & Therapeutics
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• 제18권3호
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• pp.246-256
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• 2010

Atopic dermatitis is a common skin disease affecting up to 10% of children and approximately 2% of adults. Atopic dermatitis exhibits four major symptoms, including intense itching, dry skin, redness and exudation. The "itch-scratch-itch" cycle is one of the major features in atopic dermatitis. The pathophysiology and neurobiology of pruritus is unclear. Currently there are no single and universally effective pharmacological antipruritic drugs for treatment of atopic dermatitis. Thus, controlling of itch is a very important unmet need in patients suffering from atopic dermatitis. This article will update progress during the past 10 years of research in the field of pruritus of atopic dermatitis, focusing on aspects of pruritogens (including inflammatory lipids, histamine, serotonin, proteinases, proteinase-activating receptors, neurotransmitters, neuropeptides, and opioid peptides), antipruritic therapies, and emerging new targets. Based on recent progress, researchers expect to identify exciting possibilities for improved treatments and to develop new antipruritic drugs acting through novel targets, such as histamine H4 receptor, gastrin-releasing peptide receptor, MrgprA3, thromboxane A2 receptor and the putative SPC receptor.

• The Korean Journal of Pain
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• 제11권2호
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• pp.294-298
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• 1998

The feature of neuropathic pain may occur in the absence of any apparent stimulus and be exaggerated in either amplitude or duration. Peripheral nerve injury may produce neuropathic pain and opioids have been shown to be relatively unsatisfactory for the treatment of most cases of neuropathic pain. The NMDA receptor system is involved in transmission and modulation of nociceptive information. We treated patients with severe pain, hyperaesthesia and allodynia with epidural injection of NMDA receptor antagonist, ketamine (10 mg) and morphine (0.5 mg) or other opioid. The combinations provided effective pain management in 23 patients with neuropathic pain.

• 통합자연과학논문집
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• 제9권3호
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• pp.185-189
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• 2016

Urotensin-2 receptor (UTS2R) is the most potent vasoconstrictor and plays a major role in the pathophysiology of various cardiovascular diseases and becomes a potential target for human pharmacotherapy. The crystal structure of Urotension-2 receptor has not yet been resolved. Hence, in the current study homology modelling of UTS2R was done utilizing the crystal structure of human delta opioid receptor as the template. Since the template has low sequence identity, we have incorporated both comparative modelling and threading approach to generate the three dimensional structure. 10 models were generated and validated. The reported models can be used to characterize the critical amino acid residues in the binding site of UTS2R.

• 생약학회지
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• 제50권4호
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• pp.272-276
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• 2019

Corylopsis gotoana has been widely used as a traditional medicine for the treatment of lots of disease including cold, edema and vomiting. However pharmacological and phytochemical studies on the C. gotoana are extremely limited. Here in this study, the author investigated the anti-nociceptive effects of the methanolic extract of Corylopsis gotoana (MCG) using various pain models. In the present study, MCG exhibited strong and dose-dependent anti-nociceptive activities on various experimental pain models including thermal nociception and chemical nociception, compared to positive control such as tramadol and indomethacin. In addition, the result from combination test using naloxone, analgesic activity of MCG was slightly reduced, indicating that MCG acts as a partial opioid receptor agonist. These results demonstrated that MCG has potent analgesic potential and thus it may be possibly used as a valuable anti-nociceptive agent.

• 대한약리학회지
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• 제25권1호
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• pp.23-30
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• 1989

함께 투여되는 마약성진통제에 따라 효능제 또는 길항제(mixed agonist-antagonist)로 작용하는 buprenorphine을 사용하여 개구리 좌골신경에 존재하는 아편수용체의 성질을 검토하였다. 실험은 sucrose-gap apparatus를 사용하여 활동전압에 대한 영향을 관찰하였으며 약물의 상호작용을 검토하고자 meperidine 또는 naloxone을 사용하여 다음과 같은 결과를 얻었다. 1) Buprenorphine은 현저하게 개구리 좌골신경의 활동전압을 저하시켰다. 2) 두 개의 최고작용농도를 보였는데 저농도에서는 $10^{-8}\;M$, 또 고농도에서는 $10^{-4}\;M$에서 현저하게 작용을 나타내었다. 3) Buprenorphine은 meperidine의 활동전압 저하작용을 의의있게 억제하였다. 4) Naloxone에 의하여 Buprenorphine의 저하 작용이 억제되었다. 위의 실험결과로 Buprenorphine은 순수 마약성진통제의 작용을 억제하여 차단제로 작용하는 한편 또한 효능제로 활동전압을 의의있게 억제하였다. 이로써 개구리 좌골신경에 있는 아편수용체는 세포막에 또는 세포막 주위에서 $Na^+-Channel$이 활성화되는 데 중요한 역할을 하는 것으로 간주되며 이 수용체는 또한 Naloxone에 매우 민감한 반응을 나타낸다.

• The Korean Journal of Physiology and Pharmacology
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• 제22권4호
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• pp.419-425
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• 2018

The superficial dorsal horn of the spinal cord plays an important role in pain transmission and opioid activity. Several studies have demonstrated that opioids modulate pain transmission, and the activation of ${\mu}$-opioid receptors (MORs) by opioids contributes to analgesic effects in the spinal cord. However, the effect of the activation of MORs on GABAergic interneurons and the contribution to the analgesic effect are much less clear. In this study, using transgenic mice, which allow the identification of GABAergic interneurons, we investigated how the activation of MORs affects the excitability of GABAergic interneurons and synaptic transmission between primary nociceptive afferent and GABAergic interneurons. We found that a selective ${\mu}$-opioid agonist, [$D-Ala^2$, $NMe-Phe^4$, Gly-ol]-enkephanlin (DAMGO), induced an outward current mediated by $K^+$ channels in GABAergic interneurons. In addition, DAMGO reduced the amplitude of evoked excitatory postsynaptic currents (EPSCs) of GABAergic interneurons which receive monosynaptic inputs from primary nociceptive C fibers. Taken together, we found that DAMGO reduced the excitability of GABAergic interneurons and synaptic transmission between primary nociceptive C fibers and GABAergic interneurons. These results suggest one possibility that suppression of GABAergic interneurons by DMAGO may reduce the inhibition on secondary GABAergic interneurons, which increase the inhibition of the secondary GABAergic interneurons to excitatory neurons in the spinal dorsal horn. In this circumstance, the sum of excitation of the entire spinal network will control the pain transmission.

• 한국산학기술학회논문지
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• 제16권8호
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• pp.5336-5342
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• 2015

삶의 질이 향상됨에 따라 환자의 흉터 치료 수요는 증가하고 있는 반면, 흉터 개선 제품은 대부분 수입 제품에 의존하고 있는 실정이다. 엔케팔린은 신경말단에서 분비하는 신경 펩타이드의 한 종류이다. 피부세포와 신경세포는 배엽 발달 과정 중 공통적으로 외배엽에서 유래하며, 피부세포 막에서 신경세포에서 발현되는 신경펩타이드 수용체 즉, 오피오이드 수용체(Opioid Receptor)가 발현된다. 오피오이드 수용체는 뮤-(${\mu}$), 델타-(${\delta}$), 카파-(${\kappa}$) 세 종류가 있으며, 각각을 MOR, DOR, KOR라고 부르고, 델타-오피오이드 수용체는 피부에서의 상처 치유(Wound-healing)에 직접 관여하는 것으로 보인다. 본 논문에서는 엔케팔린의 Alanine Scan 방법을 이용하여 엔케팔린 유도체를 합성하여, 피부세포내 안전성과 Cell migration assay를 통한 In vitro 상처 치유 촉진 효능, 프로 콜라겐 합성능력 및 보습효과를 실험을 통해 검증하였고, 피부 상처 마우스 모델에서 엔케팔린 유도체의 상처 치료 효과를 확인하였다. 그 결과 엔케팔린 유도체 AGGFL(AS10) 및 YGGAL(AS13)이 상처 치유 효능, 프로 콜라겐 합성증가, 보습 관련 유전자 발현 증가를 확인하였고, 특히 AS13이 피부 상처 마우스 모델에서 뛰어난 상처치료 효과를 확인하였다.

• The Korean Journal of Pain
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• 제20권2호
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• pp.100-105
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• 2007

Background: Ginseng has been used to manage various types of pain in folk medicine. This study characterized the effect of treatment with intrathecal ginsenosides, the active components of ginseng in a postoperative pain model. Methods: Male Sprague-Dawley rats were implanted with lumbar intrathecal catheters. An incision was made in the plantar surface of the hindpaw. Withdrawal thresholds following the application of a von Frey filament to the wound site were measured. To determine the role of the opioid or GABA receptors following treatment with the ginsenosides, naloxone, bicuculline (a $GABA_A$ receptor antagonist), and saclofen (a $GABA_B$ receptor antagonist) were administered intrathecally 10 min before the delivery of the ginsenosides and the changes of the withdrawal thresholds after application of the von Frey filament were Observed. Results: Treatment with the intrathecal ginsenosides increased the withdrawal threshold in a dose dependent manner. Pre-treatment with intrathecal naloxone reversed the antinociceptive effect of the ginsenosides. However, pre-treatment with intrathecal bicuculline and saclofen failed to have an effect on the activity of the ginsenosides. Conclusions: These results suggest that ginsenosides are effective to alleviate the postoperative pain evoked by paw incision. The opioid receptor, but not GABA receptors, may be involved in the antinociceptive action of the ginsenosides at the spinal level.

• Journal of Ginseng Research
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• 제26권4호
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• pp.187-190
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• 2002

Crude synaptic membrane fractions from the frontal cortex, striatum, brain stem and whole brain of rat were prepared to assay the effects of ginseng total saponin (GTS) on [$^3$H]DAGO bindings of the opioid $\mu$-receptors. Scatchard plots analysis binding data demonstrated that GTS (0.1 mg/ml) decreased the affinity of specific [$^3$H]DAGO bindings without changes in B$\_$max/ in the frontal cortex and striatum. On the other hand, GTS did not affect the [$^3$H]DAGO bindings iii the brain stem and whole brain. These results suggest that the regulation of [$^3$H]DAGO bindings by GTS may play roles in the change of the pharmacological responses of $\mu$-opioids.