• 제목/요약/키워드: Receptors, opioid

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Progress of Pruritus Research in Atopic Dermatitis

  • Lee, Chang-Hoon
    • 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.

악관절증의 침치료에 대한 고찰 (근육장애을 중심으로) (Acupuncture Treatment for T.M.D.)

  • 김용석;김창환
    • 대한한의학회지
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    • 제16권1호통권29호
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    • pp.36-50
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    • 1995
  • Acupuncture is so effective and simple to use in the pain and dysfunction syndrome of TMD. Acupuncture treatment is a point-specific. So, the selection of acupuncture point is very important. According to the traditional meridian theory, we select the points; local points around TMJ and mastication muscles(ST6, ST7, GB20, GB21) and remote point(LI4). And if there is another pain, one or two other points are added. Both neural and humoral mechanism play an important role in acupuncture analgesia. The discovery of spinal gate mechanisms shows somatic stimulation can induce pain inhibition. Humoral mechanism has been established from the discovery of opioid receptors and endogenous opioids. Acupuncture induces a relaxation in the patient, which further decreases the muscle tension.

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작열통환자에서 Morphine을 이용한 성상신경절 차단 효과 -증례 보고- (Effect of Stellate Ganglion Block with Morphine on Causalgia -A case report-)

  • 김은미;윤성근;박명혜;곽호성
    • The Korean Journal of Pain
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    • 제11권1호
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    • pp.109-112
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    • 1998
  • The sympathetic nervous system has been implicated as an important factor contributing to causalgia. Basis on reports of presence of opioid receptors in sympathetic autonomic ganglia, including human stellate ganglion, we administered morphine in stellate ganglion block for a patient with causalgia. The patient suffering from brachial plexus injury treated with stellate ganglion block in conjunction with physical therapy. Stellate ganglion block was performed in a paratracheal approach by injection of 1% lidocaine, or 0.25% bupivacaine 8 ml, with morpine 1 mg. Patient's symptoms were dramatically improved after 13 stellate ganglion blocks.

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전침(電鍼)의 collagen 유발(誘發) 관절염(關節炎)에 대한 진통(鎭痛) 효과(效果) 및 그 기전(機轉)에 관한 연구(硏究) - opioidergic mechanism을 중심으로 - (The Analgesic Effect and Its Opioidergic Mechanism of Electroacupuncture on Inflammatory Pain in the Type II Collagen-induced Arthritis Rats)

  • 김은정;백용현;강성길
    • 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.

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침의 염증 제어 기전에 관한 최근 견해;최신 연구를 바탕으로 (Current concept for anti-inflammatory mechanism of acupuncture;based on the latest studies)

  • 조종현;안성훈;손인철
    • Korean Journal of Acupuncture
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    • 제25권2호
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    • pp.43-55
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    • 2008
  • Objectives : The acupuncture has been in the classic arsenal of Oriental medicine over inflammatory diseases. Its physiological mechanism is not fully understood but being known better everyday. We reviewed several papers to describe current concepts over anti-inflammatory mechanism of acupuncture. Methods : Some computerized literature searches were done using the key words of 'acupuncture' AND 'Anti-inflammatory' in Medline via Pubmed between March 2007 and December 2007. Only rationally-designed studies were picked among practically associated materials. A well-known hypothesis on acupunctural physiology was adapted for integration. Result : 18 studies were selected. 17 studies were laboratory experiment and 1 was a clinical study. Data was classified into some comprehensive categories. Author's opinion was added at the end of each category. Study results supported the hypotheses on acupunctural physiology; Acupuncture has some influences on autonomic nerve system(ANS). And it stimulates several receptors from target cells like macrophage, and finally inhbits cytokines like TNF-${\alpha}$, IL-1${\beta}$ andIL-10 which are inflammation-mediated. Acupuncture increases the opioid releasing therefore relieves inflammation. And acupuncture inhibits cyclooxgenase(COX) but its mechanism is controversial until now. Conclusion : Current concepts over anti-inflammatory mechanism of acupuncture are as follows. Acupucture suppresses inflammation by stimulation of ANS, increasing of opioid releasing and inhibition of COX. But more studies are needed to fully describe the anti-inflammatory effect of acupuncture.

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골반경 수술시 골반내 도포한 Morphine, Morphine-Bupivacaine의 술 후 진통 효과 (Intra-pelvic Morphine, Morphine-Bupivacaine Instillation for Pain Relief after Endoscopic Pelvic Surgery)

  • 이은주;박정출;이소영;김지희;박희권;김홍순;장영진;이경천;조영례;김용욱
    • The Korean Journal of Pain
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    • 제13권1호
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    • pp.49-54
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    • 2000
  • Background: Evidence has accumulated that opioids can produce potent antinociceptive effects by interacting with opioid receptors in peripheral tissues. Bupivacaine has a potent analgesic effect with early peak onset in the postoperative period. The combination of intrapelvic bupivacaine and morphine has been suggested as an ideal analgesic after endoscopic pelvic surgery. Methods: Sixty patients scheduled for endoscopic pelvic surgery under general anesthesia were allocated randomly to three groups. Group 1 received normal saline 20 ml, group 2 received morphine 5 mg in normal saline 20 ml, and group 3 received morphine 5 mg in 0.25% bupivacaine 20 ml into the pelvic cavity. Postoperative pain was assessed using the visual analogue scale at 1, 2, 4, 8, and 24 hours after the intrapelvic instillation. Supplemental analgesic requirements, vital signs, and side effects were recorded for 24 hours. Results: Intrapelvic morphine and bupivacaine produced significant analgesia after endoscopic pelvic surgery. The patients in group 3 had lower pain scores than those in the group 1 and 2 at 1, 2 and 4th hours. There were no significant differences in the pain scores at 8 hours and 24 hours postoperatively between group 2 and 3. Supplemental analgesic requirements were significantly greater in the groups 1 and 2 than the group 3 for 24 hours. No significant side effects occurred. Conclusion: The intrapelvic instillation of morphine and bupivacaine is effective for the postoperative pain control in patients undergoing endoscopic pelvic surgery.

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Tapentadol: Can It Kill Two Birds with One Stone without Breaking Windows?

  • Chang, Eun Jung;Choi, Eun Ji;Kim, Kyung Hoon
    • The Korean Journal of Pain
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    • 제29권3호
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    • pp.153-157
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    • 2016
  • Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the ${\mu}$-opioid receptor (MOR), and as a norepinephrine reuptake inhibitor (NRI) all in a single molecule. Immediate release (IR) tapentadol shows its analgesic effect quickly, at around 30 minutes. Its MOR agonistic action produces acute nociceptive pain relief; its role as an NRI brings about chronic neuropathic pain relief. Absorption is rapid, with a mean maximal serum concentration at 1.25-1.5 h after oral intake. It is present primarily in the form of conjugated metabolites after glucuronidation, and excretes rapidly and completely via the kidneys. The most common adverse reactions are nausea, dizziness, vomiting, and somnolence. Constipation is more common in use of the ER formulation. Precautions against concomitant use of central nervous system depressants, including sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, and alcohol, or use of tapentadol within 14 days of the cessation of monoamine oxidase inhibitors, are advised. The safety and efficacy have not been established for use during pregnancy, labor, and delivery, or for nursing mothers, pediatric patients less than 18 years of age, and cases of severe renal impairment and severe hepatic impairment. The major concerns for tapentadol are abuse, addiction, seeking behavior, withdrawal, and physical dependence. The presumed problem for use of tapentadol is to control the ratio of MOR agonist and NRI. In conclusion, tapentadol produces both nociceptive and neuropathic pain relief, but with worries about abuse and dependence.

The Effects of Pre-emptive Administration of Ketamine and norBNI on Pain Behavior, c-Fos, and Prodynorphin Protein Expression in the Rat Spinal Cord after Formalin-induced Pain Is Modulated by the DREAM Protein

  • Long, Idris;Suppian, Rapeah;Ismail, Zalina
    • The Korean Journal of Pain
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    • 제26권3호
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    • pp.255-264
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    • 2013
  • Background: We investigated the effects of pre-emptive administration of ketamine and norBNI on pain behavior and the expression of DREAM, c-Fos, and prodynorphin proteins on the ipsilateral side of the rat spinal cord at 2 and 4 hours after formalin injection. Methods: Eighty-four male Sprague Dawley rats were divided into 4 major groups consisting of control rats (C) (n = 12), rats given only formalin injections (F) (n = 24), and rats treated with pre-emptive administration of either ketamine (K+F) (n = 24) or norBNI (N+F) (n = 24). The non-control groups were further divided into subgroups consisting of rats that were sacrificed at 2 and 4 hours (n = 12 for each group) after formalin injection. Pain behavior was recorded for 1 hour. After 2 and 4 hours, the rats were sacrificed and the spinal cords (L4-L5 sections) were removed for immunohistochemistry and Western blot analysis. Results: The pain behavior response was reduced in the K+F group compared to the other groups during the second phase of the formalin pain response. We detected an increase in the nuclear DREAM protein level in the K+F group at 2 and 4 hours and a transient decrease in the N+F group at 2 hours; however, it increased at 4 hours after injection. Fos-like immunoreactivity (FLI) and Prodynorphin-like immunoreactivity (PLI) neurons decreased in the K+F group but increased in the N+F group at 2 hours after injection. While FLI decreased, PLI increased in all groups at 4 hours after injection. Conclusions: We suggest that NMDA and kappa opioid receptors can modulate DREAM protein expression, which can affect pain behavior and protein transcriptional processes at 2 hours and bring about either harmful or protective effects at 4 hours after formalin injection.

Modulation of the aqueous extract of Bupleuri radix on glycine-induced current in the acutely dissociated rat periaqueductal gray neurons

  • Sung, Yun-Hee;Shin, Mal-Soon;Kim, Tae-Soo;Lee, Sang-Won;Kim, Youn-Jung;Shin, Hye-Sook;Kim, Hong;Kim, Chang-Ju
    • Advances in Traditional Medicine
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    • 제7권5호
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    • pp.549-555
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    • 2008
  • Bupleuri radix (Umbelliferae), the dried root of Bupleurum Chinense DC, has been clinically used to mitigate pain sensation. The descending pain control system consists of three major components, and modulation of pain in the periaqueductal gray is the most extensively studied descending pain control system. However, the relation of Bupleuri radix on the descending pain control system has not been clarified. In the present study, modulation of the aqueous extract of Bupleuri radix on glycine-induced ion current in the acutely dissociated periaqueductal gray neurons was investigated by using nystatin-perforated patch-clamp technique under voltage-clamp condition. In the present results, the glycine-induced ion current was significantly suppressed by 0.1 mg/ml Bupleuri radix, while treatment with $10^{-5}\;M$ naltrexone, opioid receptor antagonist, alleviated Bupleuri radix-induced inhibition on glycine-induced ion current. The present study showed that the aqueous extract of Bupleuri radix may activate descending pain control system through inhibition on glycine-induced ion current in the periaqueductal gray neurons and this effect is mediated by opioid receptors.

발목염좌에 배혈에 따른 전침과 고주파온침의 진통효과 (Analgesia of Electroacupuncture and Radio-Frequency Warm Needling in Acupoint Combination on Ankle Sprain in Rats)

  • 양승범;김민수;김재효
    • Korean Journal of Acupuncture
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    • 제35권1호
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    • pp.27-35
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    • 2018
  • Objectives : The purpose of this study was to investigate the analgesic effect of electroacupuncture(EA) and radio-frequency warm needling(RFWN) stimulation in acupoint combination on ankle sprained pain in rats. Methods : The lateral ligaments of the Sprague-Dawley rats ankle were injured surgically resulting in sprain, of which was divided into EA, RFWN treatment groups and control group without treatment. The level of pain was measured through foot weight bearing force ratio followed by calculating pain relief. To stimulate proximal or distal area in ankle sprain, combination of proximal acupoints(GB34-GB39) and distal acupoints(GB39-GB42) from sprain area were applied, respectively, to either EA or RFWN stimulation. In addition, naltrexone or phentolamine was injected intraperitoneally before the stimulation to observe the pathway of analgesic effects. Results : In the proximal combination of GB34-GB39, EA and RFWN significantly increased pain relief compared to the control group (p<0.05). However, in distal combination with GB39-GB42, both EA and RFWN stimulation did not relieve pain due to ankle sprains. In the combination of GB34-GB39, the analgesia of EA was inhibited by blockade of the ${\alpha}$-adrenoceptor receptor. The analgesia of RFWN was inhibited by blockade of the ${\alpha}$-adrenoceptor receptor as well as ${\mu}$-opioid receptor. Conclusions : We observed that the proximal combination was effective in relieving pain when the treatment by acupoint combination was applied to the ankle sprain pain. Also, it was confirmed that this analgesia was also related to the pathways of ${\mu}$-opioid receptors and/or ${\alpha}$-adrenoceptors.