• The Korean Journal of Pain
• /
• 제9권1호
• /
• pp.151-158
• /
• 1996

Background: Buprenorphine, a new synthetic thebaine derivative, is a partial agonist of the opioid $\mu$-receptor with high receptor affinity, great lipid solubility, and slow rate of opiate receptor association and dissociation. Continuous epidural infusion of opioid can possibly produced undesirable effects, such as respiratory depression, pruritus, etc, in spite of effective postoperative analgesia. Methods: The present study was undertaken to compare the analgesic properties and side effects of continuous epidural infusion of buprenorphine combined with bupivacaine, and morphine combined with bupivacaine in 90 patients following elective gynecologic lower abdominal surgery. At the end of surgery, the initial bolus doses were 3 mg morphine (M group), 0.15 mg buprenorphine (0.15B group), 0.3 mg buprenorphine (0.3B group) combined with 0.25% bupivacaine 10ml, and subsequent continuous infusion doses were 6 mg morphine plus 0.125% bupivacine 100 ml (M group) and 0.6mg buprenorphine plus 0.125% bupivacaine 100 ml (0.15B, 0.3B, group) during 48 hours. The assessment of analgesic efficacy and side effects were made at arrival of recovery room, 1 hr, 4 hr, 8 hr, 24 hr, 36 hr, and 48 hr after the epidural injection. Results: The pain score during 48 hours was significantly higher in the 0.15B group than in the M group and 0.3B group (P<0.05), and the number of patients requiring additional analgesics was significantly higher in the 0.15B group than in the M group and 0.3B group (P<0.05). Signs of respiratory depression were not noted, and the incidence of pruritus, nausea, and vomiting was slightly lower in the 0.15B group and 0.3B group than in the M group, and the incidence of sedation and urinary retention was similar in three group. The subjective rating of satisfaction was better in the 0.3B group than in the M group and 0.15B group (P<0.05). Conclusion: The above results suggest that continuous epidural infusion of buprenorphine combined with low-dose bupivacaine is an advisable method of postoperative analgesia.

• 한국약용작물학회지
• /
• 제18권4호
• /
• pp.238-243
• /
• 2010

In the present study, the antinociceptive profiles of Viola tricolor L. (V. tricolor L.) extract were examined in ICR mice. V. tricolor L. extract administered orally (200mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, V. tricolor L. extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P (0.7 ${\mu}g$) was diminished by V. tricolor L. extract. Intraperitoneal (i.p.) pretreatment with yohimbine (${\alpha}_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by V. tricolor L. extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by V. tricolor L. extract in the writhing test. Our results suggest that V. tricolor L. extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of V. tricolor L. extract may be mediated by ${\alpha}_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.

• The Korean Journal of Physiology and Pharmacology
• /
• 제16권2호
• /
• pp.119-123
• /
• 2012

In the present study, the antinociceptive profiles of $Agrimonia$ $pilosa$ $Ledeb$ extract were examined in ICR mice. $Agrimonia$ $pilosa$ $Ledeb$ extract administered orally (200 mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, $Agrimonia$ $pilosa$ $Ledeb$ extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P (0.7 ${\mu}g$) was diminished by $Agrimonia$ $pilosa$ $Ledeb$ extract. Intraperitoneal (i.p.) pretreatment with yohimbine (${\alpha}_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by $Agrimonia$ $pilosa$ $Ledeb$ extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by $Agrimonia$ $pilosa$ $Ledeb$ extract in the writhing test. Our results suggest that $Agrimonia$ $pilosa$ $Ledeb$ extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of $Agrimonia$ $pilosa$ $Ledeb$ extract may be mediated by ${\alpha}_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.

• 약학회지
• /
• 제49권5호
• /
• pp.370-374
• /
• 2005

Lactoferrin is a multifunctional protein that is found in milk, neutrophils, and other biological fluids, and its receptors have also been identified in the central nervous system. Recently, it was reported that bovine milk-derived lacto­ferrin (BLF) produced analgesia via a $\mu$-opioid receptor-mediated response in the spinal cord. However the precise mech­anism of this analgesic effect is remains unclear. In Randall-Selitto paw pressure study, each single administration of morphine (10 mg/kg) and BLF (50, 100 and 200 mg/kg) induced analgesia, however, NMDA receptor antagonist MK-801 (0.1, 0.2 and 0.3 mg/kg), inhibited analgesia induced by BLF (100 mg/kg). Intracerebroventricular infusion (I.C.V.) of N­methyl-D-aspartic acid (NMDA) ($0.3\;{\mu}g/8.0\;{\mu}l/hr/day$), as a NMDA receptor agonist, reversed inhibition of MK-801 (0.3 mg/kg) on analgesia induced by BLF (100 mg/kg). These results suggest that BLF have analgesic effect, through NMDA recep­tor activation.

• The Korean Journal of Physiology and Pharmacology
• /
• 제14권5호
• /
• pp.285-289
• /
• 2010

In the present study, the antinociceptive profiles of $Campanula$ $punctata$ extract were examined in ICR mice. The $Campanula$ $punctata$ contain a large dose of saponin. $Campanula$ $punctata$ extract administered orally (200 mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, $Campanula$ $punctata$ extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P ($0.7{\mu}g$) was diminished by $Campanula$ $punctata$ extract. Intraperitoneal (i.p.) pretreatment with yohimbine (${\alpha}_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by $Campanula$ $punctata$ extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by $Campanula$ $punctata$ extract in the writhing test. Our results suggest that $Campanula$ $punctata$ extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of $Campanula$ $punctata$ extract may be mediated by ${\alpha}_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.

• Biomolecules & Therapeutics
• /
• 제26권2호
• /
• pp.101-108
• /
• 2018

G protein-coupled receptors (GPCRs) are the largest superfamily of transmembrane receptors and have vital signaling functions in various organs. Because of their critical roles in physiology and pathology, GPCRs are the most commonly used therapeutic target. It has been suggested that GPCRs undergo massive genetic variations such as genetic polymorphisms and DNA insertions or deletions. Among these genetic variations, non-synonymous natural variations change the amino acid sequence and could thus alter GPCR functions such as expression, localization, signaling, and ligand binding, which may be involved in disease development and altered responses to GPCR-targeting drugs. Despite the clinical importance of GPCRs, studies on the genotype-phenotype relationship of GPCR natural variants have been limited to a few GPCRs such as b-adrenergic receptors and opioid receptors. Comprehensive understanding of non-synonymous natural variations within GPCRs would help to predict the unknown genotype-phenotype relationship and yet-to-be-discovered natural variants. Here, we analyzed the non-synonymous natural variants of all non-olfactory GPCRs available from a public database, UniProt. The results suggest that non-synonymous natural variations occur extensively within the GPCR superfamily especially in the N-terminus and transmembrane domains. Within the transmembrane domains, natural variations observed more frequently in the conserved residues, which leads to disruption of the receptor function. Our analysis also suggests that only few non-synonymous natural variations have been studied in efforts to link the variations with functional consequences.

• The Korean Journal of Pain
• /
• 제18권2호
• /
• pp.113-117
• /
• 2005

Background: Serotonin 3 receptor is involved in the modulation of nociceptive transmission in the spinal cord. The serotonin 3 receptor antagonist has been used for the management of opioid-induced nausea and vomiting. The aim of this study was to examine whether the analgesic effect of morphine is antagonized by serotonin 3 receptor antagonists at the spinal level. Methods: Rats were implanted with lumbar intrathecal catheters. For nociception, a formalin solution (5%, $50{\mu}l$) was injected into the hind paw of male Sprague-Dawley rats. To determine whether the effect of intrathecal morphine was mediated via serotonin 3 receptors, serotonin 3 receptor antagonists were intrathecally administered 10 min prior to the morphine delivery. Following the formalin injection, formalin-induced nociceptive behavior (flinching response) was observed for 60 min. Results: Intrathecal morphine produced a dose-dependent suppression of the flinches in both phases during the formalin test. The analgesic action of morphine was not reversed by serotonin 3 receptor antagonists (LY-278,584, ondansetron), which had little per se effect on the formalin-induced nociception. Conclusions: Spinal serotonin 3 receptors may not be involved in the analgesia of morphine on a nociceptive state evoked by a formalin stimulus.

• Natural Product Sciences
• /
• 제20권4호
• /
• pp.285-289
• /
• 2014

Pyrrosia lingua has been widely used as a traditional medicine for the treatment of lots of diseases including pain management. However pharmacological and phytochemical studies on its anti-nociceptive properties are extremely limited. In this work, we investigated the effects of methanol extract of Pyrrosia lingua (MPL, 250 and 500 mg/kg) on the both of central and peripheral nociceptive pain. The results from tail-immersion test and hotplate test revealed that MPL has potent anti-nociceptive effects on thermal nociception. In addition, MPL efficiently reduced the acetic acid-induced chemical nociception compared to indomethacin. We also carried out formalin test and MPL reduced formalin-induced pain response on both phases, suggesting MPL has antinociceptive activities on the central and peripheral pain. In combination test using naloxone, anti-nocicpetive activity of MPL was reduced, indicating that MPL acts as a partial opioid receptor agonist. These results suggest that MPL may be possibly used as a valuable natural product-derived painkiller.

• 생약학회지
• /
• 제44권1호
• /
• pp.70-74
• /
• 2013

Ligularia stenocephala has been widely used as a traditional medicine for the treatment of lots of diseases such as asthma, arthritis, and jaundice. In this study, we evaluated the anti-nocicepitve activities of methanolic extract of L. stenocephala (MLS) using various pain models including thermal nociception as well as chemical nociception methods. MLS showed significant increase in latency time in the tail immersion test and hot-plate test. In addition, the number of acetic acid-induced abdominal constrictions was decreased by MLS. MLS also attenuated paw licking time in the formalin test. The combination test using naloxone revealed that the anti-nociceptive properties of MLS was not associated with opioid receptor activation. The present results demonstrate that MLS may possibly used as valuable analgesic agent for the treatment of nociceptive pain.

• Natural Product Sciences
• /
• 제17권3호
• /
• pp.256-260
• /
• 2011

Polygoni multiflori Ramulus, the stem of Polygonum multiflorum Thunb., has been widely used as a traditional medicine for the treatment of many diseases. Presently, antinociceptive tests of the butanolic fraction of P. multiflorum (SPB) were performed using several thermal and chemical pain models. SPB had strong and dosedependent antinociceptive activities, both thermal and chemical, compared to the reference drugs Tramadol and Indomethacin. In combination with naloxone, the analgesic activity of SPB was unchanged indicating that the antinociceptive activity of SPB was not due to action as an opioid receptor agonist. The present results indicate the potential of SPB as an analgesic agent for pain control.