• Journal of Physiology & Pathology in Korean Medicine
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• v.18 no.1
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• pp.110-113
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• 2004

The Baenong-san has long been used for treatment of inflammatory in Korea. In this study, the anti-inflammatory effects of Baenong-san water extract (BWX) were investigated in proteinase-activated receptor-2 (PAR2)-mediated rat paw edema. Paw edema was induced by injection of trypsin or trans-cinnamoyl-LIGRLO-NH₂ (to-NH₂) into hindpaw of rats. BWX (10, 50, 100 and 200mg/kg) was orally administered 1 h before induction of inflammation. At doses of 50, 100 and 200 mg/kg, BWX showed significant inhibition of both change in paw volume and vascular permeability. BWX(100mg/kg) significantly also inhibited PAR2 agonist-induced myeloperoxidase (MPO) activity in paw tissue. This study demonstrated that BWX has an anti-inflammatory action for PAR2-mediated paw edema.

• Proceedings of the Korean Biophysical Society Conference
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• 1999.06a
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• pp.55-55
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• 1999

Imperatoxin A (IpTx$_{a}$), a 3.7 kDa peptide from the African scorpion Pandinus imperator, has been known as an agonist of skeletal ryanodine receptor (RyR). In order to study the structure and function of the toxins on RyR, the IpTx$_{a}$ cDNA was PCR-amplified using 3 pairs of primers and the toxin was expressed in E. coli expression system.(omitted)ted)

• YAKHAK HOEJI
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• v.47 no.5
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• pp.325-330
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• 2003

Solanum melongena L. (Solanaceae) has anti-oxidant, analgesic, and hypolipidemic effects. We previously showed that Solanum melongena (SM) aqueous extract inhibits mast cell-mediated allergic reactions. The activation of protease-activated receptor-2 (PAR-2) induces acute inflammation in rat hindpaw. In the present study, we investigated the effects of the SM aqueous extract on mouse paw edema induced by PAR2 agonists. Trypsin or trans-cinnamoyl-LIGRLO-NH$_2$ (tc-NH$_2$), PAR-2 agonists, was injected into the hind paw of mice to induce paw edema. SM aqueous extract (1, 5, 10, and 100 mg/kg) was orally administered 1 hr before induction of paw edema. SM aqueous extract (5, 10, and 100 mg/kg) significantly inhibited both paw edema and vascular permeability in the dose-dependent manner. Furthermore, SM aqueous extract (10 mg/kg) significantly inhibited PAR-2 agonist-induced myeloperoxidase (MPO) activity and tumor necrosis factor (TNF)-$\alpha$ expression in paw tissue compared to that of saline. These results suggest that SM aqueous extract may be useful for treatment of PAR-2-mediated inflammation.

• Biomolecules & Therapeutics
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• v.20 no.3
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• pp.256-267
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• 2012

Tamoxifen is a central component of the treatment of estrogen receptor (ER)-positive breast cancer as a partial agonist of ER. It has been clinically used for the last 30 years and is currently available as a chemopreventive agent in women with high risk for breast cancer. The most challenging issue with tamoxifen use is the development of resistance in an initially responsive breast tumor. This review summarizes the roles of ER as the therapeutic target of tamoxifen in cancer treatment, clinical values and issues of tamoxifen use, and molecular mechanisms of tamoxifen resistance. Emerging knowledge on the molecular mechanisms of tamoxifen resistance will provide insight into the design of regimens to overcome tamoxifen resistance and discovery of novel therapeutic agents with a decreased chance of developing resistance as well as establishing more efficient treatment strategies.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.355.1-355.1
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• 2002

Recently. we have reported that several lipoxygenases products directly activate the capsaicin-activated channel as intracellular messengers in neuron. In particular, 12-(S)-hydroperoxyeicosatetraenoic acid turned out to be the most potent endogenous VR activator. This finding prompted us to search for a novel non-vaniloid VR agonists and antagonists. We have designed and synthesized a series of non-vanilloid VR binding ligands based on the structural simllarity between 12-HPETE and capsaicin, the natural VR agonist. Our recent studies on the development of selective vanilloid receptor agonists and antagonists will be presented.

• Journal of Oriental Neuropsychiatry
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• v.15 no.1
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• pp.77-86
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• 2004

Objective : This study was performed to investigate the agonistic activity of Chunmajeongal-tang extract to the $GABA_A/benzodiazepine$ receptor complex. Methods : Male mice and Sprague-Dawley rats were used for this experiment. Chunmajeongal-tang Prescription was extracted with 80% methanol, evaporated in vacuo and dried with freeze dryer. The agonistic activity to the GABA/ benzodiazepine receptor complex and GABA transaminase activity were measured in vitro. Results : Chunmajeongal-tang extract inhibited dose-dependently the binding of [3H]Ro15-1788, an antagonist on GABA/benzodiazepine receptor complex, in rat cerebral cortices, showing $82.4{\pm}4.12%$ inhibition at a dose of 5.0 mg/kg. This extract inhibited dose-dependently the binding of [3H]flunitrazepam, an agonist on GABA/benzodiazepine receptor complex, in rat cerebral cortices, showing $5.6{\pm}1.24%$ inhibition. Furthermore, Chunmajeongal-tang extract inhibited the binding of [3H]flunitrazepam in the presence of GABA/NaCI with $13.2{\pm}0.44%$ inhibition, its inhibitory effect exhibited a positive GABA shift, which means that this extract activates a GABAergic neurotransmission.

• The Korean Journal of Pharmacology
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• v.32 no.2
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• pp.151-158
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• 1996

Following the subcutaneous administration of $R(-)N^6-(2-phenylisopropyl)adenosine(600\;nmol/kg/hr)$ to rats for 1 week using t$Alzet^{\circledR}$ mini-osmotic pumps, $A_1$ adenosine receptor functions were determined using $[^3H]DPCPX$ binding, $[^{35}S]GTP_{\gamma}S$ binding, and adenylyl cyclase assays. $A_1$ adenosine receptor binding and the inhibition of adenylyl cyclase activity by PIA was not altered in cerebrocortical membranes prepared from PIA-treated rats. However, there was a significant decrease in the $A_1$ adenosine receptor-mediated stimulation of $[^{35}S]GTP_{\gamma}S$ binding to cerebrocortical membranes prepared from PIA-treated rats(22.0% decrease in basal activity; 19.7% decrease in maximal activity). These results suggest that the desensitization of $A_1$ adenosine receptors following chronic administration involves agonist-induced uncoupling of the receptors from G proteins rather than alteration of $A_1$ adenosine receptor molecules. It is also suggested that the determination of stimulation of $[^{35}S]GTP_{\gamma}S$ binding to G proteins is a suitable tool in studying the receptor regulation including desensitization

• Proceedings of the Ginseng society Conference
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• 1990.06a
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• pp.36-44
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• 1990

The analgesic effect of morphine was antagonized and the development of tolerance was suppressed by the modification of the neurologic function in the animals treated with ginseng saponins. The activation of the spinal descending inhibitory systems as well as the supraspinal structures by the administration of morphine was inhibited in the animals treated with ginseng saponins intracerebrally or intrathecally The development of morphine tolerance and dependence, and the abrupt expression of naloxone induced abstinence syndrome were also inhibited by ginsenoside Kbl , Rba, Rgl and Re. These results suggest that ginsenoside Kbl, Rba, Rgl and Re are the bioactive components of panax ginseng on the inhibition of the development of morphine tolerance and dependence, and the inhibition of abrupt abstinence syndrome. In addition, further research on the minor components of Panax ginseng should be investigated. A single or daily treatment with ginseng saponins did not induce any appreciable changes in the brain level of monoamines at the various time intervals and at the various day intervals, respectively The inhibitory or facilitated effects of ginseng saponins on electrically evoked contractions in guinea pig ileum (U-receptor) and mouse was definers (5·receptor) were not mediated through opioid receptors. The antagonism of a x receptor agonist, U-, iO.488H was also not mediated through opioid receptors in the animals treated with ginseng saponins, bolt mediated through serotonergic mechanisms. Ginseng saponins inhibited morphine S-dehydrogenase that catalyzed the production of morphine from morphine, and increased hepatic glutathione contents for the detoxification of morphine. This result suggests that the dual action of the above plays an important role in the inhibition of the development of morphine tolerance and dependence.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.6
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• pp.647-655
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• 1997

The purpose of present study is to investigate the influence of a spinal gamma-aminobutyric acid B($GABA_B$) receptor on a central regulation of blood pressure(BP) and heart rate(HR), and to define its mechanism in the spinal cord. In urethane-anesthetized, d-tubocurarine-paralyzed and artificially ventilated male Sprague-Dawley rats, intrathecal administration of drugs were carried out using injection cannula(33-gauge stainless steel) through the guide cannula(PE 10) which was inserted intrathecally at lower thoracic level through the puncture of a atlantooccipital membrane. Intrathecal injection of an $GABA_B$ receptor agonist, baclofen(30, 60, 100 nmol) decreased both BP and HR dose-dependently. Pretreatment with 8-bromo-cAMP(50 nmol), a cAMP analog, or glipizide(50 nmol), a ATP-sensitive $K^+$ channel blocker, attenuated the depressor and bradycardic effects of baclofen(100 nmol), but not with 8-bromo-cGMP(50 nmol), a cGMP analog. These results suggest that the $GABA_B$ receptor in the spinal cord plays an inhibitory role in central cardiovascular regulation and that this depressor and bradycardic actions are mediated by the decrease of cAMP via the inhibition of adenylate cyclase and the opening of $K^+$ channel.

• Biomedical Science Letters
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• v.12 no.2
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• pp.113-118
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• 2006

Major pelvic ganglia (MPG) in rats are an unique autonomic ganglia, containing both sympathetic and parasympathetic neurons related with the function of bladder, penis and bowel. It has been widely known that ionotropic $GABA_A$ receptors are the molecular target of $\gamma$-aminobutric acid (GABA), a major inhibitory neurotransmitter in central nervous system. However, their functions and regulations of $GABA_A$ receptors expressed in autonomic ganglia have been poorly understood. 1 examined the modulatory role of adenylyl cyclase (AC) and protein kinase A(PKA) on $GABA_A$-induced inward currents in the neurons of rat MPG. $GABA_A$ receptors were identified using immunofluorescent labeling in the rat major pelvic ganglion. Electrophysiological experiments were performed to record the activities of $GABA_A$ receptors. $GABA_A$ receptors were expressed only in sympathetic neurons. GABA induced marked inward currents in a concentration-dependent manner. Mucimol ($5{\mu}M$), a $GABA_A$ receptor agonist induced inward currents were significantly reduced in the presence of SQ 225361 $20{\mu}M$, a AC inhibitor and myristoylated PKA inhibitor 100 nM. In addition, forskolin ($1{\mu}M$), AC activator, augmented the GABA induced currents. The activation of AC/PKA-dependent pathway could involve in the regulation $GABA_A$ receptors, expressed only in sympathetic neurons of rat MPG. These findings are helpful for the better understanding the function of various pelvic organs innervated by MPG.