• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.364.2-364.2
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• 2002

(S) and (R) 12-HETE. endogenous eicosanoids. have recently been discovered to be implicated in a number of important biological activities. In particular. it has recently been reported by us that both the capsaicin-activated channel of sensory neurons and the cloned capsaicin receptor (VR1) are activated by the eicosanoids including these metabolites. We report herein a novel and efficient asymmetric synthesis of highly enantiomerically enriched 12(S)-HETE via enzymatic kinetic resolution of the key allylic alcohol synthon. (omitted)

• The Korean Journal of Pain
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• 제33권2호
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• pp.108-120
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• 2020

From the perspective of the definition of pain, pain can be divided into emotional and sensory components, which originate from potential and actual tissue damage, respectively. The pharmacologic treatment of the emotional pain component includes antianxiety drugs, antidepressants, and antipsychotics. The anti-anxiety drugs have anti-anxious, sedative, and somnolent effects. The antipsychotics are effective in patients with positive symptoms of psychosis. On the other hand, the sensory pain component can be divided into nociceptive and neuropathic pain. Non-steroidal anti-inflammatory drugs (NSAIDs) and opioids are usually applied for somatic and visceral nociceptive pain, respectively; anticonvulsants and antidepressants are administered for the treatment of neuropathic pain with positive and negative symptoms, respectively. The NSAIDs, which inhibit the cyclo-oxygenase pathway, exhibit anti-inflammatory, antipyretic, and analgesic effects; however, they have a therapeutic ceiling. The adverse reactions (ADRs) of the NSAIDs include gastrointestinal problems, generalized edema, and increased bleeding tendency. The opioids, which bind to the opioid receptors, present an analgesic effect only, without anti-inflammatory, antipyretic, or ceiling effects. The ADRs of the opioids start from itching and nausea/vomiting to cardiovascular and respiratory depression, as well as constipation. The anticonvulsants include carbamazepine, related to sodium channel blockade, and gabapentin and pregabalin, related to calcium blockade. The antidepressants show their analgesic actions mainly through inhibiting the reuptake of serotonin or norepinephrine. Most drugs, except NSAIDs, need an updose titration period. The principle of polypharmacy for analgesia in case of mixed components of pain is increasing therapeutic effects while reducing ADRs, based on the origin of the pain.

• The Korean Journal of Physiology and Pharmacology
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• 제3권1호
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• pp.35-45
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• 1999

Excitatory amino acid (EAA) and substance P (SP) have been known to be primary candidates for nociceptive neurotransmitter in the spinal cord, and calcium ions are implicated in processing of the sensory informations mediated by EAA and SP in the spinal cord. In this study, we examined how $Ca^{2+}$ modified the responses of dorsal horn neurons to single or combined iontophoretical application of EAA and SP in the rat. All the LT cells tested responded to kainate, whereas about 55% of low threshold (LT) cells responded to iontophoretically applied NMDA. NMDA and kainate excited almost all wide dynamic range (WDR) cells. These NMDA- and kainate-induced WDR cell responses were augmented by iontophoretically applied EGTA, but suppressed by $Ca^{2+},\;Mn^{2+},$ verapamil and ${\omega}-conotoxin$ EVTA, effect of verapamil being more prominent and well sustained. $Ca^{2+}$ and $Mn^{2+}$ antagonized the augmenting effect of EGTA. On the other hand, prolonged spinal application of EGTA suppressed the response of WDR cell to NMDA. SP had triple effects on the spontaneous activity as well as NMDA-induced responses of WDR cells: excitation, inhibition and no change. EGTA augmented, but $Ca^{2+},\;Mn^{2+}$ and verapamil suppressed the increase in the NMDA-induced responses and spontaneous activities of WDR cells following iontophoretical application of SP. These results suggest that in the spinal cord, sensory informations mediated by single or combined action of EAA and SP can be modified by the change in calcium ion concentration.

• 혜화의학회지
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• 제9권1호
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• pp.661-689
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• 2000

We came to the conculsion after considering all of information from many kinds of books on the cause, pathogenesis and treatment of Flaccidity-syndrome. The results were as follows : 1. Flaccidity-syndrome means limb-relaxation due to muscle atony that isn't able to constraction. It's begun as mild degree from extremities, in some cases ended to quadriplegia or expire. 2. Cause factor and pathogenesis of Flaccidity-syndrome is various. After Lung fluid consuption caused by heat-evil was refered in The Yellow Emperor's Canon of Internal Medicine. They were refered as cause factor that Main channel asthenia, excess of sexual intercourse, wetness-evil, heat-evil gets into the interior, asthenia of the spleen and stomach. Since Ming Dynasty, It's classified to wetness-heat evil, wetness-phlegm, deficiency of vital energy, deficiency of blood, deficiency of yin, blood stasis and indygestion, etc. 3. In the view of treatment of Flaccidity-syndrome, Yangming was selected in The Yellow Emperor's Canon of Internal Medicine, and it's been mean to clear away wetness-heat evil located at Yangming. In the method of acupuncture it was same on the base, and many skills have been used that electronic acupuncture, point-injection theraphy, acupuncture point block, catgut implantaion at acupuncture point, cutaneous acupuncture, auriculo-acupuncture and head acupuncture by the through post generation. 4. Flaccidity-syndrome was defined to weak, disuse and non-pain. Beacause it was non-pain, so medicine to expel wind-evil was prevented to use. But through post generation Flaccidity-syndrome has been treated that is able to cause pain or numness as arthralgia-syndrome. Therefore there is tendency that medicine to expel wind-evil is capable within pathological basement of Flaccidity-syndrome in recent. 5. In the view of west-medicine, Flaccidity-syndrome is diplegia or quadriplegia with sensory disorder, muscle atropy in some cases. And there are spinal disease, peripheral nerve disease, muscular disease, nerve-muscle copula disease. The symptoms are able to amyotomia, numness, sensory disorder, pain.

• 한국응용곤충학회지
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• 제50권4호
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• pp.383-393
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• 2011

의사소통은 생존과 번식을 위해 필요한 행동을 가능하게 하기 때문에 행동과 진화연구에 중추적이다. 동물의 신호와 관련하여 가장 중요하고 어려운 문제 중의 하나는 의사소통의 정의이다. 넓게 봐서 의사소통은 신호자로부터 수신자로의 정보제공이다. 그러나 신호의 진화는 정보교환으로 신호자와 수신자 모두 적합도가 증가할 때만 가능하다. 이것을 '참의사소통'이라한다. 동물들이 의사소통할 때 감각채널로 흔히 화학물질, 빛, 소리를 이용한다. 화학신호를 이용한 의사소통은 가장 오래되고, 거의 모든 동물들이 사용하는 방법이다. 변조의 용이, 신호생산의 유연성, 빠른 전송 때문에 빛 과 소리를 이용한 의사소통은 보다 많은 양의 정보를 전달할 수 있다. 교미행동과 충돌해결은 동물들이 의사소통하는 가장 흔한 상황이다. 교미행동에 사용되는 신호는 보통 종에 대한 정보와 성적 매력도에 대한 정보를 담고 있으며, 충돌해결에 사용되는 정보는 신호자의 싸움능력에 대한 정보를 담고 있다. 이외에도 동물들이 의사소통하는 상황은 영역방어, 부모자식 상호작용, 사회통합, 환경정보 공유, 자기의사 소통을 포함한다.

• International Journal of Oral Biology
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• 제46권3호
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• pp.119-126
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• 2021

Activation of transient receptor potential vanilloid 1 (TRPV1), a calcium permeable channel expressed in primary sensory neurons, induces the release of glutamate from their central and peripheral afferents during normal acute and pathological pain. However, little information is available regarding the glutamate release mechanism associated with TRPV1 activation in primary sensory neurons. To address this issue, we investigated the expression of vesicular glutamate transporter (VGLUT) in TRPV1-immunopositive (+) neurons in the rat trigeminal ganglion (TG) under normal and complete Freund's adjuvant (CFA)-induced inflammatory pain conditions using behavioral testing as well as double immunofluorescence staining with antisera against TRPV1 and VGLUT1 or VGLUT2. TRPV1 was primarily expressed in small and medium-sized TG neurons. TRPV1+ neurons constituted approximately 27% of all TG neurons. Among all TRPV1+ neurons, the proportion of TRPV1+ neurons coexpressing VGLUT1 (VGLUT1+/TRPV1+ neurons) and VGLUT2 (VGLUT2+/TRPV1+ neurons) was 0.4% ± 0.2% and 22.4% ± 2.8%, respectively. The proportion of TRPV1+ and VGLUT2+ neurons was higher in the CFA group than in the control group (TRPV1+ neurons: 31.5% ± 2.5% vs. 26.5% ± 1.2%, VGLUT2+ neurons: 31.8% ± 1.1% vs. 24.6% ± 1.5%, p < 0.05), whereas the proportion of VGLUT1+, VGLUT1+/TRPV1+, and VGLUT2+/TRPV1+ neurons did not differ significantly between the CFA and control groups. These findings together suggest that VGLUT2, a major isoform of VGLUTs, is involved in TRPV1 activation-associated glutamate release during normal acute and inflammatory pain.

• The Korean Journal of Physiology and Pharmacology
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• 제1권6호
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• pp.625-637
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• 1997

Calcium ions are implicated in a variety of physiological functions, including enzyme activity, membrane excitability, neurotransmitter release, and synaptic transmission, etc. Calcium antagonists have been known to be effective for the treatment of exertional angina and essential hypertension. Selective and nonselective voltage-dependent calcium channel blockers also have inhibitory action on the acute and tonic pain behaviors resulting from thermal stimulation, subcutaneous formalin injection and nerve injury. This study was undertaken to investigate the effects of iontophoretically applied $Ca^{++}$ and its antagonists on the responses of WDR (wide dynamic range) cells to sensory inputs. The responses of WDR cells to graded electrical stimulation of the afferent nerve and also to thermal stimulation of the receptive field were recorded before and after iontophoretical application of $Ca^{++}$, EGTA, $Mn^{++}$, verapamil, ${\omega}-conotoxin$ GVIA, ${\omega}-conotoxin$ MVIIC and ${\omega}-agatoxin$ IVA. Also studied were the effects of a few calcium antagonists on the C-fiber responses of WDR cells sensitized by subcutaneous injection of mustard oil (10%). Calcium ions and calcium channel antagonists ($Mn^{++}$, verapamil, ${\omega}-conotoxin$ GVIA & ${\omega}-agatoxin$ IVA) current-dependently suppressed the C-fiber responses of WDR cells without any significant effects on the A-fiber responses. But ${\omega}-conotoxin$ MVIIC did not have any inhibitory actions on the responses of WDR cell to A-fiber, C-fiber and thermal stimulation. Iontophoretically applied EGTA augmented the WDR cell responses to C-fiber and thermal stimulations while spinal application of EGTA for about $20{\sim}30\;min$ strongly inhibited the C-fiber responses. The augmenting and the inhibitory actions of EGTA were blocked by calcium ions. The WDR cell responses to thermal stimulation of the receptive field were reduced by iontophoretical application of $Ca^{++}$, verapamil, ${\omega}-agatoxin$ IVA, and ${\omega}-conotoxin$ GVIA but not by ${\omega}-conotoxin$ MVIIC. The responses of WDR cells to C-fiber stimulation were augmented after subcutaneous injection of mustard oil (10%, 0.15 ml) into the receptive field and these sensitized C-fiber responses were strongly suppressed by iontophoretically applied $Ca^{++}$, verapamil, ${\omega}-conotoxin$ GVIA and ${\omega}-agatoxin$ IVA. These experimental findings suggest that in the rat spinal cord, L-, N-, and P-type, but not Q-type, voltage-sensitive calcium channels are implicated in the calcium antagonist-induced inhibition of the normal and the sensitized responses of WDR cells to C-fiber and thermal stimulation, and that the suppressive effect of calcium and augmenting action of EGTA on WDR cell responses are due to changes in excitability of the cell.

• 한국자기공명학회논문지
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• 제11권2호
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• pp.85-94
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• 2007

Vanilloid receptor I [transient receptor potential vanilloid subfamily member 1 (TRPV1), also known as VR1] is a non-selective cationic channel activated by noxious heat, vanilloids, and acid, thereby causing pain. VR1 possesses six transmembrane domain and N-and C-terminus cytosolic domains, and appears to be a homotetramer. We studied the structural properties of Cterminus of VR1 (VR1C) using CD and NMR spectroscopy. DPC micelles, with a zwitterionic surface, and SDS micelles, with a negatively charged surface, were used as a membrane mimetic model system. Both SDS and DPC micelles could increase the stability of helical structures and/or reduce the aggregation form of the VR1C. However, the structural changing mode of the VR1C induced by the SDS and DPC micelles was different. The changes according to the various pHs were also different in two micelles conditions. Because the net charges of the SDS and DPC micelles are negative and neutral, respectively, we anticipate that this difference might affect the structure of the VR1C by electrostatic interaction between the surface of the VR1C and phospholipids of the detergent micelles. Based on these similarity and dissimilarity of changing aspects of the VR1C, it is supposed that the VR1C probably has the real pI value near the pH 7. Generally, mild extracellular acidic pH ($6.5{\sim}6.8$) potentiates VRI channel activation by noxious heat and vanilloids, whereas acidic conditions directly activate the channel. The channel activation of the VRI might be related to the structural change of VR1C caused by pH (electrostatic interactions), especially near the pH 7. By measuring the $^1-^{15}N$ TROSY spectra of the VR1C, we could get more resolved and dispersed spectra at the low pH and/or detergent micelles conditions. We will try to do further NMR experiments in low pH with micelles conditions in order to get more information about the structure of VR1C.

• Korean Journal of Acupuncture
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• 제23권2호
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• pp.89-103
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• 2006

Objectives: Recently, the effect of acupuncture has been approved not only in the East but also in the West, so the interest on acupuncture was greatly improved. Especially, functional magnetic resonance imaging(fMRI) was embossed as the study tool for the mechanism of acupuncture noninvasively and many studies on the mechanism of acupuncture using fMRI were carried out. We archived the fMRI study on the brain activity induced by manual acupuncture at BL62(申脈). Methods: The study was the acupuncture at BL62(申脈) and we acquired 9 fMRI results from 6 persons$(age\;20{\sim}30,\;4\;male\;and\;2\;female)$. These studies employed The block design for mapping brain activity and acupuncture was perfomed at BL62(申脈) on the left foot. Results: The brain related motor function was cerebellum, basal ganglia and cerebral cortex and thalamus connected these elements. In the result of this study, the regions of significant activation in the cerebellum was centered on the spinocerebellum in the anterior lobe, so we presumed that this result showed the input of stimulation by the acupuncture on BL62(申脈). But basal ganglia and cerebral cortex showed the regions of significant activation in the left larger than the right and regions of the cerebral cortex was the motor and sensory cortex. Such a result explained that acupuncture at BL62(申脈) could have influence the motor function and acupuncture at left BL62(申脈) could affect the right side through the activation of the left basal ganglia and cerebral cortex. Conclusions: In the theory of crossing needling at collaterals(繆刺論), it the pathogenic factor invaded in the Yang Heel channel(陽?脈) that was one of the eight Extra meridians(奇經八脈), we recognized the disease of the collateral channel and used contralateral BL62(申脈) for treatment of the Yang Heel channel(陽?脈). Moreover the result of this study could bear the construction that acupuncture at the left BL62(申脈) treats the contralateral lesion and this construction is related to the theory of crossing needling at collaterals(繆刺論).

• Korean Journal of Acupuncture
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• 제21권2호
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• pp.1-28
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• 2004

Objectives : Human physiological changes in the state of qigong has been measured using EEG(Electroencephalography), functional MRI(functional Magnetic Resonance Image), EAV(Electro-Acupuncture according to Voll) and SQUID(Superconducting Quantum Interference Device) measurements. Methods & Results : EEGs were measured to study the differences between Qigong masters and Qi receiver on the changes of EEG. During Qigong, an alpha waves were increased. The power spectra indicate that the peak frequency of alpha waves increased during Qigong. Qi receiver's EEG signals seemed to affected by the state of himself. Brain activation did not observed when qigong master concentrates the Qi at Laogong(P8). But a localization of fMRI signal in the sensory cortex was observed by electric acupuncture stimulation at Laogong(P8). Five phase deviation of EAV were clearly changed in the both cases of Qigong master and Qi receiver. When a Qigong master concentrates the Qi at Yintang, Laogong(P8), Qihai(CV6) meridian points during Qigong state, the change of magnetic field around acupoints Yintang, Laogong points has been measured using 40-Channel DROS-SQUID apparatus. After smoothing process of the continuously measured magnetic signal around acupoints for a few minutes, we could observe that a series of peaks, magnitude of -1.0~2.5pT appeared. But there was no significant difference in changes of magnetic signal around acupoints. Physical signals of magnetocardiogram has been measured by using 2-Channel DROS SQUID(Magnetocardiogram). Physical signals of magnetocardiogram were clealy changed at the ST segments after S-wave when qigong master concentrates the Qi.