• Title/Summary/Keyword: benzodiazepine receptor

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Sinomenine, an Alkaloid Derived from Sinomenium acutum Potentiates Pentobarbital-Induced Sleep Behaviors and Non-Rapid Eye Movement (NREM) Sleep in Rodents

  • Yoo, Jae Hyeon;Ha, Tae-Woo;Hong, Jin Tae;Oh, Ki-Wan
    • Biomolecules & Therapeutics
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    • v.25 no.6
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    • pp.586-592
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    • 2017
  • Sinomenium acutum has been long used in the preparations of traditional medicine in Japan, China and Korea for the treatment of various disorders including rheumatism, fever, pulmonary diseases and mood disorders. Recently, it was reported that Sinomenium acutum, has sedative and anxiolytic effects mediated by GABA-ergic systems. These experiments were performed to investigate whether sinomenine (SIN), an alkaloid derived from Sinomenium acutum enhances pentobarbital-induced sleep via ${\gamma}$-aminobutyric acid (GABA)-ergic systems, and modulates sleep architecture in mice. Oral administration of SIN (40 mg/kg) markedly reduced spontaneous locomotor activity, similar to diazepam (a benzodiazepine agonist) in mice. SIN shortened sleep latency, and increased total sleep time in a dose-dependent manner when co-administrated with pentobarbital (42 mg/kg, i.p.). SIN also increased the number of sleeping mice and total sleep time by concomitant administration with the sub-hypnotic dosage of pentobarbital (28 mg/kg, i.p.). SIN reduced the number of sleep-wake cycles, and increased total sleep time and non-rapid eye movement (NREM) sleep. In addition, SIN also increased chloride influx in the primary cultured hypothalamic neuronal cells. Furthermore, protein overexpression of glutamic acid decarboxylase ($GAD_{65/67}$) and $GABA_A$ receptor subunits by western blot were found, being activated by SIN. In conclusion, SIN augments pentobarbital-induced sleeping behaviors through $GABA_A$-ergic systems, and increased NREM sleep. It could be a candidate for the treatment of insomnia.

A Case Report of Korean Medicine Treatment Including Samchulgunbi-tang-gagambang in a Patient with Vestibular Neuritis (비위허약으로 변증된 전정신경염 환자의 삼출건비탕가감방을 포함한 한의 치료 치험 1례)

  • Ye-seul Park;Jeong-hui Kim;Ju-yeon Song;Ho-ryong Yoo;In-chan Seol;Yoon-sik Kim
    • The Journal of Internal Korean Medicine
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    • v.44 no.4
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    • pp.757-764
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    • 2023
  • Background: Vestibular neuritis is a common cause of acute unilateral peripheral vestibulopathy. Vestibular neuritis is the second most common disease among patients with dizziness. Clinical symptoms of vestibular neuritis include the sudden onset of vertigo with spontaneous nystagmus, unsteady gait, nausea, and vomiting that last from days to weeks. However, even after the vertigo disappears, difficulty maintaining balance while walking may persist for weeks to months. Antihistamines, serotonin receptor blockers, and benzodiazepine vestibular suppressants are widely used as symptomatic treatments to reduce the severity of symptoms that occur in the acute phase. Case Summary: A patient diagnosed with acute vestibular neuritis was treated with acupuncture, moxibustion, and herbal medicine. We used the visual analog scale (VAS) to assess each symptom and the vertigo score to observe the effect of treatment. After treatment, the VAS scores for each symptom and the vertigo score decreased, and the severity of nystagmus was reduced. Conclusion: This study suggests that Korean medicine treatments, including Samchulgunbi-tang-gagam, could be effective in improving the clinical symptoms of vestibular neuritis.

Effect of Cooking Methods and Reheating on Texture of Sausage (시판소시지의 조리방법 및 재가열이 조직특성에 미치는 영향)

  • 김성희;이숙미;조정순
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.1
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    • pp.37-44
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    • 1997
  • The Purpose of this study was to evaluate the effect of cooking methods and reheating on texture characteristics of sausage. Sausage samples were cooked(microwaving, gas-broiling and frying), reheated on day 3 and 6 after refrigeration and put to evaluation of sensory and texture characteristics. The results of sensory evaluation showed that hardness, salty taste, rancid flavor and after-taste were increased but wetness and chewiness were decreased by reheating after refrigeration. Overall acceptability was the highest when the samples were gas broiled and reheated on day 3 after refrigeration. As for the estimation of texture changes by rheometer, hardness, cohesiveness, elasticity, gum-miness and chewiness tended to increase by reheating after refrigeration. Hardness, cohesiveness, gumminess and chewiness were the highest when the samples were gas-broiled and reheated on day 3 after refrigeration.

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Neuropeptides in Clinical Psychiatric Research : Endorphins and Cholecystokinins (정신질환에 있어서의 신경펩타이드 연구 - Endorphin과 cholecystokinin을 중심으로 -)

  • Kim, Young Hoon;Shim, Joo Chul
    • Korean Journal of Biological Psychiatry
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    • v.5 no.1
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    • pp.34-45
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    • 1998
  • We provide the reader with a brief introduction to the neurobiology of neuropeptides. Several comprehensive reviews of the distribution and neurochemical, neurophysiological, neuropharmacological and behavioral effects of the major neuropeptides have recently appeared. In reviews of the large number of neuropeptides in brain and their occurance in brain regions thought to be involved in the pathogenesis of major psychiatric disorders, investigators have sought to determine whether alternations in neuropeptide systems are associated with schizophrenia, mood disorders, anxiety disorders, alcoholism and neurodegenerative disease. There is no longer any doubt that neuropeptide-containing neurons are altered in several neuropsychiatric disorders. One of the factors that has hindered neuropeptide research to a considerable extent is the lack of pharmacological agents that specifically alter the synaptic availability of neuropeptides. With the exception of naloxone and naltrexone, the opiate-receptor antagonists, there are few available neuropeptide- receptor antagonists. Two independent classes of neuropeptide-receptor antagonists has been expected to be clinically useful. Naltrexone, a potent ${\mu}$-receptor antagonist, has been used successfully to reduce the need for alcohol consumption. And cholecycstokinin antagonists are now in development as a new class of anxiolytics, which would be expected to be free from tolerance and physical dependence and lack of sedation. In this review, we deal with these two kinds of neuropeptide system, the opioid system and cholesystokinins in the brain. The role of opioid systems in the reinforcement after alcohol consumtion and that of cholesystokinins in the pathogenesis of anxiety will be discussed briefly. As we know, the future for neuropeptides in psychiatry remains bright indeed.

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A Convenient Radiolabeling of [$^{11}$C](R)-PK11195 Using Loop Method in Automatic Synthesis Module ($^{11}$C 표지 자동합성장치에서 루프법을 이용한 ($^{11}$C)(R)-PK11195의 간편한 합성법)

  • Lee, Hak-Jeong;Jeong, Jae-Min;Lee, Yun-Sang;Kim, Hyung-Woo;Choi, Jae-Yeon;Lee, Dong-Soo;Chung, June-Key;Lee, Myung-Chul
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.4
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    • pp.337-343
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    • 2009
  • Purpose: ((R)-1-(2-chlorophenyl)-N-1-[$^{11}$C]methyl-N(1-propyl)-3-isoquinoline carboxamide ((R)-PK11195) is a specific ligand for the peripheral type benzodiazepine receptor and a marker of activated microglia, used to measure inflammation in neurologic disorders. We report here that a direct and simple radiosynthesis of [$^{11}$C](R)-PK11195 in mild condition using NaH suspension in DMF and one-step loop method. Materials and Methods: (R)-N-Desmethyl-PK11195 (1 mg) in DMSO (0.1 mL) and NaH suspension in DMF (0.1 mL) were injected into a semi-prep HPLC loop. [$^{11}$C]methyl iodide was passed through HPLC loop at room temperature. Purification was performed using semi-preparative HPLC. Aliquots eluted at 11.3 min were collected and analyzed by analytical HPLC and mass spectrometer. Results: The labeling efficiency of [$^{11}$C](R)-PK11195 was 71.8$\pm$8.5%. The specific activity was 11.8:$\pm$6.4 GBq/$\mu$mol and radiochemical purity was higher than 99.2%. The mass spectrum of the product eluted at 11.3 min showed m/z peaks at 353.1 (M+1), indicating the mass and structure of (R)-PK11195. Conclusion: By the one-step loop method with the [$^{11}$C]CH3l automated synthesis module, [$^{11}C$](R)-PK11195 could be easily prepared in high radiochemical yield using NaH suspension in DMF.