• Title/Summary/Keyword: 5HT5A 수용체

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Characterization of the drug receptors responsible for intestinal contraction in Israeli carp (이스라엘잉어 장관 수축에 관여하는 약물수용체에 관한 연구)

  • Yun, Hyo-in;Han, Kyong-oh;Park, Seung-chun;Cho, Joon-hyoung;Oh, Tae-kwang
    • Korean Journal of Veterinary Research
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    • v.34 no.3
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    • pp.447-456
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    • 1994
  • In order to elucidate the characterization of receptors involved in inestinal motility of Israeli carp, spontaneously contracting Israeli carp intestinal preperations were prepared and mounted in the organ chambers for contraction traicings using a polygraph. Various contractile agonists were treated and their dose-response curves were constructed. $EC_{50}$ values$(pD_2)$ of each agonist on specific receptors, $pA_2$ values of competitive antagonists against some agonists, and $K_1$, values of noncompetitive antagonists against some agonists were analyzed for characterization of receptors related with the intestinal contraction. Results obtained through the experiments were summarized as follows: 1. Acetylcholine(ACh) exhibited biphasic dose-response curves: initial ACh-induced dose dependent contractions were observed in pM levels but followed by decreased response in in-between concentration levels. Dose dependent contractions reappeared in ${\mu}M$ level. The peaks in pM and ${\mu}M$ levels appeared in $10^{-13}M$ and $3{\times}10^{-5}M$, respectvely. 2. Carbachol(CaCh) exhibited dose dependent contractions from $10^{-9}M$ to $10^{-5}M$, and its $pD_2$ values were higher than those of ACh($5.60{\pm}0.11$). ACh and CaCh exhibited equiactive contractions. Nicotine had no effects on contractile responses of Israeli carp intestine. 3. ACh-induced responses were inhibited by atropine($K_1:7{\times}10^{-8}M$), a muscarinic antagonist, in a non-competitive manner. But CaCh-induced responses were inhibited by both antimuscarinic atropine($pA_2:9.52{\pm}0.14$) and selective $M_2$ antagonistic 4-DAMP($pA_2:8.16{\pm}0.09$), in competitive manners. Nicotine receptor antagonistic decamethonium and hexamethonium had no effects on ACh-and CaCh-induced contractions. Therefore, the cholinergic receptor related to intestinal motility of Israeli carp was assumed as $M_2$ type. 4. In Israeli carp intestine, 5-HT (serotonin) exhibited dose dependent contractions in concentration range from $10^{-8}M$ to $10^{-5}M$. The maximal responses, however, were corresponded to about 50% of those of ACh or CaCh. 5-HT induced contractions were inhibited by $5-HT_2$ antagonistic ketanserin ($K_1: 7.8{\times}10^{-4}M$) in a non-competitive manner, but not by both of anti $5-HT_1$, spiperone and anti $5-HT_3$, MDL-72222. Hence, $5-HT_2$ receptors are suggested to be existed in Isreli carp intestine.

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The Effects of Self-administration of Methamphetamine on Serotonin Receptors Level in Rat Brain (메스암페타민 자발섭취가 흰쥐 뇌조직 중 세로토닌 수용체에 미치는 영향)

  • 박기숙;홍진태;한진이;김혜진;김용규;이종권;안광수;이선희
    • Biomolecules & Therapeutics
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    • v.9 no.2
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    • pp.88-95
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    • 2001
  • (+)-Methamphetamine (METH) is a psychostimulant, which has been the most popular abused drug in Korea. The rewarding mechanism in METH abuse has been reported to be mediated by dopaminergic system. Recently, it has been reported that dopamine releaser (phentermine) plays a dominant role in the discriminative stimulus effects of METH, whereas 5-HT releaser (fenfluramine) can strongly modify METH self-administration. The present study is designed to assess the behavioral changes and the changes of the serotonin receptors in the brains of rats administered repeated of self-administered METH. The repeated administration of 1.0 mg/kg/day METH for 12 days increased locomotor activities, and there was no difference between i.v. and i.p. treatment. Rats had actively acquired METH self-administration for 3 weeks at 0.1 or 0.2 mg/kg/injection. Whereas, it was taken few days to acquire sucrose pellet self-administration. The binding of [$^3$H]-8-hydroxy-DPAT (5-H $T_{1A}$ receptors) and [$^3$H]-5-carboxytryptamine (5-H $T_{1B}$ receptors) to brain sections was examined. Both passive administration and self-administration of METH did not change significantly the serotonin receptors levels in hippocampus, striatum and nucleus accumbens. These results suggest that serotonin receptors may not change in the acquisition period of METH self-administration, and we are trying to investigate the serotonin receptors levels of brain in rats maintained of METH self-administration.n.n.

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Comparison of Specific Proteins of Shiga Toxin-producing E. coli (STEC) Adhesion by Lactobacillus acidophilus Strains Using Two Dimensional Gel Electrophoresis (이차원 전기영동을 이용한 Lactobacillus acidophilus Strains의 Shiga Toxin-producing E. coli (STEC) 부착 억제와 관련된 단백질 발현 변화 분석)

  • Kim Young-Hoon;Moon Yong-Il
    • Food Science of Animal Resources
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    • v.26 no.2
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    • pp.263-268
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    • 2006
  • Probiotics including Lactobacillus acidophilus, refer to a group of nonpathogenic organisms that protect the human host against gastrointestinal(GI) infections by pathogenic bacteria such as Shiga toxin-producing E. coli(STEC). In the study, the inhibitory effects of STEC ATCC 43894 adhesion by L. acidophilus A4 was investigated on the HT-29 epithelial cells. Specific proteins regulated by cell Iysates of L. acidophilus A4 on STEC ATCC 43894 were also characterized by proteomic analysis. Both cell mass and Iysate of L. acidophilus A4 have exhibited the profound inhibitory activity on the HT-29 cells(about 1.5 log scale reduction). Two-dimensional gel electrophoresis(2-DE) revealed seven proteins that were up-regulated by cell Iysates of L. acidophilus A4 and three proteins that were down-regulated. In addition, three protein spots were only detected in the presence of cell Iysates. These results suggest that inhibitory effects of STEC adhesion by L. acidophilus may be due to the regulation of specific protein of STEC.

The Actions of Majarine on the Central Nervous System (II) -The Effects of Dopaminergic and Serotonergic Antagonists on Majarine-induced Hypothermia in the Mouse- (Majarine의 중추신경계에 대한 작용(II) -마우스에 있어서 Majarine의 체온감소에 미치는 dopamine, serotonin 길항제의 작용에 관한 연구-)

  • Park, Young-Hyun;Lee, Jong-Hwoa;Kim, Yu-Jae;Cho, Byung-Heon
    • The Korean Journal of Pharmacology
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    • v.21 no.2
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    • pp.99-110
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    • 1985
  • Majarine that was isolated from Berberis Koreasra Palibin (Berberidaceae) is the isoquinoline alkaloid. The effects of dopaminergic and serotonergic antagonists on majarine induced changes in body temperature were studied in the mouse. Intraperitoneal administration of majarine produced dose-dependent hypothermia. At a dose of 0.1 mg/kg, majarine caused a slight increase in body temperature. Majarine-induced hyperthermia was attenuated by the 5-HT antagonist, cyproheptadine However, it caused hyothermia in mice pretreated with the DA antagonist, haloperidol, and hyperthermia in mice pretreated with haloperidol and cyproheptadine in comparision with haloperidol pretreatment. At a dose of 2.0 mg/kg, majarine-induced hypothermia was attenuated by haloperidol and cyproheptadine, respectively. In reserpine pretreated mice, majarine produced dose-dependent hypothermia. At a dose of 0.1 mg/kg, majarine pretreated with haloperidol caused no significant effect in body temperature. At a dose of 2.0 mg/kg, majarine-induced hypothermia was attenuated by haloperidol pretreatment in mice treated with reserpine and ${\alpha}$-methyl-p-tyrosine. These data suppose that both dopaminergic and serotonergic mechanisms in the brain mediate the effects of majarine on body temperature. We propose that majarine directly stimulate DA receptor, which secondarilly activate 5-HT neurons to cause changes in body temperature.

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Review about effects of sleep disturbances on Burning mouth syndrome (수면장애가 구강작열감 증후군에 미치는 영향에 대한 고찰)

  • Lim, Hyun-Dae;Lee, You-Mee
    • Journal of Oral Medicine and Pain
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    • v.38 no.4
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    • pp.313-318
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    • 2013
  • The aim of this study was to the relationship between sleep disturbances and Burning mouth syndrome(BMS). BMS presents as a chronic burning sensation in the oral mucous membrane that is frequently associated with sleep disturbances. BMS is considered neuropathic pain condition with dysfunction of small diameter afferent sensory fiber. A review of the studies reveals, BMS suggested peripheral and cental nervous system changes. Sleep disruption or Rem sleep deprivation cause an inhibition of opioid protein synthesis and a reduced affinity of ${\mu}$ and ${\delta}$ opioid receptors. Let me say that sleep disturbances suggest a risk factor For BMS and support to evaluate as a part of BMS treatment. Further study will be required to ascertain the relationship between distruption of sleep continuity or Rem sleep deprivation and BMS and the evidence of altered neurochemical degeneration of BMS.

Anxiolytic-like Effects of the Methanol Extract of Sophorae Fructus (괴각(Sophorae Fructus) 메탄올 추출물의 항불안 효과)

  • Oh, Han Saem;Lee, Gil Yong;Jung, Ji Wook
    • Food Science and Preservation
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    • v.19 no.5
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    • pp.767-773
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    • 2012
  • The purpose of this study was to investigate the anxiolytic-like effect of the methanol extract of Sophorae fructus (MESF) using elevated plus-maze (EPM), open field test, and horizontal wire test in mice. MESF was orally administered at doses of 50, 100, 200, or 400 mg/kg to ICR mice 1 h before behavioral evaluation. The control group was given an equal volume of 10% Tween 80, and the positive control group was given diazepam (1 mg/kg, i.p.). The administration of MESF significantly increased the percentage of time spent in open arms and the entries into the open arms of the EPM compared with the 10% Tween 80-treated control group (p < 0.05). In addition, the anxiolytic-like activities of MESF were antagonized by flumazenil (a GABAA antagonist, 10 mg/kg) but not by WAY-100635 (a 5-HT1A antagonist, 0.3 mg/kg). Futhermore, there were no changes in the locomotor activity and myorelaxant effects of the experimental group, as opposed to the 10% Tween 80-treated control group. Therefore, these findings suggest that MESF promotes the anxiolytic-like activity mediated by the GABAergic nervous system in mice.