- tropisetron hydrochloride
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- The Neuroprotective Effect of Tropisetron on Vincristine-Induced Neurotoxicity.
- Barzegar-Fallah A1, Alimoradi H2, Mehrzadi S3, Barzegar-Fallah N4, Zendedel A5, Abbasi A6, Dehpour AR7.Author information 1Department of Pharmacology, School of Medicine, Iran University of Medical Sciences, Tehran, Iran.2Department of Pharmacology and Toxicology, University of Otago, P.O. Box 913, Dunedin, New Zealand.3Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.4Department of Pharmacology, Islamic Azad University of Pharmaceutical Sciences, Tehran, Iran.5Institute of Neuroanatomy, Faculty of Medicine, RWTH Aachen University, Germany.6Department of Pathology, Tehran University of Medical Science, Tehran, Iran.7Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran. Electronic address: firstname.lastname@example.org.AbstractVincristine (VCR) peripheral neuropathy is a dose-limiting side effect. Several studies have shown that tropisetron, a 5-HT3 receptor antagonist, exerts anti-inflammatory and immunomodulatory properties. Current study was designed to investigate a suppressive effect of tropisetron on VCR-induced neuropathy and whether this effect exerts through the 5-HT3 receptor or not. Neuropathy was induced in rats by administration of vincristine (0.5 mg/kg, 3 intraperitoneal injections on alternate days) and in treatment group, tropisetron (3mg/kg); m-chlorophenylbiguanide (mCPBG), a selective 5-HT3 receptor agonist (15mg/kg); tropisetron (3mg/kg) plus mCPBG (15mg/kg); granisetron, another selective 5-HT3 receptor antagonist (3mg/kg) were administered intraperitoneally 1h prior to vincristine injection. Hot plate, open field tests (total distance moved, mean velocity and percentage of total duration of the movement) and Motor Nerve Conduction Velocity (MNCV) were performed to evaluate the sensory and motor neuropathy. Further, plasma levels of tumor necrosis factor-alpha (TNF-α) and interleukin-2 (IL-2) and the level of TNF-α in sciatic nerve were assessed as well as histological examination. In only VCR-treated rats hot plate latencies were significantly increased, total distance moved, mean velocity, total duration of the movement and sciatic MNCV significantly decreased compared with control. In tropisetron and tropisetron plus mCPBG groups, one injection of tropisetron prior to each VCR injection robustly diminished TNF-α and IL-2 levels, and also prevented mixed sensory-motor neuropathy, as indicated by less mortality rate, better general conditions, behavioral and electrophysiological studies. Moreover, pathological evidence confirmed the results obtained from other findings. But granisetron and mCPBG had no significant effect on the mentioned parameters. In conclusion, these studies demonstrate that tropisetron significantly suppressed VCR-induced neuropathy and could be a neuroprotective agent for prevention of VCR-induced neuropathy via a receptor-independent pathway.
- Neurotoxicology.Neurotoxicology.2013 Dec 26. pii: S0161-813X(13)00183-6. doi: 10.1016/j.neuro.2013.12.002. [Epub ahead of print]
- Vincristine (VCR) peripheral neuropathy is a dose-limiting side effect. Several studies have shown that tropisetron, a 5-HT3 receptor antagonist, exerts anti-inflammatory and immunomodulatory properties. Current study was designed to investigate a suppressive effect of tropisetron on VCR-induced neu
- PMID 24374478
- Prophylaxis of intra- and postoperative nausea and vomiting in patients during cesarean section in spinal anesthesia.
- Voigt M, Fröhlich CW, Hüttel C, Kranke P, Mennen J, Boessneck O, Lenz C, Erbes T, Ernst J, Kerger H.Author information Evangelian Deaconry Hospital, Freiburg, Germany.AbstractBACKGROUND: This paper describes a randomized prospective study conducted in 308 patients undergoing caesarean section in spinal anaesthesia at a single hospital between 2010 and 2012 to find a suitable anti-emetic strategy for these patients.
- Medical science monitor : international medical journal of experimental and clinical research.Med Sci Monit.2013 Nov 14;19:993-1000. doi: 10.12659/MSM.889597.
- BACKGROUND: This paper describes a randomized prospective study conducted in 308 patients undergoing caesarean section in spinal anaesthesia at a single hospital between 2010 and 2012 to find a suitable anti-emetic strategy for these patients.MATERIAL AND METHODS: Spinal anesthesia was performed in
- PMID 24226381
- P2X3 receptors induced inflammatory nociception modulated by TRPA1, 5-HT3 and 5-HT1A receptors.
- Krimon S, Araldi D, do Prado FC, Tambeli CH, Oliveira-Fusaro MC, Parada CA.Author information Department of Structural and Functional Biology, Institute of Biology, State University of Campinas - UNICAMP, Brazil.AbstractIt has been described that endogenous ATP via activation of P2X3 and P2X2/3 receptors contributes to inflammatory nociception in different models, including the formalin injected in subcutaneous tissue of the rat's hind paw. In this study, we have evaluated whether TRPA1, 5-HT3 and 5-HT1A receptors, whose activation is essential to formalin-induced inflammatory nociception, are involved in the nociception induced by activation of P2X3 receptors on subcutaneous tissue of the rat's hind paw. We have also evaluated whether the activation of P2X3 receptors increases the susceptibility of primary afferent neurons to formalin action modulated by activation of TRPA1, 5-HT3 or 5-HT1A receptors. Nociceptive response intensity was measured by observing the rat's behavior and considering the number of times the animal reflexively raised its hind paw (flinches) in 60min. Local subcutaneous administration of the selective TRPA1, 5-HT3 or 5-HT1A receptor antagonists HC 030031, tropisetron and WAY 100,135, respectively, prevented the nociceptive responses induced by the administration in the same site of the non-selective P2X3 receptor agonist αβmeATP. Administration of the selective P2X3 and P2X2/3 receptor antagonist A-317491 or pretreatment with oligonucleotides antisense against P2X3 receptor prevented the formalin-induced behavioral nociceptive responses during the first and second phases. Also, the co-administration of a subthreshold dose of αβmeATP with a subthreshold dose of formalin induced nociceptive behavior, which was prevented by local administration of tropisetron, HC 030031 or WAY 100, 135. These findings have demonstrated that the activation of P2X3 receptors induces inflammatory nociception modulated by TRPA1, 5-HT3 and 5-HT1A receptors. Also, they suggest that inflammatory nociception is modulated by the release of endogenous ATP and P2X3 receptor activation, which in turn, increases primary afferent nociceptor susceptibility to the action of inflammatory mediators via interaction with TRPA1, 5-HT3 and 5-HT1A receptors in the peripheral tissue.
- Pharmacology, biochemistry, and behavior.Pharmacol Biochem Behav.2013 Nov;112:49-55. doi: 10.1016/j.pbb.2013.09.017. Epub 2013 Oct 9.
- It has been described that endogenous ATP via activation of P2X3 and P2X2/3 receptors contributes to inflammatory nociception in different models, including the formalin injected in subcutaneous tissue of the rat's hind paw. In this study, we have evaluated whether TRPA1, 5-HT3 and 5-HT1A receptors,
- PMID 24120766
- Endogenously released 5-HT inhibits A and C fiber-evoked synaptic transmission in the rat spinal cord by the facilitation of GABA/glycine and 5-HT release via 5-HT2A and 5-HT3 receptors
- Iwasaki Takeyuki,Otsuguro Ken-ichi,Kobayashi Takeshi,Ohta Toshio,Ito Shigeo
- European Journal of Pharmacology 702(1-3), 149-157, 2013-02-28
- … The pCA-mediated inhibition was reversed by ketanserin (a 5-HT2A receptor antagonist) and tropisetron (a 5-HT3 receptor antagonist). … in this case, the actions of 5-HT were antagonized by ketanserin, but not by tropisetron. … Furthermore, ketanserin inhibited the pCA-evoked release of gamma-aminobutyric acid (GABA) and glycine, while tropisetron inhibited the pCA-evoked release of 5-HT. …
- NAID 120005228705
- Antiemetic prophylaxis in thyroid surgery : a randomized, double-blind comparison of three 5-HT_3 agents
- METAXARI Maria,PAPAIOANNOU Alexandra,PETROU Anastasios,CHATZIMICHALI Aikaterini,PHARMAKALIDOU Elena,ASKITOPOULOU Helen
- Journal of anesthesia 25(3), 356-362, 2011-06-20
- NAID 10029022996
- Changes in Characteristics of the Specific Binding of [^3H]LY-278584, a 5-HT_3-Receptor Antagonist, on Differentiated NG108-15 Cells
- Matsushima Kayoko,Imanishi Takashi,Asano Hajime [他],FUNAKAMI Yoshinori,WADA Tetsuyuki,ICHIDA Seiji
- Journal of pharmacological sciences 113(3), 281-284, 2010-07-20
- … The binding was significantly inhibited by 10 nM tropisetron, a specific 5-HT<SUB>3</SUB>–receptor antagonist, but not by any other types of 5-HT–receptor antagonists. …
- NAID 10029889466
- 企業系リソース (薬価情報含む) トロピセトロン - QLifeお薬検索 - QLife. Inc. トロピセトロン - 医薬品情報・検索 イ－ファ－マ - Allied Medical Associates Co., Ltd. 管理系リソース tropisetron - 規制物質法(CSA) - DEA, アメリカ合衆国
- 制吐薬 一般名：塩酸トロピセトロン [5-HT 3 受容体拮抗薬] 作用機序 求心性迷走神経終末部の5-HT3受容体でセロトニンと競合的に働いて悪心・嘔吐を抑える。 効能・用途 抗ガン剤（シスプラチンなど）投与に伴う悪心。嘔吐に用いる。
- serotonin receptor
- 5-HT3受容体はリガンドの結合により開閉してNa+, K+の等価に関わる。ニコチン性受容体に似ている。(GOO.299)
- somatodendritic 5-HT1A autoreceptors descrease raphe cell fireing when activated by 5-HT released from axon collaterals of the same or adjacent neurons. (GOO.301)
- 塩酸トロピセトロン tropisetron hydrochloride