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Tezampanel (anhydrous)

NMR下載 COA and HPLC MSDS下載
names：
(3S,4aR,6R,8aR)-6-(2-(1H-tetrazol-5-yl)ethyl)decahydroisoquinoline-3-carboxylic acid
CAS號：
154652-83-2
MDL Number：
MF(分子式)： C13H21N5O2 MW(分子量)： 279.344
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	(3S,4aR,6R,8aR)-6-(2-(1H-tetrazol-5-yl)ethyl)decahydroisoquinoline-3-carboxylic acid
英文別名	LY 293558; LY-293558; LY293558; NGX-424; NGX 424; NGX424; Tezampanel
CAS號	154652-83-2
Inchi	InChI=1S/C13H21N5O2/c19-13(20)11-6-10-5-8(1-3-9(10)7-14-11)2-4-12-15-17-18-16-12/h8-11,14H,1-7H2,(H,19,20)(H,15,16,17,18)/t8-,9+,10-,11+/m1/s1
InchiKey	ZXFRFPSZAKNPQQ-YTWAJWBKSA-N
分子式 Formula	C13H21N5O2
分子量 Molecular Weight	279.344
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	Tezampanel (anhydrous)(CAS:154652-83-2 ):僅限應(yīng)用于工業(yè)或者科學研究過程中非醫(yī)療目的，不應(yīng)用于人類或動物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	Tezampanel, also known as LY 293558 and NGX-424, is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective and anticonvulsant properties, the former of which may, at least in part, occur via blockade of calcium uptake into neurons. Tezampanel has a range of effects which may be useful for medicinal purposes, as well as its applications in scientific research. It suppresses both the withdrawal symptoms from morphine and other opioids, and the development of tolerance, as well as having antihyperalgesic and analgesic effects in its own right..
Application1
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警示圖
危險性	Warning
危險性警示
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[1]Miller SL, Aroniadou-Anderjaska V, Figueiredo TH, Prager EM, Almeida-Suhett CP, Apland JP, Braga MF. A rat model of nerve agent exposure applicable to the pediatric population: The anticonvulsant efficacies of atropine and GluK1 antagonists. Toxicol Appl Pharmacol. 2015 Apr 15;284(2):204-16. doi: 10.1016/j.taap.2015.02.008. Epub 2015 Feb 15. PubMed PMID: 25689173; PubMed Central PMCID: PMC4545593.

[2]Prager EM, Figueiredo TH, Long RP 2nd, Aroniadou-Anderjaska V, Apland JP, Braga MF. LY293558 prevents soman-induced pathophysiological alterations in the basolateral amygdala and the development of anxiety. Neuropharmacology. 2015 Feb;89:11-8. doi: 10.1016/j.neuropharm.2014.08.014. Epub 2014 Sep 6. PubMed PMID: 25204221; PubMed Central PMCID: PMC4250288.

[3] Chan K, MaassenVanDenBrink A. Glutamate receptor antagonists in the management of migraine. Drugs. 2014 Jul;74(11):1165-76. doi: 10.1007/s40265-014-0262-0. Review. PubMed PMID: 25030431.

[4] Moshiri M, Darchini-Maragheh E, Balali-Mood M. Advances in toxicology and medical treatment of chemical warfare nerve agents. Daru. 2012 Nov 28;20(1):81. doi: 10.1186/2008-2231-20-81. PubMed PMID: 23351280; PubMed Central PMCID: PMC3556041.

[5] Wallace MS, Lam V, Schettler J. NGX426, an oral AMPA-kainate antagonist, is effective in human capsaicin-induced pain and hyperalgesia. Pain Med. 2012 Dec;13(12):1601-10. doi: 10.1111/j.1526-4637.2012.01509.x. Epub 2012 Oct 30. PubMed PMID: 23110368.

6: Apland JP, Aroniadou-Anderjaska V, Figueiredo TH, Green CE, Swezey R, Yang C, Qashu F, Braga MF. Efficacy of the GluK1/AMPA receptor antagonist LY293558 against seizures and neuropathology in a soman-exposure model without pretreatment and its pharmacokinetics after intramuscular administration. J Pharmacol Exp Ther. 2013 Jan;344(1):133-40. doi: 10.1124/jpet.112.198689. Epub 2012 Oct 5. PubMed PMID: 23042954; PubMed Central PMCID: PMC3533413.7: Lionetto L, Negro A, Palmisani S, Gentile G, Del Fiore MR, Mercieri M, Simmaco M, Smith T, Al-Kaisy A, Arcioni R, Martelletti P. Emerging treatment for chronic migraine and refractory chronic migraine. Expert Opin Emerg Drugs. 2012 Sep;17(3):393-406. doi: 10.1517/14728214.2012.709846. Epub 2012 Aug 3. Review. PubMed PMID: 22862686.8: Moon MJ, Kim HY, Park S, Kim DK, Cho EB, Hwang JI, Seong JY. Insulin contributes to fine-tuning of the pancreatic beta-cell response to glucagon-like peptide-1. Mol Cells. 2011 Oct;32(4):389-95. doi: 10.1007/s10059-011-0157-9. Epub 2011 Sep 7. PubMed PMID: 21904878; PubMed Central PMCID: PMC3887647.9: Oshiro M, Hefferan MP, Kakinohana O, Lukacova N, Sugahara K, Yaksh TL, Marsala M. Suppression of stretch reflex activity after spinal or systemic treatment with AMPA receptor antagonist NGX424 in rats with developed baclofen tolerance. Br J Pharmacol. 2010 Nov;161(5):976-85. doi: 10.1111/j.1476-5381.2010.00954.x. PubMed PMID: 20977450; PubMed Central PMCID: PMC2998680.10: Figueiredo TH, Qashu F, Apland JP, Aroniadou-Anderjaska V, Souza AP, Braga MF. The GluK1 (GluR5) Kainate/{alpha}-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist LY293558 reduces soman-induced seizures and neuropathology. J Pharmacol Exp Ther. 2011 Feb;336(2):303-12. doi: 10.1124/jpet.110.171835. Epub 2010 Oct 20. PubMed PMID: 20962029; PubMed Central PMCID: PMC3033714.1

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