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{{Infobox drug | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 407376289 | image = Gadoteric acid.png | width = | alt = | caption = | USAN = Gadoterate meglumine（钆特酸葡胺） <!-- Clinical data --> | pronounce = | tradename = Artirem, Dotarem（多它灵）, Clariscan等<ref name = "造影剂">{{cite web | title=Gadoteric Acid International | website=Drugs.com | date=6 January 2021 | url=https://www.drugs.com/international/gadoteric-acid.html | access-date=21 January 2021 | archive-date=2019-08-17 | archive-url=https://web.archive.org/web/20190817103910/https://www.drugs.com/international/gadoteric-acid.html | dead-url=no }}</ref> | MedlinePlus = | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | pregnancy_AU_comment = | pregnancy_category = | routes_of_administration = [[静脉注射]] | class = | ATC_prefix = V08 | ATC_suffix = CA02 | ATC_supplemental = <!-- Legal status --> | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled --> | legal_AU_comment = | legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F --> | legal_BR_comment = | legal_CA = Rx-only | legal_CA_comment = | legal_UK = POM | legal_UK_comment = | legal_US = Rx-only | legal_US_comment = | legal_UN = <!-- N I, II, III, IV / P I, II, III, IV --> | legal_UN_comment = | legal_CN = 处方药 | legal_status = Rx-only <!-- Pharmacokinetic data --> | bioavailability = | protein_bound = 几乎无 | metabolism = 几乎无 | metabolites = | onset = | elimination_half-life = 约90分钟（血浆）<br>2-3分钟（分布） | duration_of_action = | excretion = 原体药物经[[腎]]，极少部分经粪便排出 <!-- Identifiers --> | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 72573-82-1 | CAS_supplemental = | PubChem = 158536 | IUPHAR_ligand = | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB09132 | ChemSpiderID = 139460 | UNII_Ref = {{fdacite|changed|FDA}} | UNII = QVF9Y6955W | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08007 | ChEBI = 73732 | ChEMBL = 3833326 | NIAID_ChemDB = | PDB_ligand = | synonyms = DOTA-Gd，Gd-DOTA <!-- Chemical and physical data --> | IUPAC_name = gadolinium(3+) 2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetate<br>2-[4,7,10-三(羧甲基)-1,4,7,10-四氮杂环十二-1-基]乙酸钆（III） | C=16 | H=25 | Gd=1 | N=4 | O=8 | SMILES = [Gd+3].OC(=O)CN1CCN(CC([O-])=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC1 | StdInChI = 1S/C16H28N4O8.Gd/c21-13(22)9-17-1-2-18(10-14(23)24)5-6-20(12-16(27)28)8-7-19(4-3-17)11-15(25)26;/h1-12H2,(H,21,22)(H,23,24)(H,25,26)(H,27,28);/q;+3/p-3 | StdInChI_comment = | StdInChIKey = GFSTXYOTEVLASN-UHFFFAOYSA-K | density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }} '''钆特酸'''（[[INN]]：gadoteric acid，简写Ga-DOTA），为钆离子(Ga<sup>3+</sup>)的大环配体[[DOTA (螯合剂)|DOTA]]形成的[[螯合物]]。在医学上是一种钆造影剂(gadolinium-based contrast agents，GBCA)，属大环离子型造影剂，用于[[磁共振成像]]造影<ref name= "造影剂书">{{cite book |author1=何国祥 |author2=王毅翔 |title=造影剂药理学及临床应用 |date=2002 |publisher=上海科学技术出版社 |location=上海 |isbn=7532362264}}</ref>。其动力学稳定常数<math>lgK = 25.6</math>，是已知稳定常数和解离半衰期最大的螯合物<ref>{{cite journal |author1=P Caravan, JJ Ellison, TJ McMurry, RB Lauffer |title=Gadolinium (III) chelates as MRI contrast agents: structure, dynamics, and applications |journal=Chemical Reviews |date=1999 |volume=99 |pages=2293−2352 |doi=10.1021/cr980440x}}</ref><ref>{{cite journal |author1=Herborn, Christoph U. MD; Honold, Elmar MD; Wolf, Michael; Kemper, Jörn MD; Kinner, Sonja MD; Adam, Gerhard MD; Barkhausen, Jörg MD|title=Clinical Safety and Diagnostic Value of the Gadolinium Chelate Gadoterate Meglumine (Gd-DOTA) |url=https://archive.org/details/sim_investigative-radiology_2007-01_42_1/page/58|journal=Investigative Radiology |date=2007 |volume=42 |issue=1 |pages=58-62 |doi=10.1097/01.rli.0000248893.01067.e5}}</ref>。 医学上常以其葡甲胺盐的形式，即钆特酸葡胺（[[美国采用名称|USAN]]：Gadoterate meglumine）进行注射给药<ref name="Dotarem FDA label">{{cite web | title=Dotarem- gadoterate meglumine injection | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e2c4a5ac-2df2-4cf4-a2d3-6fbe2d898ebc | access-date=29 August 2021 | archive-date=2024-12-06 | archive-url=https://web.archive.org/web/20241206091934/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e2c4a5ac-2df2-4cf4-a2d3-6fbe2d898ebc | dead-url=no }}</ref><ref name="Clariscan FDA label">{{cite web | title=Clariscan- gadoterate meglumine injection, solution | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6f8c9fac-c995-4bf4-950d-ab89deb291b5 | access-date=29 August 2021 | archive-date=2024-12-12 | archive-url=https://web.archive.org/web/20241212002954/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6f8c9fac-c995-4bf4-950d-ab89deb291b5 | dead-url=no }}</ref>。 == 历史 == [[File:گادلیم.jpg|150px|thumb|Dotarem注射液]] 钆特酸由法国加柏公司(Guerbet)研制开发，以商品名Dotarem(多它灵)于1989年获准在法国上市，2013年3月20日通过美国[[美国食品药品监督管理局|FDA]]批准用于MRI造影<ref name=Fierce2014>{{cite news|last1=Hollmer|first1=Mark|name-list-style=vanc|title=Dotarem: A safe(r) gadolinium-based contrast imaging agent|url=http://www.fiercebiotech.com/special-report/dotarem-a-safe-r-gadolinium-based-contrast-imaging-agent|work=FierceBiotech|date=6 January 2014|accessdate=2024-06-25|archive-date=2021-08-21|archive-url=https://web.archive.org/web/20210821200157/https://www.fiercebiotech.com/special-report/dotarem-a-safe-r-gadolinium-based-contrast-imaging-agent|dead-url=no}}</ref>。 同时也是继1982年第一个MRI造影剂[[马根维显]]（钆喷酸，Gd-DPTA）问世后的第二个MRI造影剂<ref name= "造影剂书"/>。 == 医学用途 == 钆特酸中心离子Ga<sup>3+</sup>具有强[[順磁性|顺磁性]]，可缩短磁共振（MRI）中T<sub>1</sub>弛豫时间，形成像衬度，为阳性造影剂。但高浓度下T<sub>2</sub>弛豫时间缩短占优为阴性造影剂，高浓度常用于动脉期血管造影<ref name= "造影剂书"/>。 其被批准用于2岁以上患者的全身MRI检查，可用于大脑、脊髓以及血管检查。其本身无法透过血脑屏障，但大脑血管发生病变部分则可透过血脑屏障，因此可识别脑部肿瘤<ref name=>{{Cite web|date=22 August 2016|editor-last=DrugBank|title=Gadoteric acid|url=http://www.drugbank.ca/drugs/DB09132|website=DrugBank|access-date=2024-06-25|archive-date=2019-08-17|archive-url=https://web.archive.org/web/20190817103919/https://www.drugbank.ca/drugs/DB09132|dead-url=no}}</ref>。其以钆特酸葡胺注射液形式进行静脉注射，药物可在身体中存在数年<ref name="Dotarem FDA label"/><ref name="Clariscan FDA label"/>。 == 药理学 == 钆特酸和第一代MRI造影剂马根维显理化性能和临床应用相似。经静脉注射后，钆特酸先经血管扩散，然后迅速扩散细胞外空间。钆特酸通过肾脏以原体药物排泄，少部分分泌到肠胃道经粪便排出。钆特酸非选择性地分布在所有脑外组织的细胞外空间中，无器官特异性。钆特酸蛋白质结合力非常低因此通过肾脏相对较快地排泄。<ref name= "造影剂书"/> == 风险 == 钆特酸作为含钆制剂，体外研究表明其具有的神经毒性，但相比于线性钆螯合物，作为大环螯合物的钆特酸相比风险更低<ref>{{cite journal | title=Gadolinium-Based MRI Contrast Agents Induce Mitochondrial Toxicity and Cell Death in Human Neurons, and Toxicity Increases With Reduced Kinetic Stability of the Agent | vauthors=Bower DV, Richter JK, von Tengg-Kobligk H, Heverhagen JT, Runge VM | volume=54 | journal=Investigative Radiology | number=8 | date=August 2019 | pmid=31265439 | doi=10.1097/RLI.0000000000000567 | pages=453–463 | s2cid=164486744 | url=https://boris.unibe.ch/132314/ | access-date=2024-06-25 | archive-date=2024-12-13 | archive-url=https://web.archive.org/web/20241213142033/https://boris.unibe.ch/132314/ | dead-url=no }}</ref><ref>{{cite journal |author1=Alexander Radbruch , Lukas D. Weberling, Pascal J. Kieslich, Oliver Eidel, Sina Burth, Philipp Kickingereder, Sabine Heiland, Wolfgang Wick, Heinz-Peter Schlemmer, Martin Bendszus |title=Gadolinium Retention in the Dentate Nucleus and Globus Pallidus Is Dependent on the Class of Contrast Agent |journal=RADIOLOG |date=2015 |volume=275 |issue=3 |pages=783-791 |doi=10.1148/radiol.2015150337}}</ref>。在标准用量下，在大脑可检测到药物残留<ref>{{cite journal | title=Brain tissue gadolinium retention in pediatric patients after contrast-enhanced magnetic resonance exams: pathological confirmation | vauthors = Stanescu AL, Shaw DW, Murata N, Murata K, Rutledge JC, Maloney E, Maravilla KR | display-authors = 6 | volume=50 | journal=Pediatric Radiology | number=3 | date=March 2020 | pmid=31989188 | doi=10.1007/s00247-019-04535-w | pages=388–396 | s2cid=210913930}}</ref>。 同时具有肾源性系统纤维化(Nephrogenic systemic fibros,NSF)风险，但目前未有相关案例报道，因此不适用于肾功能受损患者<ref>{{cite journal | vauthors=Todd DJ, Kay J | date=2016 | title=Gadolinium-Induced Fibrosis | journal=Annual Review of Medicine | volume=67 | pages=273–91 | doi=10.1146/annurev-med-063014-124936 | pmid=26768242}}</ref><ref>{{cite journal |author1=Csilla Balassy, Donna Roberts, Stephen F. Miller3 |title=Safety and efficacy of gadoteric acid in pediatric magnetic resonance imaging: overview of clinical trials and post-marketing studies |journal=Pediatr Radiol |date=2015 |volume=45 |pages=1831-1841 |doi=10.1007/s00247-015-3394-9}}</ref>。 ==合成== 由[[DOTA (螯合剂)|DOTA]]与[[氢氧化钆]]先在80摄氏度螯合12小时，再用氨水室温下碱化使pH=11即得到钆特酸Ga-DOTA。 :[[file:Tetraxetan structure.svg|120px]]+ Ga(OH)<sub>3</sub> →[[file:Gadoteric acid.png|110px]]+3H<sub>2</sub>O 钆特酸进一步与[[葡萄糖]]和[[甲胺]]还原胺化得到的葡甲胺1：1混合成盐，即可得到钆特酸葡胺<ref>{{cite journal |author1=S KauráLuthra, V MorissonáIveson, NE Felicity, J Nicholas |title=Gd 3+ cFLFLFK conjugate for MRI: a targeted contrast agent for FPR1 in inflammation |journal=Chemical communications |date=2013 |volume=49 |issue=6 |pages=564-566 |doi=10.1039/C2CC37460A}}</ref><ref>{{cite journal |author1=韩晓丹,郭春 |title=钆特酸葡甲胺 |journal=中国药物化学杂志 |date=2013 |volume=23 |issue=5 |page=1 |url=https://www.cnki.com.cn/Article/CJFDTotal-ZGYH201305019.htm}}</ref>。 :[[file:Glucose chain structure.svg|120px]]（葡萄糖）+[[file:CH3-NH2.svg|60px]]<math> \xrightarrow{\mathrm{H_2, Ru}} </math>[[file:Meglumine.svg|120px]]（葡甲胺） ：[[file:Gadoteric acid.png|110px]]+[[file:Meglumine.svg|120px]]→[[file:Gadoteric acid.png|110px]]· [[file:N-Methyl-D-glucamin2.svg|60px]]（钆特酸葡胺） [[File:Fig3-Images-of-spinal-angiography-with-gadoterate-meglumine-at-the-level-of-3rd6th-thoracic-vertebra-conducted-7days-aft.jpg|150px|thumb|钆特酸的葡甲胺盐(钆特酸葡胺)进行脊髓MRI造影]] ==参考文献== {{reflist}} {{Contrast media |state=collapsed}} [[Category:造影剂]] [[category:钆化合物]]
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