Baclofen (BioDeep_00000001426)
Secondary id: BioDeep_00000016555, BioDeep_00001868423
human metabolite PANOMIX_OTCML-2023 blood metabolite natural product
代谢物信息卡片
化学式: C10H12ClNO2 (213.0557)
中文名称: (R)-巴氯芬(mM/ml), 巴氯酚, 巴氯芬
谱图信息:
最多检出来源 Homo sapiens(otcml) 13.87%
分子结构信息
SMILES: C1=CC(=CC=C1C(CC(=O)O)CN)Cl
InChI: InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)
描述信息
Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant. Baclofen stimulates GABA-B receptors leading to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury. It appears to act primarily at the spinal cord level by inhibiting spinal polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways.
M - Musculo-skeletal system > M03 - Muscle relaxants > M03B - Muscle relaxants, centrally acting agents
D018377 - Neurotransmitter Agents > D018682 - GABA Agents > D018755 - GABA Agonists
D018373 - Peripheral Nervous System Agents > D009465 - Neuromuscular Agents
C78281 - Agent Affecting Musculoskeletal System > C29696 - Muscle Relaxant
D002491 - Central Nervous System Agents
(R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist[1].
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
同义名列表
97 个代谢物同义名
beta-(Aminomethyl)-4-chlorobenzenepropanoic acid; b-(Aminomethyl)-4-chlorobenzenepropanoic acid; beta-(p-Chlorophenyl)-gamma-aminobutyric acid; beta-(Aminomethyl)-p-chlorohydrocinnamic acid; gamma-Amino-beta-(p-chlorophenyl)butyric acid; Β-(aminomethyl)-4-chlorobenzenepropanoic acid; beta-(Aminomethyl)-4-chlorobenzenepropanoate; Β-(aminomethyl)-p-chlorohydrocinnamic acid; b-(Aminomethyl)-p-chlorohydrocinnamic acid; beta-(Aminomethyl)-p-chlorohydrocinnamate; b-(Aminomethyl)-4-chlorobenzenepropanoate; gamma-Amino-beta-(p-chlorophenyl)butyrate; beta-(p-Chlorophenyl)-gamma-aminobutyrate; Β-(aminomethyl)-4-chlorobenzenepropanoate; DL-4-Amino-3-p-chlorophenylbutanoic acid; 4-amino-3-(4-chlorophenyl)butanoic acid; g-Amino-b-(p-chlorophenyl)butyric acid; Γ-amino-β-(p-chlorophenyl)butyric acid; Β-(p-chlorophenyl)-γ-aminobutyric acid; 4-Amino-3-(4-chlorophenyl)butyric acid; Β-(aminomethyl)-p-chlorohydrocinnamate; b-(p-Chlorophenyl)-g-aminobutyric acid; b-(Aminomethyl)-p-chlorohydrocinnamate; DL-4-Amino-3-p-chlorophenylbutanoate; g-Amino-b-(p-chlorophenyl)butyrate; 4-Amino-3-(4-chlorophenyl)butyrate; b-(p-Chlorophenyl)-g-aminobutyrate; Γ-amino-β-(p-chlorophenyl)butyrate; Β-(p-chlorophenyl)-γ-aminobutyrate; Pharmascience brand OF baclofen; ASTA medica brand OF baclofen; Alphapharm brand OF baclofen; Ciba-geigy brand OF baclofen; Ciba geigy brand OF baclofen; Baclofen pharmascience brand; Medtronic brand OF baclofen; Ashbourne brand OF baclofen; Nu pharm brand OF baclofen; Nu-pharm brand OF baclofen; Novartis brand OF baclofen; Baclofen ciba-geigy brand; Baclofen alphapharm brand; beta-(4-Chlorophenyl)gaba; Athena brand OF baclofen; Baclofen medtronic brand; Baclofen ashbourne brand; Apotex brand OF baclofen; Baclofen nu-pharm brand; Baclofen novartis brand; Irex brand OF baclofen; Isis brand OF baclofen; b-(4-Chlorophenyl)gaba; Β-(4-chlorophenyl)gaba; Baclofen apotex brand; Baclofen athena brand; Baclofen isis brand; Baclofen irex brand; GABA, chlorophenyl; Chlorophenyl gaba; CIBA-34,647-ba; Baclofène-irex; Baclofène irex; AWD, baclofen; BaclofèneIrex; (+-)-Baclofen; CIBA34,647ba; Gen-baclofen; PMS Baclofen; Baclofen awd; apo-Baclofen; Gen baclofen; apo Baclofen; PMS-Baclofen; (R)-Baclofen; ApoBaclofen; GenBaclofen; PMSBaclofen; DL-Baclofen; Arbaclofen; Baclofenum; Baclofene; Baclophen; Baclospas; Baclofeno; Nu baclo; PCP-GABA; Genpharm; Baclofen; Lioresal; Nu-baclo; Atrofen; Kemstro; NuBaclo; Clofen; Lebic; STX209; Baclofen
数据库引用编号
22 个数据库交叉引用编号
- ChEBI: CHEBI:190735
- ChEBI: CHEBI:2972
- KEGG: C21605
- KEGGdrug: D09791
- PubChem: 44602
- PubChem: 2284
- HMDB: HMDB0014327
- DrugBank: DB00181
- DrugBank: DB08891
- ChEMBL: CHEMBL301742
- ChEMBL: CHEMBL701
- Wikipedia: Baclofen
- MeSH: Baclofen
- chemspider: 2197
- CAS: 69308-37-8
- CAS: 1134-47-0
- PMhub: MS000000491
- PubChem: 340125663
- PDB-CCD: 2C0
- medchemexpress: HY-17354
- medchemexpress: HY-B0007
- LOTUS: LTS0169480
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
6 个相关的物种来源信息
- 2 - Bacteria: LTS0169480
- 9606 - Homo sapiens: -
- 1883 - Streptomyces: LTS0169480
- 1944 - Streptomyces halstedii: LTS0169480
- 1944 - Streptomyces halstedii: NA
- 2062 - Streptomycetaceae: LTS0169480
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有:
- PubMed: 来源于PubMed文献库中的文献信息,我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表,这个列表按照代谢物同时出现的文献数量降序排序,取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘,得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序,取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中,存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称,可以跳转到相关代谢物的信息页面。
文献列表
- Xiaoju Liu, Haijuan Wang, Xiaoyu Wang, Yinxia Ning, Wei Liu, Jie Gao. Baixiangdan capsule and Shuyu capsule regulate anger-out and anger-in, respectively: GB1-mediated GABA can regulate 5-HT levels in multiple brain regions.
Aging.
2023 Mar; 15(6):2046-2065. doi:
10.18632/aging.204589
. [PMID: 36988497] - Thomas John Pisano, Jessica Ace, Beverly Hon. Transient alteration of consciousness in spinal cord injury secondary to Baclofen use: a case report.
Spinal cord series and cases.
2022 05; 8(1):56. doi:
10.1038/s41394-022-00511-z
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Forensic science international.
2022 May; 334(?):111246. doi:
10.1016/j.forsciint.2022.111246
. [PMID: 35276541] - Bryan VanDreese, Ashley Holland, Andrew Murray. Chronic Phenibut Use: Symptoms, Severe Withdrawal, and Recovery.
WMJ : official publication of the State Medical Society of Wisconsin.
2022 Apr; 121(1):E1-E4. doi:
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Neuroscience letters.
2022 03; 773(?):136481. doi:
10.1016/j.neulet.2022.136481
. [PMID: 35104617] - Steven E Epstein, Kate Hopper, Kate S Farrell. Manual plasma exchange to treat an accidental overdose of intravenous lipid emulsion in a dog with baclofen toxicosis.
Journal of the American Veterinary Medical Association.
2022 01; 260(6):650-656. doi:
10.2460/javma.21.03.0152
. [PMID: 35066487] - Resha Khanal, Sharad Oli, Janet Chan Gomez, Sahar Tahir, Binita Bhandari, Saketram Komanduri. Severe Case of Oral Baclofen Withdrawal Resulting in Mechanical Ventilation.
Journal of investigative medicine high impact case reports.
2022 Jan; 10(?):23247096211060584. doi:
10.1177/23247096211060584
. [PMID: 35356848] - Tzu-Yu Lin, Cheng-Wei Lu, Pei-Wen Hsieh, Kuan-Ming Chiu, Ming-Yi Lee, Su-Jane Wang. Natural Product Isoliquiritigenin Activates GABAB Receptors to Decrease Voltage-Gate Ca2+ Channels and Glutamate Release in Rat Cerebrocortical Nerve Terminals.
Biomolecules.
2021 10; 11(10):. doi:
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Kidney international.
2021 10; 100(4):720-736. doi:
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American journal of kidney diseases : the official journal of the National Kidney Foundation.
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Cell reports.
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2021 Mar; 248(?):119165. doi:
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Respiratory investigation.
2021 Mar; 59(2):263-265. doi:
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Journal of pharmaceutical sciences.
2021 03; 110(3):1227-1239. doi:
10.1016/j.xphs.2020.10.025
. [PMID: 33069710] - Vincent R Lee, Rachel M Shively, Michael K Connolly, Robert S Hoffman, Joshua Nogar. Removal of baclofen with hemodialysis is negligible compared to intact kidney excretion in a pediatric overdose: a case report.
Clinical toxicology (Philadelphia, Pa.).
2021 Mar; 59(3):231-234. doi:
10.1080/15563650.2020.1795188
. [PMID: 32734785] - Victor Echeverry-Alzate, Jérôme Jeanblanc, Pierre Sauton, Vanessa Bloch, Laurence Labat, Marion Soichot, Florence Vorspan, Mickael Naassila. Is R(+)-Baclofen the best option for the future of Baclofen in alcohol dependence pharmacotherapy? Insights from the preclinical side.
Addiction biology.
2021 03; 26(2):e12892. doi:
10.1111/adb.12892
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Molecular psychiatry.
2021 02; 26(2):545-555. doi:
10.1038/s41380-018-0287-y
. [PMID: 30382188] - Mingheng Li, Yan Huang, Rongchun Chen, Ning Liu, Shibing Fang. Efficacy and safety of tolperisone versus baclofen among Chinese patients with spasticity associated with spinal cord injury: a non-randomized retrospective study.
Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas.
2021; 54(11):e11293. doi:
10.1590/1414-431x2021e11293
. [PMID: 34495247] - Marion Brunet, Maxime Léger, Pierre-André Billat, Bénédicte Lelièvre, Nicolas Lerolle, David Boels, Gaël Le Roux. Baclofen self-poisoning: Is renal replacement therapy efficient in patient with normal kidney function?.
Anaesthesia, critical care & pain medicine.
2020 12; 39(6):813-817. doi:
10.1016/j.accpm.2020.07.021
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Forensic science international.
2020 Nov; 316(?):110541. doi:
10.1016/j.forsciint.2020.110541
. [PMID: 33096455] - Sayna Norouzi, Samira S Farouk, Matthew A Sparks. Back off baclofen when the kidneys don't work.
Kidney international.
2020 10; 98(4):829-831. doi:
10.1016/j.kint.2020.05.026
. [PMID: 32998812] - Kianna J Chauvin, Peter G Blake, Amit X Garg, Matthew A Weir, Lavanya Bathini, Stephanie N Dixon, Eric McArthur, Jessica M Sontrop, Louise Moist, Richard B Kim, Flory T Muanda. Baclofen has a risk of encephalopathy in older adults receiving dialysis.
Kidney international.
2020 10; 98(4):979-988. doi:
10.1016/j.kint.2020.04.047
. [PMID: 32450156] - Minseon Cheong, Jongmin Lee, Tae Yeon Lee, Soon Bae Kim. Prevalence and risk factors of baclofen neurotoxicity in patients with severely impaired renal function.
Nefrologia.
2020 Sep; 40(5):543-551. doi:
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Medicine.
2020 Aug; 99(32):e21634. doi:
10.1097/md.0000000000021634
. [PMID: 32769929] - Mohamed Ibrahim, Hatem A Sarhan, Youssef W Naguib, Hamdy Abdelkader. Design, characterization and in vivo evaluation of modified release baclofen floating coated beads.
International journal of pharmaceutics.
2020 May; 582(?):119344. doi:
10.1016/j.ijpharm.2020.119344
. [PMID: 32315750] - Justin Gold, Kevin Zhao, Mickey Abraham, Rosemary Behmer Hansen, Meeki Lad, Antonios Mammis. Encephalopathy of Unknown Origin in a Baclofen Patient: Case Report and Review of the Literature.
World neurosurgery.
2020 Apr; 136(?):136-139. doi:
10.1016/j.wneu.2020.01.044
. [PMID: 31954899] - Shahram Ala, Mina Alvandipour, Majid Saeedi, Mohaddeseh Mansourifar, Mahila Monajati, Afshin Shiva. Effect of Topical Baclofen 5\% on Post-Hemorrhoidectomy Pain: Randomized Double Blind Placebo-Controlled Clinical Trial.
Journal of gastrointestinal surgery : official journal of the Society for Surgery of the Alimentary Tract.
2020 02; 24(2):405-410. doi:
10.1007/s11605-019-04147-7
. [PMID: 30783957] - Qingfeng He, Yashpal S Chhonker, Matthew J McLaughlin, Daryl J Murry. Simultaneous Quantitation of S(+)- and R(-)-Baclofen and Its Metabolite in Human Plasma and Cerebrospinal Fluid using LC-APCI-MS/MS: An Application for Clinical Studies.
Molecules (Basel, Switzerland).
2020 Jan; 25(2):. doi:
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. [PMID: 31936209] - Sruthi P Thomas, Christina K Hardesty, Kristin A Buxton, Andrew B Collins, Jessica Pruente, Kelly L D Pham, Jordan Sheriko, M Elise McClanahan, Didem Inanoglu, Rajashree Srinivasan, Laura Ridnour, Robert Cooper, Seema Khurana, The Pediatric Itb Network. Pediatric intrathecal baclofen management during the COVID-19 pandemic in the US and Canada.
Journal of pediatric rehabilitation medicine.
2020 ; 13(3):379-384. doi:
10.3233/prm-200755
. [PMID: 33164962] - Giovanni D'Orazio, Chiara Fanali, Alessandra Gentili, Franco Tagliaro, Salvatore Fanali. Nano-liquid chromatography for enantiomers separation of baclofen by using vancomycin silica stationary phase.
Journal of chromatography. A.
2019 Nov; 1605(?):360358. doi:
10.1016/j.chroma.2019.07.012
. [PMID: 31337499] - Tobie D Lee, Olivia W Lee, Kyle R Brimacombe, Lu Chen, Rajarshi Guha, Sabrina Lusvarghi, Bethilehem G Tebase, Carleen Klumpp-Thomas, Robert W Robey, Suresh V Ambudkar, Min Shen, Michael M Gottesman, Matthew D Hall. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology.
2019 11; 96(5):629-640. doi:
10.1124/mol.119.115964
. [PMID: 31515284] - C de Marcellus, S le Bot, X Decleves, F Baud, S Renolleau, M Oualha. Report of severe accidental baclofen intoxication in a healthy 4-year-old boy and review of the literature.
Archives de pediatrie : organe officiel de la Societe francaise de pediatrie.
2019 Nov; 26(8):475-478. doi:
10.1016/j.arcped.2019.10.003
. [PMID: 31685412] - Thotalampatti Pachiyappan Jeyaselvasenthilkumar, Deiveegan Kunjithapatham, Sekar Chinnasamy, Mohamed Abith Ali. Baclofen-induced Coma and Respiratory Depression in a Patient with Cervical Spondylotic Myelopathy with Chronic Kidney Disease.
Neurology India.
2019 Jul; 67(4):1120-1121. doi:
10.4103/0028-3886.266260
. [PMID: 31512651] - Mickael Vourc'h, Eric Dailly, Yannick Hourmant, Ronan Bellouard, Pierre-Joachim Mahe, Guillaume Deslandes, Matthieu Grégoire, Karim Asehnoune. Pharmacokinetics and toxicity of high-dose baclofen in ICU patients.
Progress in neuro-psychopharmacology & biological psychiatry.
2019 06; 92(?):450-456. doi:
10.1016/j.pnpbp.2019.02.016
. [PMID: 30826461] - Paolo Nikolai Hao So, Maria Ruby Rose Quijano Castañeda, Anne Rolaine Velasco Morante, Raymond Villacorta Oliva. Muscle spasm-induced exothermia in dystonic cerebral palsy: uncommon and frequently misdiagnosed condition.
BMJ case reports.
2019 Mar; 12(3):. doi:
10.1136/bcr-2018-227488
. [PMID: 30837235] - Sriram Sriperumbuduri, Swapnil Hiremath. The case for cautious consumption: NSAIDs in chronic kidney disease.
Current opinion in nephrology and hypertension.
2019 03; 28(2):163-170. doi:
10.1097/mnh.0000000000000473
. [PMID: 30531470] - Tae Hwan Kim, Jürgen B Bulitta, Do-Hyung Kim, Soyoung Shin, Beom Soo Shin. Novel extended in vitro-in vivo correlation model for the development of extended-release formulations for baclofen: From formulation composition to in vivo pharmacokinetics.
International journal of pharmaceutics.
2019 Feb; 556(?):276-286. doi:
10.1016/j.ijpharm.2018.12.007
. [PMID: 30543888] - Olga Geisel, Rainer Hellweg, Klaus-Dieter Wernecke, Klaus Wiedemann, Christian A Müller. Total and acylated ghrelin plasma levels as potential long-term response markers in alcohol-dependent patients receiving high-dose of the GABA-B receptor agonist baclofen.
Psychiatry research.
2019 02; 272(?):431-437. doi:
10.1016/j.psychres.2018.12.095
. [PMID: 30611960] - Olga Geisel, Ludwig Schlemm, Rainer Hellweg, Klaus Wiedemann, Christian A Müller. Hypothalamic-Pituitary-Adrenocortical Axis Activity in Alcohol-Dependent Patients During Treatment with High-Dose Baclofen.
Pharmacopsychiatry.
2019 Jan; 52(1):32-37. doi:
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Journal of pediatric rehabilitation medicine.
2019 ; 12(3):313-315. doi:
10.3233/prm-180598
. [PMID: 31476182] - Emad Khazneh, Alaa Shamlawi, Kamel Jebrin, Zakaria Hamdan, Osama Sawalmeh. Single-dose baclofen-induced neurotoxicity in a patient with end stage renal disease: case report.
BMC nephrology.
2018 12; 19(1):352. doi:
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. [PMID: 30537935] - Claudia V Turco, Jenin El-Sayes, Mitchell B Locke, Robert Chen, Steven Baker, Aimee J Nelson. Effects of lorazepam and baclofen on short- and long-latency afferent inhibition.
The Journal of physiology.
2018 11; 596(21):5267-5280. doi:
10.1113/jp276710
. [PMID: 30192388] - Rafael Arroyo González. A review of the effects of baclofen and of THC:CBD oromucosal spray on spasticity-related walking impairment in multiple sclerosis.
Expert review of neurotherapeutics.
2018 10; 18(10):785-791. doi:
10.1080/14737175.2018.1510772
. [PMID: 30235965] - Magali Chartier, Isabelle Malissin, Salma Tannous, Laurence Labat, Patricia Risède, Bruno Mégarbane, Lucie Chevillard. Baclofen-induced encephalopathy in overdose - Modeling of the electroencephalographic effect/concentration relationships and contribution of tolerance in the rat.
Progress in neuro-psychopharmacology & biological psychiatry.
2018 08; 86(?):131-139. doi:
10.1016/j.pnpbp.2018.05.016
. [PMID: 29782961] - Magali Chartier, Salma Tannous, Nadia Benturquia, Laurence Labat, Rafael Reis, Patricia Risède, Lucie Chevillard, Bruno Mégarbane. Baclofen-Induced Neuro-Respiratory Toxicity in the Rat: Contribution of Tolerance and Characterization of Withdrawal Syndrome.
Toxicological sciences : an official journal of the Society of Toxicology.
2018 07; 164(1):153-165. doi:
10.1093/toxsci/kfy073
. [PMID: 29945230] - Majid Ghareghani, Kazem Zibara, Hossein Sadeghi, Naser Farhadi. Spasticity Treatment Ameliorates the Efficacy of Melatonin Therapy in Experimental Autoimmune Encephalomyelitis (EAE) Mouse Model of Multiple Sclerosis.
Cellular and molecular neurobiology.
2018 Jul; 38(5):1145-1151. doi:
10.1007/s10571-018-0580-y
. [PMID: 29497878] - Nurul H M Yusoff, Sharif M Mansor, Christian P Müller, Zurina Hassan. Baclofen blocks the acquisition and expression of mitragynine-induced conditioned place preference in rats.
Behavioural brain research.
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Fundamental & clinical pharmacology.
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Anaesthesia, critical care & pain medicine.
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Journal of analytical toxicology.
2016 Mar; 40(2):117-23. doi:
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European neurology.
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Drug delivery.
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European neurology.
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European neurology.
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Alcoholism, clinical and experimental research.
2015 Sep; 39(9):1602-8. doi:
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Seminars in dialysis.
2015 Sep; 28(5):525-9. doi:
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Journal of pharmacy practice.
2015 Aug; 28(4):430-3. doi:
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Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition.
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The American journal of case reports.
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European journal of clinical pharmacology.
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The Journal of general physiology.
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Alcoholism, clinical and experimental research.
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Pharmacotherapy.
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Contemporary clinical trials.
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Nihon Jibiinkoka Gakkai kaiho.
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