Target Information

Target General Infomation
Target ID
T75440
Former ID
TTDS00454
Target Name
Peripheral-type benzodiazepine receptor
Gene Name
TSPO
Synonyms
Mitochondrial benzodiazepine receptor; PBR; PKBS; Peripheral benzodiazepine receptor; Translocator protein; TSPO
Target Type
Successful
Disease Anxiety disorder; Insomnia [ICD9: 300, 307.4, 327.0; ICD10: F40-F42, F51.0, G47.0]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Alzheimer disease [ICD9: 331; ICD10: G30]
Anxiety disorder; Status epilepticus [ICD9: 300, 345.3; ICD10: F40-F42, G40]
Brain diseases [ICD10: G00-G99]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Convulsions [ICD9: 780.3; ICD10: R56.0]
Epilepsy [ICD10: G40]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Lateral sclerosis [ICD10: G12.2]
Muscle relaxant [ICD10: N39.3, N39.4, R32]
Nootropic [ICD10: F00-F99]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Sedation [ICD9: 338; ICD10: R52, G89]
Spasms; Pain; Anxiety disorder [ICD9:338, 780, 300, 311; ICD10: R52, G89, F32, F40-F42]
Function
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides(PubMed:1847678).
BioChemical Class
Cholesterol porphyrin uptake translocator
Target Validation
T75440
UniProt ID
P30536
Sequence
MAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAM
GYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAA
ATTVAWYQVSPLAARLLYPYLAWLAFTTTLNYCVWRDNHGWRGGRRLPE
Drugs and Mode of Action
Drug(s) Adinazolam Drug Info Approved Anxiety disorder; Status epilepticus [1]
ALPIDEM Drug Info Approved Anxiety disorder [2]
Alprazolam Drug Info Approved Anxiety disorder [3], [4]
Chlordiazepoxide Drug Info Approved Anxiety disorder [5], [6]
Chlormezanone Drug Info Approved Spasms; Pain; Anxiety disorder [7], [8], [2]
Cinolazepam Drug Info Approved Muscle relaxant [9]
Clorazepate Drug Info Approved Anxiety disorder; Insomnia [10], [11]
Clotiazepam Drug Info Approved Anxiety disorder [12]
Diazepam Drug Info Approved Epilepsy [13], [14]
Estazolam Drug Info Approved Insomnia [15], [16]
Eszopiclone Drug Info Approved Insomnia [17], [18]
Fludiazepam Drug Info Approved Anxiety disorder [19]
Flumazenil Drug Info Approved Benzodiazepine overdoses [20], [21]
Flunitrazepam Drug Info Approved Insomnia [22], [23]
Flurazepam Drug Info Approved Insomnia [24], [25]
Halazepam Drug Info Approved Anxiety disorder [26], [27]
Lorazepam Drug Info Approved Anxiety disorder [28], [29]
Midazolam Drug Info Approved Sedation [30], [31]
Oxazepam Drug Info Approved Anxiety disorder [32], [33]
Prazepam Drug Info Approved Anxiety disorder [34], [35]
Quazepam Drug Info Approved Insomnia [36], [37]
Temazepam Drug Info Approved Insomnia [38], [39]
Triazolam Drug Info Approved Insomnia [32], [40]
11C-PBR-28 Drug Info Phase 2 Brain diseases [41]
Dextofisopam Drug Info Phase 2 Irritable bowel syndrome [42]
ONO-2952 Drug Info Phase 2 Irritable bowel syndrome [43]
SSR-180575 Drug Info Phase 2 Rheumatoid arthritis [44]
TLN-4601 Drug Info Phase 2 Cancer [45]
18F-FEDAA-1106 Drug Info Phase 1 Alzheimer disease [46]
BAY-85-8102 Drug Info Phase 1 Brain diseases [47]
Ro-16-6028 Drug Info Discontinued in Phase 3 Anxiety disorder [48], [49]
Emapunil Drug Info Discontinued in Phase 2 Anxiety disorder [50], [51]
Lirequinil Drug Info Discontinued in Phase 2 Anxiety disorder [52]
S-8510 Drug Info Discontinued in Phase 2 Nootropic [53]
TRO-40303 Drug Info Discontinued in Phase 2 Lateral sclerosis [54]
Imepitoin Drug Info Discontinued in Phase 1 Convulsions [55]
DAA-1097 Drug Info Terminated Anxiety disorder [56]
Ginkgolide B (GKB) Drug Info Terminated Discovery agent [57]
Miltirone Drug Info Terminated Anxiety disorder [58]
NNC-13-8119 Drug Info Terminated Anxiety disorder [59]
NS-2979 Drug Info Terminated Pain [60]
PK 11195 Drug Info Terminated Discovery agent [61], [62]
Ro 5-4864 Drug Info Terminated Discovery agent [63]
Inhibitor (R)PK-11195 Drug Info [64]
2-(2-Phenyl-1H-indol-3-yl)-N,N-dipropyl-acetamide Drug Info [65]
4-Methoxy-5-phenyl-6-thia-10b-aza-benzo[e]azulene Drug Info [66]
5-Phenyl-6-thia-10b-aza-benzo[e]azulen-4-one Drug Info [67]
5-Phenyl-6-thia-10b-aza-benzo[e]azulene Drug Info [66]
6-Thia-10b-aza-benzo[e]azulen-4-one Drug Info [67]
ALPIDEM Drug Info [68]
N,N-Diethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [65]
N,N-Dihexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [65]
N,N-Dimethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [65]
N-Hexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [65]
SSR-180575 Drug Info [69], [2]
Binder 11C-PBR-170 Drug Info [70]
11C-PBR-28 Drug Info [71]
Cinolazepam Drug Info [72]
FGIN-1-27 Drug Info [73]
PK 11195 Drug Info [73]
Ro 5-4864 Drug Info [73], [74]
TGSC01AA(4) Drug Info [70]
Modulator 18F-FEDAA-1106 Drug Info [75]
Chlordiazepoxide Drug Info [76]
Clorazepate Drug Info [76]
Flurazepam Drug Info [76]
Halazepam Drug Info [76]
Lorazepam Drug Info [76]
Midazolam Drug Info [76]
Miltirone Drug Info [77]
NNC-13-8119 Drug Info [78]
NS-2979 Drug Info [79]
Prazepam Drug Info [76]
Quazepam Drug Info [76]
Ro-16-6028 Drug Info
Temazepam Drug Info [76]
TLN-4601 Drug Info
Triazolam Drug Info [76]
TRO-40303 Drug Info [80]
U-89854 Drug Info [70]
Agonist Adinazolam Drug Info [81]
Alprazolam Drug Info [82], [83]
BAY-85-8102 Drug Info [70]
Benzodiazepine Drug Info [70]
Chlormezanone Drug Info [84]
Clotiazepam Drug Info [85]
DAA-1097 Drug Info [86]
Dextofisopam Drug Info [42]
Diazemuls Drug Info [87]
Diazepam Drug Info [88]
Emapunil Drug Info [89]
Estazolam Drug Info [90], [91]
Eszopiclone Drug Info [82], [92]
Fludiazepam Drug Info [93]
Flunitrazepam Drug Info [83]
Imepitoin Drug Info [94]
Lirequinil Drug Info [95]
Oxazepam Drug Info [96]
S-8510 Drug Info [2]
Antagonist Flumazenil Drug Info [70]
ONO-2952 Drug Info [97]
Suppressor Ginkgolide B (GKB) Drug Info [98]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
HTLV-I infection
References
REF 1Drug information of Adinazolam, 2008. eduDrugs.
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074046.
REF 4(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7111).
REF 5Use of the accelerating rotarod for assessment of motor performance decrement induced by potential anticonvulsant compounds in nerve agent poisoning. Drug Chem Toxicol. 1992;15(3):177-201.
REF 6(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3370).
REF 7FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011467.
REF 8(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7323).
REF 9Drug information of Cinolazepam, 2008. eduDrugs.
REF 10FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071852.
REF 11(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7548).
REF 12Drug information of Clotiazepam, 2008. eduDrugs.
REF 13ClinicalTrials.gov (NCT01939093) Therapeutic Effect of Quetiapine on Methamphetamine-Induced Psychosis. U.S. National Institutes of Health.
REF 14(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3364).
REF 15FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074818.
REF 16(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7550).
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REF 19Drug information of Fludiazepam, 2008. eduDrugs.
REF 20(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4192).
REF 21ClinicalTrials.gov (NCT00997087) A Randomized, Double-Blind, Placebo-Controlled Trial of Flumazenil for the Treatment of Obsessive Compulsive Disorder. U.S. National Institutes of Health.
REF 22(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4360).
REF 23Drug information of Flunitrazepam, 2008. eduDrugs.
REF 24FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070344.
REF 25(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7188).
REF 26FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017736.
REF 27(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7195).
REF 28FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071117.
REF 29(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5884).
REF 30FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075154.
REF 31(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3342).
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REF 33(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7253).
REF 34(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7275).
REF 35Drug information of Prazepam, 2008. eduDrugs.
REF 36FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018708.
REF 37(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7288).
REF 38FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070919.
REF 39(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7300).
REF 40(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7313).
REF 41ClinicalTrials.gov (NCT02513589) Molecular Imaging of Inflammation With 18F-PBR06 to Identify Unstable Carotid Plaques in Patients With Stroke.
REF 42Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
REF 43ClinicalTrials.gov (NCT01887002) Study to Evaluate the Effects of ONO-2952 on Pain Perception Produced by Rectal Distention in Female Subjects With Diarrhea-Predominant Irritable Bowel Syndrome (IBS-D). U.S. National Institutes of Health.
REF 44ClinicalTrials.gov (NCT00502515) Dose-effect of SSR180575 in Diabetic Neuropathy. U.S. National Institutes of Health.
REF 45ClinicalTrials.gov (NCT00730262) Efficacy Study of TLN-4601 in Patients With Recurring Glioblastoma Multiforme. U.S. National Institutes of Health.
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031827)
REF 47ClinicalTrials.gov (NCT01009359) Evaluation of the Neuroinflammation Pattern of BAY85-8102 F-18, DPA-714 in Probable Alzheimers Disease Patients Versus Healthy Volunteers and Radiation Dosimetry of F18, DPA-714 in Healthy Volunteers. U.S. National Institutes of Health.
REF 48(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4146).
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000640)
REF 50(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8704).
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013611)
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001968)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005238)
REF 54Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033814)
REF 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008368)
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012540)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000117)
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003466)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004060)
REF 60Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013494)
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REF 62Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000635)
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REF 64Bioorg Med Chem Lett. 2003 Jan 20;13(2):201-4.[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).
REF 65J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
REF 66J Med Chem. 1995 Nov 10;38(23):4730-8.A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.
REF 67J Med Chem. 1994 May 13;37(10):1427-38.Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.
REF 68J Med Chem. 2008 Sep 25;51(18):5798-806. Epub 2008 Aug 26.Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
REF 69SSR180575 (7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide), a peripheral benzodiazepine receptor ligand, promotes neuronal survival and repair. J PharmacolExp Ther. 2002 Jun;301(3):1067-78.
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REF 72Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise. Int J Clin Pharmacol Res. 1987;7(5):407-18.
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REF 84Successful treatment of anxiety with a single night-time dose of chlormezanone: double-blind comparison with diazepam. Curr Med Res Opin. 1982;8(1):33-8.
REF 85Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones. Br J Pharmacol. 1989 Nov;98(3):735-40.
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REF 87The alpha5(H105R) mutation impairs alpha5 selective binding properties by altered positioning of the alpha5 subunit in GABAA receptors containing two distinct types of alpha subunits. J Neurochem. 2009 Jul;110(1):244-54. Epub 2009 Apr 27.
REF 88Translocator protein (18 kDa) mediates the pro-growth effects of diazepam on Ehrlich tumor cells in vivo. Eur J Pharmacol. 2010 Jan 25;626(2-3):131-8.
REF 89Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
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REF 91Design and synthesis of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles as benzodiazepine receptor agonists. Bioorg Med Chem Lett. 2005 Jun 15;15(12):3126-9.
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REF 95Pharmacokinetics and pharmacodynamics of Ro 41-3696, a novel nonbenzodiazepine hypnotic. J Clin Pharmacol. 1995 Aug;35(8):821-9.
REF 96Effects of the combination of metyrapone and oxazepam on cocaine and food self-administration in rats. Pharmacol Biochem Behav. 2008 Nov;91(1):181-9. Epub 2008 Jul 19.
REF 97Anti-stress effects of ONO-2952, a novel translocator protein 18 kDa antagonist, in rats. Neuropharmacology. 2015 Jul 17;99:51-66.
REF 98Drug-induced inhibition of the peripheral-type benzodiazepine receptor expression and cell proliferation in human breast cancer cells. Anticancer Res. 2000 Sep-Oct;20(5A):2835-47.

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