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 [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]
Anxiety disorder; Insomnia [ICD9: 300, 307.4, 327.0; ICD10: F40-F42, F51.0, G47.0]
Brain diseases [ICD10: G00-G99]
Convulsions [ICD9: 780.3; ICD10: R56.0]
Cancer [ICD9: 140-229; ICD10: C00-C96]
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]
Spasms; Pain; Anxiety disorder [ICD9:338, 780, 300, 311; ICD10: R52, G89, F32, F40-F42]
Sedation [ICD9: 338; ICD10: R52, G89]
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 [550684]
ALPIDEM Drug Info Approved Anxiety disorder [551871]
Alprazolam Drug Info Approved Anxiety disorder [538259], [542118]
Chlordiazepoxide Drug Info Approved Anxiety disorder [535828], [540324]
Chlormezanone Drug Info Approved Spasms; Pain; Anxiety disorder [538447], [542346], [551871]
Cinolazepam Drug Info Approved Muscle relaxant [550708]
Clorazepate Drug Info Approved Anxiety disorder; Insomnia [538240], [542549]
Clotiazepam Drug Info Approved Anxiety disorder [550777]
Diazepam Drug Info Approved Epilepsy [524426], [540319]
Estazolam Drug Info Approved Insomnia [538287], [542551]
Eszopiclone Drug Info Approved Insomnia [536647], [542452]
Fludiazepam Drug Info Approved Anxiety disorder [550695]
Flumazenil Drug Info Approved Benzodiazepine overdoses [467528], [522823]
Flunitrazepam Drug Info Approved Insomnia [467696], [550754]
Flurazepam Drug Info Approved Insomnia [538223], [542199]
Halazepam Drug Info Approved Anxiety disorder [538493], [542207]
Lorazepam Drug Info Approved Anxiety disorder [538231], [541183]
Midazolam Drug Info Approved Sedation [538292], [540301]
Oxazepam Drug Info Approved Anxiety disorder [536565], [542271]
Prazepam Drug Info Approved Anxiety disorder [542295], [550778]
Quazepam Drug Info Approved Insomnia [538513], [542308]
Temazepam Drug Info Approved Insomnia [538229], [542322]
Triazolam Drug Info Approved Insomnia [536565], [542336]
11C-PBR-28 Drug Info Phase 2 Brain diseases [525281]
Dextofisopam Drug Info Phase 2 Irritable bowel syndrome [536224]
ONO-2952 Drug Info Phase 2 Irritable bowel syndrome [524339]
SSR-180575 Drug Info Phase 2 Rheumatoid arthritis [522067]
TLN-4601 Drug Info Phase 2 Cancer [522396]
18F-FEDAA-1106 Drug Info Phase 1 Alzheimer disease [549054]
BAY-85-8102 Drug Info Phase 1 Brain diseases [522842]
Ro-16-6028 Drug Info Discontinued in Phase 3 Anxiety disorder [467491], [544696]
Emapunil Drug Info Discontinued in Phase 2 Anxiety disorder [543259], [547175]
Lirequinil Drug Info Discontinued in Phase 2 Anxiety disorder [545048]
S-8510 Drug Info Discontinued in Phase 2 Nootropic [545890]
TRO-40303 Drug Info Discontinued in Phase 2 Lateral sclerosis [549216]
Imepitoin Drug Info Discontinued in Phase 1 Convulsions [546470]
DAA-1097 Drug Info Terminated Anxiety disorder [547051]
Ginkgolide B (GKB) Drug Info Terminated Discovery agent [544554]
Miltirone Drug Info Terminated Anxiety disorder [545493]
NNC-13-8119 Drug Info Terminated Anxiety disorder [545660]
NS-2979 Drug Info Terminated Pain [547155]
PK 11195 Drug Info Terminated Discovery agent [543258], [544695]
Ro 5-4864 Drug Info Terminated Discovery agent [545047]
Inhibitor (R)PK-11195 Drug Info [526488]
2-(2-Phenyl-1H-indol-3-yl)-N,N-dipropyl-acetamide Drug Info [534032]
4-Methoxy-5-phenyl-6-thia-10b-aza-benzo[e]azulene Drug Info [533589]
5-Phenyl-6-thia-10b-aza-benzo[e]azulen-4-one Drug Info [533922]
5-Phenyl-6-thia-10b-aza-benzo[e]azulene Drug Info [533589]
6-Thia-10b-aza-benzo[e]azulen-4-one Drug Info [533922]
ALPIDEM Drug Info [529656]
N,N-Diethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [534032]
N,N-Dihexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [534032]
N,N-Dimethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [534032]
N-Hexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info [534032]
SSR-180575 Drug Info [526341], [551871]
Binder 11C-PBR-170 Drug Info [543743]
11C-PBR-28 Drug Info [528547]
Cinolazepam Drug Info [537708]
FGIN-1-27 Drug Info [535317]
PK 11195 Drug Info [535317]
Ro 5-4864 Drug Info [535317], [538133]
TGSC01AA(4) Drug Info [543743]
Modulator 18F-FEDAA-1106 Drug Info [526694]
Chlordiazepoxide Drug Info [556264]
Clorazepate Drug Info [556264]
Flurazepam Drug Info [556264]
Halazepam Drug Info [556264]
Lorazepam Drug Info [556264]
Midazolam Drug Info [556264]
Miltirone Drug Info [528077]
NNC-13-8119 Drug Info [545661]
NS-2979 Drug Info [547156]
Prazepam Drug Info [556264]
Quazepam Drug Info [556264]
Ro-16-6028 Drug Info
Temazepam Drug Info [556264]
TLN-4601 Drug Info
Triazolam Drug Info [556264]
TRO-40303 Drug Info [544374]
U-89854 Drug Info [543743]
Agonist Adinazolam Drug Info [534872]
Alprazolam Drug Info [536166], [537330]
BAY-85-8102 Drug Info [543743]
Benzodiazepine Drug Info [543743]
Chlormezanone Drug Info [537816]
Clotiazepam Drug Info [537693]
DAA-1097 Drug Info [525488]
Dextofisopam Drug Info [536224]
Diazemuls Drug Info [537354]
Diazepam Drug Info [530408]
Emapunil Drug Info [536580]
Estazolam Drug Info [535677], [536079]
Eszopiclone Drug Info [536166], [536625]
Fludiazepam Drug Info [537701]
Flunitrazepam Drug Info [537330]
Imepitoin Drug Info [532596]
Lirequinil Drug Info [534064]
Oxazepam Drug Info [536807]
S-8510 Drug Info [551871]
Antagonist Flumazenil Drug Info [543743]
ONO-2952 Drug Info [533291]
Suppressor Ginkgolide B (GKB) Drug Info [535072]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
HTLV-I infection
References
Ref 467491(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 467528(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 467696(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 522067ClinicalTrials.gov (NCT00502515) Dose-effect of SSR180575 in Diabetic Neuropathy. U.S. National Institutes of Health.
Ref 522396ClinicalTrials.gov (NCT00730262) Efficacy Study of TLN-4601 in Patients With Recurring Glioblastoma Multiforme. U.S. National Institutes of Health.
Ref 522823ClinicalTrials.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 522842ClinicalTrials.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 524339ClinicalTrials.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 524426ClinicalTrials.gov (NCT01939093) Therapeutic Effect of Quetiapine on Methamphetamine-Induced Psychosis. U.S. National Institutes of Health.
Ref 525281ClinicalTrials.gov (NCT02513589) Molecular Imaging of Inflammation With 18F-PBR06 to Identify Unstable Carotid Plaques in Patients With Stroke.
Ref 535828Use 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 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536565What every dentist should know about the "z-sedatives". J Mass Dent Soc. 2007 Fall;56(3):44-5.
Ref 536647Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
Ref 538223FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070344.
Ref 538229FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070919.
Ref 538231FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071117.
Ref 538240FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071852.
Ref 538259FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074046.
Ref 538287FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074818.
Ref 538292FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075154.
Ref 538447FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011467.
Ref 538493FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017736.
Ref 538513FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018708.
Ref 540301(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).
Ref 540319(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 540324(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 541183(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 542118(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 542199(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 542207(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 542271(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 542295(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 542308(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 542322(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 542336(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 542346(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 542452(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: 7429).
Ref 542549(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 542551(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).
Ref 543258(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: 8703).
Ref 543259(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 544554Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000117)
Ref 544695Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000635)
Ref 544696Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000640)
Ref 545047Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001966)
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Ref 545493Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003466)
Ref 545660Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004060)
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Ref 546470Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008368)
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Ref 547155Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013494)
Ref 547175Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013611)
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Ref 549216Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033814)
Ref 550684Drug information of Adinazolam, 2008. eduDrugs.
Ref 550695Drug information of Fludiazepam, 2008. eduDrugs.
Ref 550708Drug information of Cinolazepam, 2008. eduDrugs.
Ref 550754Drug information of Flunitrazepam, 2008. eduDrugs.
Ref 550777Drug information of Clotiazepam, 2008. eduDrugs.
Ref 550778Drug information of Prazepam, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525488Neuropharmacological profile of peripheral benzodiazepine receptor agonists, DAA1097 and DAA1106. Life Sci. 1999;64(16):1455-64.
Ref 526341SSR180575 (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.
Ref 526488Bioorg 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 526694Role of peripheral benzodiazepine receptors in mitochondrial, cellular, and cardiac damage induced by oxidative stress and ischemia-reperfusion. J Pharmacol Exp Ther. 2003 Sep;306(3):828-37.
Ref 528077Miltirone, a central benzodiazepine receptor partial agonist from a Chinese medicinal herb Salvia miltiorrhiza. Neurosci Lett. 1991 Jun 24;127(2):237-41.
Ref 528547PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat. Neurosci Lett. 2007 Jan 16;411(3):200-5. Epub 2006 Nov28.
Ref 529656J 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 530408Translocator 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 532596The pharmacology of imepitoin: the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy. CNS Drugs. 2014 Jan;28(1):29-43.
Ref 533291Anti-stress effects of ONO-2952, a novel translocator protein 18 kDa antagonist, in rats. Neuropharmacology. 2015 Jul 17;99:51-66.
Ref 533589J 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 533922J 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 534032J 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 534064Pharmacokinetics and pharmacodynamics of Ro 41-3696, a novel nonbenzodiazepine hypnotic. J Clin Pharmacol. 1995 Aug;35(8):821-9.
Ref 534872Effects of antidepressants and benzodiazepine treatments on the dendritic structure of CA3 pyramidal neurons after chronic stress. Eur J Pharmacol. 1999 Apr 29;371(2-3):113-22.
Ref 535072Drug-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.
Ref 535317Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells. Br J Cancer. 2001 Nov 30;85(11):1771-80.
Ref 535677Design and synthesis of 4H-3-(2-phenoxy)phenyl-1,2,4-triazole derivatives as benzodiazepine receptor agonists. Bioorg Med Chem. 2003 Mar 6;11(5):769-73.
Ref 536079Design 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.
Ref 536166Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 536625New hypnotics: perspectives from sleep physiology. Vertex. 2007 Jul-Aug;18(74):294-9.
Ref 536807Effects 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 537330Comparison of five benzodiazepine-receptor agonists on buprenorphine-induced mu-opioid receptor regulation. J Pharmacol Sci. 2009 May;110(1):36-46.
Ref 537354The 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 537693Effects 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.
Ref 537701Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9.
Ref 537708Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise. Int J Clin Pharmacol Res. 1987;7(5):407-18.
Ref 537816Successful 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 538133Antiproliferative and differentiating effects of benzodiazepine receptor ligands on B16 melanoma cells. Biochem Pharmacol. 1998 Oct 15;56(8):1029-34.
Ref 543743(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. (Target id: 2879).
Ref 544374Translation of TRO40303 from myocardial infarction models to demonstration of safety and tolerance in a randomized Phase I trial. J Transl Med. 2014; 12: 38.
Ref 545661Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004060)
Ref 547156Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013494)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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