General Information of Drug (ID: DMPTM6V)

Drug Name
TOLSERINE Drug Info
Synonyms tolserine.tartaric acid; 2-methylphenserine; CHEMBL130458; SCHEMBL8920175; BDBM10959; (3aS,8aR)-1,3a,8-trimethyl-1H,2H,3H,3aH,8H,8aH-pyrrolo[2,3-b]indol-5-yl N-(2-methylphenyl)carbamate
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9928397
TTD Drug ID
DMPTM6V

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug(s) Targeting Acetylcholinesterase (AChE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [4]
Donepezil DMIYG7Z Advanced cancer 2A00-2F9Z Approved [5]
Malathion DMXZ84M Pediculus capitis infestation 1G00.0 Approved [6]
Galantamine DMEO794 Alzheimer disease 8A20 Approved [7]
Huperzine A DMMAWLU Alzheimer disease 8A20 Approved [8]
Neostigmine DM6T2J3 Myasthenia gravis 8C6Y Approved [9]
YM443 DMNZCI1 Functional dyspepsia DD90.3 Approved [10]
Ambenonium DMOP0BL Myasthenia gravis 8C6Y Approved [11]
Demecarium bromide DMAYEU1 Open-angle glaucoma 9C61 Approved [12]
Isoflurophate DMBSK7X Glaucoma/ocular hypertension 9C61 Approved [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Cholinesterase (BCHE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hexafluronium bromide DMFY307 Spasm MB47.3 Approved [14]
MEPTAZINOL DMPSB8F Pain MG30-MG3Z Approved [15]
Eptastigmine DMTV7ZM Cognitive impairment 6D71 Phase 3 [1]
(-)-Phenserine DMNCY1I Alzheimer disease 8A20 Phase 3 [16]
Plasma derived human butyrylcholinesterase DMF3IBC Neurotoxicity NE61 Phase 1 [17]
Protexia DME1Y9W Alzheimer disease 8A20 Phase 1 [18]
JES-9501 DMYR3IE Alzheimer disease 8A20 Phase 1 [19]
Tetra-hydro-isoquinoline derivative 3 DMCZA45 N. A. N. A. Patented [20]
Tetra-hydro-isoquinoline derivative 1 DML86IO N. A. N. A. Patented [20]
Tetra-hydro-isoquinoline derivative 2 DM5CKVF N. A. N. A. Patented [20]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cocaine esterase (CES2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [21]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [22]
Dextropropoxyphene DM23HCX Pain MG30-MG3Z Approved [23]
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
Quercetin DM3NC4M Obesity 5B81 Approved [25]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [3]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [26]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [27]
Testosterone enanthate DMB6871 N. A. N. A. Approved [28]
Cantharidin DMBP5N3 Molluscum contagiosum infection 1E76 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [30]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [31]
Dextropropoxyphene DM23HCX Pain MG30-MG3Z Approved [23]
Selenium DM25CGV N. A. N. A. Approved [32]
Naloxone DM3FXMA Narcotic depression 6A7Z Approved [33]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [34]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [35]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [21]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [36]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [37]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Acetylcholinesterase (AChE) TT1RS9F ACES_HUMAN Inhibitor [2]
Cholinesterase (BCHE) TTEB0GD CHLE_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cocaine esterase (CES2) OTC647SQ EST2_HUMAN Gene/Protein Processing [3]
Liver carboxylesterase 1 (CES1) OT9L0LR8 EST1_HUMAN Gene/Protein Processing [3]

References

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2 Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based vi... J Med Chem. 2010 Sep 9;53(17):6490-505.
3 Inhibition of human carboxylesterases hCE1 and hiCE by cholinesterase inhibitors. Chem Biol Interact. 2013 Mar 25;203(1):226-30.
4 Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002 Jun;(127):6-19.
5 URL: 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: 2465).
6 Acetylcholinesterase activity in Corbicula fluminea Mull., as a biomarker of organophosphate pesticide pollution in Pinacanauan River, Philippines. Environ Monit Assess. 2010 Jun;165(1-4):331-40.
7 [From symptomatic to disease modifying therapy Recent developments in the pharmacotherapy of Alzheimer's disease]. Fortschr Neurol Psychiatr. 2009 Jun;77(6):326-33.
8 Huperzine A attenuates cognitive deficits and brain injury in neonatal rats after hypoxia-ischemia. Brain Res. 2002 Sep 13;949(1-2):162-70.
9 Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet. J Sep Sci. 2009 May;32(10):1748-56.
10 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
11 Alpha6-containing nicotinic acetylcholine receptors dominate the nicotine control of dopamine neurotransmission in nucleus accumbens. Neuropsychopharmacology. 2008 Aug;33(9):2158-66.
12 The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs. Vet Ophthalmol. 2003 Mar;6(1):23-5.
13 Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. Chem Biol. 2003 Jun;10(6):491-502.
14 Synergistic effect of acidosis and succinylcholine-induced hyperkalemia in spinal cord transected rats. Acta Anaesthesiol Scand. 1984 Feb;28(1):87-90.
15 Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation. J Med Chem. 2008 Apr 10;51(7):2027-36.
16 Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine. Bioorg Med Chem. 2010 Jul 1;18(13):4687-93.
17 Acetylcholinesterase-Fc Fusion Protein (AChE-Fc): A Novel Potential Organophosphate Bioscavenger with Extended Plasma Half-Life. Bioconjug Chem. 2015 Aug 19;26(8):1753-8.
18 In vitro and in vivo characterization of recombinant human butyrylcholinesterase (Protexia) as a potential nerve agent bioscavenger. Chem Biol Interact. 2005 Dec 15;157-158:363-5.
19 Dehydroevodiamine attenuates beta-amyloid peptide-induced amnesia in mice. Eur J Pharmacol. 2001 Feb 16;413(2-3):221-5.
20 A patent review of butyrylcholinesterase inhibitors and reactivators 2010-2017.Expert Opin Ther Pat. 2018 Jun;28(6):455-465.
21 Dexamethasone differentially regulates expression of carboxylesterase genes in humans and rats. Drug Metab Dispos. 2000 Feb;28(2):186-91.
22 Transcriptional activation of the carboxylesterase 2 gene by the p53 pathway. Cancer Biol Ther. 2006 Nov;5(11):1450-6.
23 Binding and hydrolysis of meperidine by human liver carboxylesterase hCE-1. J Pharmacol Exp Ther. 1999 Jul;290(1):314-8.
24 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
25 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
26 Photochemotherapeutic agent 8-methoxypsoralen induces cytochrome P450 3A4 and carboxylesterase HCE2: evidence on an involvement of the pregnane X receptor. Toxicol Sci. 2007 Jan;95(1):13-22.
27 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
28 Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
29 Hepatoxicity mechanism of cantharidin-induced liver LO2 cells by LC-MS metabolomics combined traditional approaches. Toxicol Lett. 2020 Oct 15;333:49-61. doi: 10.1016/j.toxlet.2020.07.024. Epub 2020 Jul 26.
30 Concise prediction models of anticancer efficacy of 8 drugs using expression data from 12 selected genes. Int J Cancer. 2004 Sep 10;111(4):617-26. doi: 10.1002/ijc.20289.
31 Cannabidiol Activates Neuronal Precursor Genes in Human Gingival Mesenchymal Stromal Cells. J Cell Biochem. 2017 Jun;118(6):1531-1546. doi: 10.1002/jcb.25815. Epub 2016 Dec 29.
32 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
33 Human carboxylesterase 1: from drug metabolism to drug discovery. Biochem Soc Trans. 2003 Jun;31(Pt 3):620-4. doi: 10.1042/bst0310620.
34 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
35 Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. Chem Biol. 2003 Apr;10(4):341-9. doi: 10.1016/s1074-5521(03)00071-1.
36 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
37 Proteomics investigations of drug-induced hepatotoxicity in HepG2 cells. Toxicol Sci. 2011 Mar;120(1):109-22.