General Information of Drug (ID: DMTV7ZM)

Drug Name
Eptastigmine Drug Info
Synonyms
heptastigmine; Heptylphysostigmine; Physostigmine heptyl; Eptastigmine [INN]; (-)-Heptylphysostigmine; Eptastigminum [INN-Latin]; Eptastigmina [INN-Spanish]; UNII-6PZZ52D76Q; N-Demethyl-N-heptylphysostigmine; 101246-68-8; BRN 4883778; CHEMBL433041; 6PZZ52D76Q; Heptylstigmine; heptyl-physostigmine; Eptastigminum; Eptastigmina; heptyl physostigmine; Carbamic acid, heptyl-, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)indol-5-yl ester, (3aS-cis)-; AC1Q60XA; SCHEMBL195028; BDBM10972; Epiastigmine; Eptastigmine tartrate; Heptylstigmine tartrate; Heptyl-physostigmine; L-693487; MF-201; HEPTYPHYSOSTIGMINE
Indication
Disease Entry ICD 11 Status REF
Cognitive impairment 6D71 Phase 3 [1]
Cross-matching ID
PubChem CID
65872
CAS Number
CAS 101246-68-8
TTD Drug ID
DMTV7ZM

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 [5]
Donepezil DMIYG7Z Advanced cancer 2A00-2F9Z Approved [6]
Malathion DMXZ84M Pediculus capitis infestation 1G00.0 Approved [7]
Galantamine DMEO794 Alzheimer disease 8A20 Approved [8]
Huperzine A DMMAWLU Alzheimer disease 8A20 Approved [9]
Neostigmine DM6T2J3 Myasthenia gravis 8C6Y Approved [10]
YM443 DMNZCI1 Functional dyspepsia DD90.3 Approved [11]
Ambenonium DMOP0BL Myasthenia gravis 8C6Y Approved [12]
Demecarium bromide DMAYEU1 Open-angle glaucoma 9C61 Approved [13]
Isoflurophate DMBSK7X Glaucoma/ocular hypertension 9C61 Approved [14]
⏷ 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 [15]
MEPTAZINOL DMPSB8F Pain MG30-MG3Z Approved [16]
(-)-Phenserine DMNCY1I Alzheimer disease 8A20 Phase 3 [17]
Plasma derived human butyrylcholinesterase DMF3IBC Neurotoxicity NE61 Phase 1 [18]
Protexia DME1Y9W Alzheimer disease 8A20 Phase 1 [19]
JES-9501 DMYR3IE Alzheimer disease 8A20 Phase 1 [20]
Tetra-hydro-isoquinoline derivative 3 DMCZA45 N. A. N. A. Patented [21]
Tetra-hydro-isoquinoline derivative 1 DML86IO N. A. N. A. Patented [21]
Tetra-hydro-isoquinoline derivative 2 DM5CKVF N. A. N. A. Patented [21]
Tetra-hydro-isoquinoline derivative 4 DMDV0MP N. A. N. A. Patented [21]
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [22]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [23]
Galantamine DMEO794 Alzheimer disease 8A20 Approved [24]
Rivastigmine DMG629M Alzheimer disease 8A20 Approved [25]
Donepezil DMIYG7Z Advanced cancer 2A00-2F9Z Approved [4]
Succinylcholine DM2ET1M Plasma cell myeloma 2A83.1 Approved [26]
Ethopropazine DM0N3L7 Parkinson disease 8A00.0 Approved [23]
Dimenhydrinate DM264B3 Meniere disease AB31.0 Approved [27]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [28]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [27]
⏷ Show the Full List of 20 Drug(s)
Drug(s) Affected By Acetylcholinesterase (ACHE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetylcholine DMDF79Z Cataract 9B10 Approved [29]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [30]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [31]
Methotrexate DM2TEOL Anterior urethra cancer Approved [32]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [33]
L-Glutamic Acid DM4PUDW Schizophrenia 6A20 Approved [31]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [34]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [35]
Neostigmine DM6T2J3 Myasthenia gravis 8C6Y Approved [36]
Testosterone DM7HUNW Hot flushes GA30 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 [1]
Cholinesterase (BCHE) TTEB0GD CHLE_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Acetylcholinesterase (ACHE) OT2H8HG6 ACES_HUMAN Gene/Protein Processing [3]
Cholinesterase (BCHE) OTOH3WQ9 CHLE_HUMAN Drug Response [4]

References

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2 Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. J Med Chem. 2006 Apr 6;49(7):2174-85.
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4 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
5 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.
6 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).
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9 Huperzine A attenuates cognitive deficits and brain injury in neonatal rats after hypoxia-ischemia. Brain Res. 2002 Sep 13;949(1-2):162-70.
10 Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet. J Sep Sci. 2009 May;32(10):1748-56.
11 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
12 Alpha6-containing nicotinic acetylcholine receptors dominate the nicotine control of dopamine neurotransmission in nucleus accumbens. Neuropsychopharmacology. 2008 Aug;33(9):2158-66.
13 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.
14 Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. Chem Biol. 2003 Jun;10(6):491-502.
15 Synergistic effect of acidosis and succinylcholine-induced hyperkalemia in spinal cord transected rats. Acta Anaesthesiol Scand. 1984 Feb;28(1):87-90.
16 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.
17 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.
18 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.
19 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.
20 Dehydroevodiamine attenuates beta-amyloid peptide-induced amnesia in mice. Eur J Pharmacol. 2001 Feb 16;413(2-3):221-5.
21 A patent review of butyrylcholinesterase inhibitors and reactivators 2010-2017.Expert Opin Ther Pat. 2018 Jun;28(6):455-465.
22 Increased organophosphate scavenging in a butyrylcholinesterase mutant. Chem Biol Interact. 2008 Sep 25;175(1-3):376-9. doi: 10.1016/j.cbi.2008.04.012. Epub 2008 Apr 22.
23 Comparative effects of cationic triarylmethane, phenoxazine and phenothiazine dyes on horse serum butyrylcholinesterase. Arch Biochem Biophys. 2008 Oct 15;478(2):201-5.
24 Lichens of parmelioid clade as promising multitarget neuroprotective agents. Chem Res Toxicol. 2019 Jun 17;32(6):1165-1177.
25 Potencies and selectivities of inhibitors of acetylcholinesterase and its molecular forms in normal and Alzheimer's disease brain. Acta Biol Hung. 2003;54(2):183-9. doi: 10.1556/ABiol.54.2003.2.7.
26 Response of the newborn to succinlycholine injection in homozygotic atypical mothers. Anesthesiology. 1975 Jul;43(1):115-6. doi: 10.1097/00000542-197507000-00028.
27 Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: analysis of its postulated role in synergizing organophosphate toxicity. Toxicol Appl Pharmacol. 1975 Feb;31(2):179-90.
28 Qualitative defects of pseudocholinesterase activity. Anaesthesia. 1967 Jan;22(1):55-68.
29 Monitoring the reaction of carbachol with acetylcholinesterase by thioflavin T fluorescence and acetylthiocholine hydrolysis. Chem Biol Interact. 2008 Sep 25;175(1-3):235-41. doi: 10.1016/j.cbi.2008.06.002. Epub 2008 Jun 17.
30 Effect of reversible ligands on oxime-induced reactivation of sarin- and cyclosarin-inhibited human acetylcholinesterase. Toxicol Lett. 2015 Feb 3;232(3):557-65.
31 Dihydroactinidiolide regulates Nrf2/HO-1 expression and inhibits caspase-3/Bax pathway to protect SH-SY5Y human neuroblastoma cells from oxidative stress induced neuronal apoptosis. Neurotoxicology. 2021 May;84:53-63. doi: 10.1016/j.neuro.2021.02.006. Epub 2021 Feb 20.
32 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
33 Tribromophenol induces the differentiation of SH-SY5Y human neuroblastoma cells in vitro. Toxicol In Vitro. 2003 Oct-Dec;17(5-6):635-41. doi: 10.1016/s0887-2333(03)00110-3.
34 Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changes. Eur J Pharmacol. 1989 Nov 28;173(1):53-64. doi: 10.1016/0014-2999(89)90008-3.
35 Interaction of dichlorvos and anticholinesterases on the in vitro inhibition of human blood cholinesterases. Toxicol Appl Pharmacol. 1974 Feb;27(2):456-63.
36 Hairy-root organ cultures for the production of human acetylcholinesterase. BMC Biotechnol. 2008 Dec 23;8:95.
37 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.