Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H25NO3.ClH |
Molecular Weight | 363.878 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCN(CC)CCOC(=O)C(O)(C1=CC=CC=C1)C2=CC=CC=C2
InChI
InChIKey=ZCEHOOLYWQBGQO-UHFFFAOYSA-N
InChI=1S/C20H25NO3.ClH/c1-3-21(4-2)15-16-24-19(22)20(23,17-11-7-5-8-12-17)18-13-9-6-10-14-18;/h5-14,23H,3-4,15-16H2,1-2H3;1H
Benactyzine, an anticholinergic drug, had been used as an antidepressant in the treatment of depression and associated anxiety. It is no longer used in medicine due to its ineffectiveness but is widely used in scientific research. Benactyzine is a muscarinic antagonist which also inhibits the nicotinic acetylcholine receptor.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094109 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3683366 |
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Target ID: Nicotinic acetylcholine receptor Sources: https://www.ncbi.nlm.nih.gov/pubmed/3683366 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Deprol Approved Usetreatment of depression |
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Primary | Anxiolit plus Approved UseAnxiety states of tension and excitement change of symptoms discomfort of the gastrointestinal tract, the cardiovascular system and the urinary tract due to psychological causes (psychovegetative complaints) |
Doses
Dose | Population | Adverse events |
---|---|---|
1300 mg single, oral Overdose Dose: 1300 mg Route: oral Route: single Dose: 1300 mg Sources: Page: p.86 |
unknown n = 1 |
Disc. AE: Psychosis... AEs leading to discontinuation/dose reduction: Psychosis Sources: Page: p.86 |
200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Sources: Page: p.86 |
healthy n = 1 |
Disc. AE: Delirium... AEs leading to discontinuation/dose reduction: Delirium (severe) Sources: Page: p.86 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Psychosis | Disc. AE | 1300 mg single, oral Overdose Dose: 1300 mg Route: oral Route: single Dose: 1300 mg Sources: Page: p.86 |
unknown n = 1 |
Delirium | severe Disc. AE |
200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Sources: Page: p.86 |
healthy n = 1 |
PubMed
Title | Date | PubMed |
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Meprobamate-benactyzine (Deprol) and placebo in two depressed outpatient populations. | 1969 Mar-Apr |
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[Effect of several neuroleptic, adreno-, sympatho- and cholinolytic substances on the development of experimental cerebral edema induced by nicotine]. | 1977 May-Jun |
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[The possible role of presynaptic effects in realizing the protective action of M-cholinolytics in dimethyl dichlorovinyl phosphate poisoning]. | 1991 Jul-Aug |
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The influence of anticholinergic drug selection on the effectiveness of oximes against soman-induced supralethal poisoning in mice. | 2001 |
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[Effect of diazepam on the effectiveness of antidote therapy in eliminating the acute lethal effects of soman in mice]. | 2001 Aug |
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Effects of advanced candidate anticonvulsants under two rodent models of 'counting'. | 2001 Dec |
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Effects of selected anticholinergics on acoustic startle response in rats. | 2001 Dec |
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Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. | 2001 Feb 1 |
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[Effect of diazepam on antidote therapy of lethal toxic effects of soman in rats]. | 2001 Sep |
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The influence of anticholinergic drug and oxime selection on the effectiveness of antidotal treatment against tabun-induced poisoning in mice. | 2002 |
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A comparison of the efficacy of pyridostigmine alone and the combination of pyridostigmine with anticholinergic drugs as pharmacological pretreatment of tabun-poisoned rats and mice. | 2002 Aug 15 |
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Effect of methoxime combined with anticholinergic, anticonvulsant or anti-HCN drugs in tabun-poisoned mice. | 2003 |
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A comparison of the neuroprotective efficacy of pharmacological pretreatment and antidotal treatment in soman-poisoned rats. | 2003 |
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Neuroprotective efficacy of pharmacological pretreatment and antidotal treatment in tabun-poisoned rats. | 2003 Mar 14 |
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Anticholinergic and antiglutamatergic agents protect against soman-induced brain damage and cognitive dysfunction. | 2003 Sep |
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Therapeutic efficacy of different antidotal mixtures against poisoning with GF-agent in mice. | 2004 |
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Anticholinergic drugs--functional antidotes for the treatment of tabun intoxication. | 2004 |
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Acute experimental tabun-induced intoxication and its therapy in rats. | 2004 Mar |
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Protection and inflammatory markers following exposure of guinea pigs to sarin vapour: comparative efficacy of three oximes. | 2004 Nov-Dec |
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Role of cholinergic structures in individual resistance of rat circulatory system to posthemorrhagic hypoxia. | 2005 Aug |
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Therapeutic and neuroprotective efficacy of pharmacological pretreatment and antidotal treatment of acute tabun or soman poisoning with the emphasis on pretreatment drug PANPAL. | 2006 Dec |
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The influence of oxime and anticholinergic drug selection on the potency of antidotal treatment to counteract acute toxic effects of tabun in mice. | 2006 Jan |
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Protective effect of reversible cholinesterase inhibitors (tacrine, pyridostigmine) and eqbuche against VX poisoning and brain acetylcholinesterase inhibition in rats. | 2008 |
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Anticonvulsant efficacy of drugs with cholinergic and/or glutamatergic antagonism microinfused into area tempestas of rats exposed to soman. | 2008 Feb |
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Efficacy of antidotal treatment against sarin poisoning: the superiority of benactyzine and caramiphen. | 2008 Feb 15 |
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The present approaches to the development of prophylactic and therapeutic antidotes against nerve agents. | 2008 Jun |
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Antiparkinson drugs used as prophylactics for nerve agents: studies of cognitive side effects in rats. | 2008 Jun |
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Role of the cholinergic mechanisms of the ventrolateral preoptic area of the hypothalamus in regulating the state of sleep and waking in pigeons. | 2008 Mar |
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[The sexual function of mature rat males after prenatal modulation of cholinergic system]. | 2008 May |
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Therapy against organophosphate poisoning: the importance of anticholinergic drugs with antiglutamatergic properties. | 2008 Oct 15 |
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Chemical aspects of pharmacological prophylaxis against nerve agent poisoning. | 2009 |
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Sexual function in adult male rats after prenatal modulation of the cholinergic system. | 2009 Jun |
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Paraoxon attenuates vascular smooth muscle contraction through inhibiting Ca2+ influx in the rabbit thoracic aorta. | 2010 |
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[Tolerance of prostate biopsy with use of local anesthesia and benzodiazepines: a randomized, prospective study]. | 2010 Jan |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/13396241
The patient is receiving benactyzine at a dose starting with 1 mg three times a day rising within five days to 2 mg four times a day, and remaining at that level until the end of the test period
Route of Administration:
Oral
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NCI_THESAURUS |
C29704
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SUB00693MIG
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26R628272Q
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m2301
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66448
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C78059
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16339
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DTXSID8052774
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ACTIVE MOIETY
SUBSTANCE RECORD