U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C13H14N2.ClH.H2O
Molecular Weight 252.74
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TACRINE HYDROCHLORIDE MONOHYDRATE

SMILES

O.Cl.NC1=C2CCCCC2=NC3=C1C=CC=C3

InChI

InChIKey=PXGRMZYJAOQPNZ-UHFFFAOYSA-N
InChI=1S/C13H14N2.ClH.H2O/c14-13-9-5-1-3-7-11(9)15-12-8-4-2-6-10(12)13;;/h1,3,5,7H,2,4,6,8H2,(H2,14,15);1H;1H2

HIDE SMILES / InChI
Molecular Formula C13H14N2
Molecular Weight 198.2637
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/pro/cognex.html

Tacrine is a parasympathomimetic- a reversible cholinesterase inhibitor that is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine at cholinergic synapses through reversible inhibition of its hydrolysis by acetylcholinesterase. If this proposed mechanism of action is correct, tacrine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact. There is no evidence that tacrine alters the course of the underlying dementing process. The mechanism of tacrine is not fully known, but it is suggested that the drug is an anticholinesterase agent which reversibly binds with and inactivates cholinesterases. This inhibits the hydrolysis of acetylcholine released from functioning cholinergic neurons, thus leading to an accumulation of acetylcholine at cholinergic synapses. The result is a prolonged effect of acetylcholine. is used for the palliative treatment of mild to moderate dementia of the Alzheimer's type. Tacrine was marketed under the trade name Cognex. Because of its liver toxicity and attendant requirement for monitoring liver function, tacrine prescriptions dropped after other acetylcholinesterase inhibitors were introduced, and its use has been largely discontinued.

CNS Activity

Originator

Warner-Lambert
23
Curator's Comment: Originally developed by Warner-Lambert Co.

Approval Year

1993
136
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 500.0 nM [IC50]
Inhibitor
8297
 23.0 nM [IC50]
Inhibitor
8297
 0.46 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
Cognex

Approved Use

Cognex® (tacrine hydrochloride capsules) is indicated for the treatment of mild to moderate dementia of the Alzheimer's type.

Launch Date

7.474464E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
15.8 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/7836549
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TACRINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
91.8 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/7836549
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TACRINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.8 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/7836549
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TACRINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (21 patient)
Vomiting (21 patient)
Anorexia (21 patient)
Dyspepsia (21 patient)
Diarrhea (21 patient)
Abdominal pain (21 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 146
Health Status: unhealthy
Age Group: adult
Population Size: 146
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Disc. AE: Transaminases increased, Atrial fibrillation...
AEs leading to
discontinuation/dose reduction:
Transaminases increased (1 patient)
Atrial fibrillation (1 patient)
Dyspnea (1 patient)
Chest pain (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Disc. AE: Transaminases increased, Nausea...
AEs leading to
discontinuation/dose reduction:
Transaminases increased (1 patient)
Nausea (1 patient)
Vomiting (1 patient)
Pallor (1 patient)
Vasodilatation (1 patient)
Sweating increased (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
AEs

AEs

AESignificanceDosePopulation
Abdominal pain 21 patient
Disc. AE
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Anorexia 21 patient
Disc. AE
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Diarrhea 21 patient
Disc. AE
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Dyspepsia 21 patient
Disc. AE
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Nausea 21 patient
Disc. AE
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Vomiting 21 patient
Disc. AE
160 mg 1 times / day multiple, oral
Highest studied dose
Dose: 160 mg, 1 times / day
Route: oral
Route: multiple
Dose: 160 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
unhealthy, 71.2 years (range: 52-88 years)
n = 64
Health Status: unhealthy
Condition: Alzheimer's disease
Age Group: 71.2 years (range: 52-88 years)
Sex: M+F
Population Size: 64
Sources:
https://pubmed.ncbi.nlm.nih.gov/9236571
https://pubmed.ncbi.nlm.nih.gov/8139083
Atrial fibrillation 1 patient
Disc. AE
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 146
Health Status: unhealthy
Age Group: adult
Population Size: 146
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Chest pain 1 patient
Disc. AE
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 146
Health Status: unhealthy
Age Group: adult
Population Size: 146
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Dyspnea 1 patient
Disc. AE
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 146
Health Status: unhealthy
Age Group: adult
Population Size: 146
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Transaminases increased 1 patient
Disc. AE
40 mg 1 times / day multiple, oral
Recommended
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 146
Health Status: unhealthy
Age Group: adult
Population Size: 146
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Nausea 1 patient
Disc. AE
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Pallor 1 patient
Disc. AE
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Sweating increased 1 patient
Disc. AE
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Transaminases increased 1 patient
Disc. AE
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Vasodilatation 1 patient
Disc. AE
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Vomiting 1 patient
Disc. AE
80 mg 1 times / day multiple, oral
Recommended
Dose: 80 mg, 1 times / day
Route: oral
Route: multiple
Dose: 80 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
unhealthy, adult
n = 150
Health Status: unhealthy
Age Group: adult
Population Size: 150
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020070ap.pdf
Page: p. 5
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1054

OCT1
327

OCT3
80

OCTN2
50

P-gp
1537
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
1537
 inconclusive
CYP1A2
1054
 yes
OCT1
327
 yes
OCT3
80
 yes
OCTN2
50
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:45980
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:45980
ChemicalBook
CB7699634
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7699634
MolPort
MolPort-000-881-472
https://www.molport.com/shop/molecule-link/MolPort-000-881-472
ZINC
ZINC000019014866
http://zinc15.docking.org/substances/ZINC000019014866
eMolecules
872890
https://www.emolecules.com/cgi-bin/more?vid=872890
PubMed

PubMed

TitleDatePubMed
Ketamine-induced postanesthetic delirium attenuated by tetrahydroaminoacridine.
1974 Jul
Suxamethonium apnoea masked by tetrahydroaminacrine.
1978 Jul-Aug
Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changes.
1989 Nov 28
Effects of four non-cholinergic cognitive enhancers in comparison with tacrine and galanthamine on scopolamine-induced amnesia in rats.
1992
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
1992 Mar 20
Tacrine inhibits ventricular fibrillation induced by ischaemia and reperfusion and widens QT interval in rat.
1993 Mar
Antiamnesic and cholinomimetic side-effects of the cholinesterase inhibitors, physostigmine, tacrine and NIK-247 in rats.
1993 Nov 30
Severe parkinsonian symptom development on combination treatment with tacrine and haloperidol.
1995 Aug
Systemic administration of lithium chloride and tacrine but not kainic acid augments citrulline content of rat brain.
1995 Dec 27
Delirium caused by tacrine and ibuprofen interaction.
1996 Jun
Adverse interaction of tacrine and haloperidol.
1996 Nov
Sleep-wake mechanisms and drug discovery: sleep EEG as a tool for the development of CNS-acting drugs.
2002 Dec
Nicotine and sensory memory in Alzheimer's disease: an event-related potential study.
2002 Jul
The evaluation of cognitive function in the dementias: methodological and regulatory considerations.
2003 Mar
Inhibition of murine cytochrome P4501A by tacrine: in vitro studies.
2004 Aug
Cholinesterase inhibitors modify the activity of intrinsic cardiac neurons.
2004 Aug
[Study of the cholinesterase active site using a fluorescent probe].
2004 Mar-Apr
In vitro inactivation of rat brain acetylcholinesterase by DSP-4 and its derivatives OS-21 and OS-23 and protective activity of tacrine (9-amino-1,2,3,4-tetrahydroacridine).
2005
Validation of the tremulous jaw movement model for assessment of the motor effects of typical and atypical antipychotics: effects of pimozide (Orap) in rats.
2005 Feb
Cholinergic drugs potentiate human nicotinic alpha4beta2 acetylcholine receptors by a competitive mechanism.
2005 Feb 21
Prediction of genotoxicity of chemical compounds by statistical learning methods.
2005 Jun
2006 Jun
Identification of various allosteric interaction sites on M1 muscarinic receptor using 125I-Met35-oxidized muscarinic toxin 7.
2006 May
Progress update: Pharmacological treatment of Alzheimer's disease.
2007
Heterologous amyloid seeding: revisiting the role of acetylcholinesterase in Alzheimer's disease.
2007 Jul 25
Allosteric modulation of muscarinic acetylcholine receptors.
2007 Sep
The investigation of structure-activity relationships of tacrine analogues: electronic-topological method.
2008 Aug 6
Pharmacologic profiling of human and rat cytochrome P450 1A1 and 1A2 induction and competition.
2008 Dec
Dose-related effects of the acetylcholinesterase inhibitor tacrine on cocaine and food self-administration in rats.
2008 Jan
1-Phenyl-6,7,8,9-hexa-hydro-1H,5H-cyclo-hepta-[1',2':2,3]pyrido[6,5-c]pyrazol-4-amine: a new tacrine analogue.
2008 May 10
New performance of biosensor technology for Alzheimer's disease drugs: in vitro comparison of tacrine and 7-methoxytacrine.
2008 Oct
A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model.
2008 Oct
Study of neuroprotection of donepezil, a therapy for Alzheimer's disease.
2008 Sep 25
Comparison studies of tacrine and bis7-tacrine on the suppression of scopolamine-induced behavioral changes and inhibition of acetylcholinesterase in mice.
2009
The 5-choice continuous performance test: evidence for a translational test of vigilance for mice.
2009
Cholinergic influence on memory stages: A study on scopolamine amnesic mice.
2009 Aug
Rapid determination of tacrine and other drug metabolites in microsomal incubate by newly developed targeting algorithm on UHPLC/TOFMS.
2009 Dec 15
Effects of zonisamide on c-Fos expression under conditions of tacrine-induced tremulous jaw movements in rats: a potential mechanism underlying its anti-parkinsonian tremor effect.
2009 Jan
Identification of FDA-approved drugs and bioactives that protect hair cells in the zebrafish (Danio rerio) lateral line and mouse (Mus musculus) utricle.
2009 Jun
An integrated approach to improved toxicity prediction for the safety assessment during preclinical drug development using Hep G2 cells.
2009 Jun 1
Long-lasting decreases in cocaine-reinforced behavior following treatment with the cholinesterase inhibitor tacrine in rats selectively bred for drug self-administration.
2009 Nov
Coupling an HCN2-expressing cell to a myocyte creates a two-cell pacing unit.
2009 Nov 1
Contribution of the d-Serine-Dependent Pathway to the Cellular Mechanisms Underlying Cognitive Aging.
2010
Use of angiotensin receptor blockers and risk of dementia in a predominantly male population: prospective cohort analysis.
2010 Jan 12
Development of a highly sensitive cytotoxicity assay system for CYP3A4-mediated metabolic activation.
2011 Aug
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
2011 Jul 14
Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model.
2013 Dec
Inhibition of human carboxylesterases hCE1 and hiCE by cholinesterase inhibitors.
2013 Mar 25
A correlation between the in vitro drug toxicity of drugs to cell lines that express human P450s and their propensity to cause liver injury in humans.
2014 Jan
N-palmitoyl serotonin alleviates scopolamine-induced memory impairment via regulation of cholinergic and antioxidant systems, and expression of BDNF and p-CREB in mice.
2015 Dec 5
Patents

Patents

05013741
3
JP2003512428A
9
JP2004315496A
25
JP2007508336A
3
JP4722295B2
104
JPH0366670A
3
JPH0820577A
3

Sample Use Guides

In Vivo Use Guide
Oral Initially, 10 mg 4 times daily for at least 4 weeks. If well tolerated and increased serum ALT concentrations have not occurred, increase dosage to 20 mg 4 times daily; if tolerated, increase dosage in 40-mg daily increments (divided into 4 doses daily) at 4-week intervals up to a maximum of 160 mg daily (40 mg 4 times daily).
Route of Administration: Oral
In Vitro Use Guide
Tacrine (0.01-10 uM) inhibited both human and rat HNMT activity in a concentration-dependent manner, but was less potent on both human embryonic kidney and recombinant human brain HNMT than on rat kidney HNMT (IC50 values were 0.46 and 0.70 uM vs. 0.29 uM, respectively).
Substance Class Chemical
Created
by admin
on Sat Dec 16 05:54:51 UTC 2023
Edited
by admin
on Sat Dec 16 05:54:51 UTC 2023
Record UNII
MQ603P8SBL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TACRINE HYDROCHLORIDE MONOHYDRATE
Common Name English
9-ACRIDINAMINE, 1,2,3,4-TETRAHYDRO-, HYDROCHLORIDE, HYDRATE (1:1:1)
Systematic Name English
9-ACRIDINAMINE, 1,2,3,4-TETRAHYDRO-, MONOHYDROCHLORIDE, MONOHYDRATE
Common Name English
Code System Code Type Description
FDA UNII
MQ603P8SBL
Created by admin on Sat Dec 16 05:54:51 UTC 2023 , Edited by admin on Sat Dec 16 05:54:51 UTC 2023
PRIMARY
EPA CompTox
DTXSID80221711
Created by admin on Sat Dec 16 05:54:51 UTC 2023 , Edited by admin on Sat Dec 16 05:54:51 UTC 2023
PRIMARY
PUBCHEM
6420002
Created by admin on Sat Dec 16 05:54:52 UTC 2023 , Edited by admin on Sat Dec 16 05:54:52 UTC 2023
PRIMARY
CAS
7149-50-0
Created by admin on Sat Dec 16 05:54:51 UTC 2023 , Edited by admin on Sat Dec 16 05:54:51 UTC 2023
PRIMARY
Related Record Type Details
Structure of TACRINE
PARENT -> SALT/SOLVATE
Structure of TACRINE HYDROCHLORIDE
ANHYDROUS->SOLVATE
Related Record Type Details
Structure of TACRINE
ACTIVE MOIETY
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