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Drug-Target Interaction

Drug

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PubChem ID:4054
Structure:
Synonyms:
1,3-Dimethyl-5-adamantanamine
1-Amino-3,5-dimethyladamantane
19982-08-2
3,5-Dimethyl-1-adamantanamine
3,5-Dimethyl-1-adamantylamine
3,5-dimethyladamantan-1-amine
3,5-Dimethyladamantan-1-ylamine
3,5-dimethyladamantanylamine
3,5-Dimethyltricyclo(3.3.1.1(3,7))decan-1-amine
3,5-dimethyltricyclo[3.3.1.1~3,7~]decan-1-amine
41100-52-1
41100-52-1 (Hydrochloride)
51052-62-1
AB00053600
AC1L1HB7
AIDS-002464
AIDS002464
AKOS000113995
BBL000737
Biomol-NT_000209
BPBio1_001117
BPBio1_001270
BSPBio_001015
C12H21N
C13736
CBMicro_020348
CCG-204092
CHEBI:152523
CHEMBL807
D-145
D08174
D145
DB01043
DivK1c_000068
DMAA
DRG-0267
Ebixa
EU-0053634
Exiba (TN)
HMS500D10
HSDB 7327
IDI1_000068
KBio1_000068
KBio2_001087
KBio2_003655
KBio2_006223
KBio3_001926
KBioGR_001543
KBioSS_001087
Lopac0_000861
LS-157051
Memantin
Memantina
Memantina [INN-Spanish]
Memantine
Memantine (INN)
Memantine HCL
MEMANTINE HYDROCHLORIDE
Memantine [INN:BAN]
Memantine [INN]
Memantinum
Memantinum [INN-Latin]
Namenda
NCGC00015705-03
NCGC00015705-04
NCGC00015705-05
NCGC00024782-02
NCGC00024782-03
NINDS_000068
Oprea1_480562
Prestwick0_000978
Prestwick1_000978
Prestwick2_000978
Prestwick3_000978
SPBio_001456
SPBio_002926
Spectrum2_001408
Spectrum3_000923
Spectrum4_001022
Spectrum5_001355
Spectrum_000607
ST057652
STK520682
Tricyclo(3.3.1.1(3,7))decan-1-amine, 3,5-dimethyl-
Tricyclo(3.3.1.13,7)decan-1-amine, 3,5-dimethyl-
UNII-W8O17SJF3T
ZERO/006024
ATC-Codes:
Side-Effects:
Side-EffectFrequency
cataract1.0
conjunctivitis1.0
transient ischemic attack1.0
pneumonia1.0
vertigo1.0
cardiac failure1.0
ataxia1.0
cerebrovascular accident1.0
syncope1.0
anemia1.0
rash0.505
dizziness0.07
headache0.06
confusion0.06
constipation0.05
hypertension0.04
coughing0.04
somnolence0.03
hallucination0.03
vomiting0.03
back pain0.03
pain0.02
dyspnea0.02
fatigue0.02
neuralgia0.01
pulmonary embolism0.01
nervousness0.01
paroniria0.01
neurosis0.01
personality disorder0.01
pulmonary edema0.01
psychosis0.01
pruritus0.01
ptosis0.01
paresthesia0.01
retinal detachment0.01
retinal hemorrhage0.01
decreased hearing0.01
sleep disorder0.01
neuropathy0.01
blurred vision0.01
parkinson0.01
esophageal ulceration0.01
eye pain0.01
urinary retention0.01
urticaria0.01
tremor0.01
tinnitus0.01
thrombophlebitis0.01
bradycardia0.01
suicide attempt0.01
skin ulceration0.01
allergic reaction0.01
myopia0.01
amnesia0.01
diverticulitis0.01
diplopia0.01
diabetes mellitus0.01
dermatitis0.01
delirium0.01
dehydration0.01
corneal opacity0.01
convulsions0.01
cerebral hemorrhage0.01
cellulitis0.01
blepharitis0.01
atrial fibrillation0.01
asthma0.01
apnea0.01
aphasia0.01
angina pectoris0.01
dysuria0.01
eczema0.01
myocardial infarction0.01
melena0.01
macula lutea degeneration0.01
leukopenia0.01
hypothermia0.01
postural hypotension0.01
hypotension0.01
hyponatremia0.01
hemorrhage0.01
hemoptysis0.01
gastroenteritis0.01
gastrointestinal hemorrhage0.01
glaucoma0.01
alopecia0.01
cardiac arrest0.01
hematuria0.01
hemiplegia0.01
thrombocytopenia0
otitis media0
tachycardia0
coma0
loss of consciousness0
acute pancreatitis0
av block0
hypoglycemia0
tardive dyskinesia0
anorexia0
dysphagia0
peripheral edema0
grand mal0
hepatitis0
cerebral infarction0
cholelithiasis0
apathy0
emotional lability0
depersonalization0
thinking abnormal0
stupor0
upper respiratory tract infection0
arthralgia0
anxiety0
sepsis0
carpal tunnel syndrome0
insomnia0
claudication0
delusions0
influenza0
acute renal failure0
organic brain syndrome0
colitis0
hepatic failure0
gastroesophageal reflux0
renal insufficiency0
chest pain0
urinary incontinence0
stevens - johnson syndrome0
urinary tract infection0
impotence0
acne0
supraventricular tachycardia0
nausea0
deep vein thrombosis0
hyperglycemia0
abnormal gait0
hyperlipidemia0
dyskinesia0
agitation0
malaise0
lymphatic disorders0
intracranial hemorrhage0
encephalopathy0
bronchitis0
diarrhea0
aspiration pneumonia0
asthenia0
gastritis0

Target

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Uniprot ID:ACES_RAT
Synonyms:
Acetylcholinesterase
AChE
EC-Numbers:3.1.1.7
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

17188316
Neuronal oxidative injury and dendritic damage induced by carbofuran: protection by memantine.. Ramesh C Gupta; Snjezana Milatovic; Wolf-D Dettbarn; Michael Aschner; Dejan Milatovic (2007) Toxicology and applied pharmacology display abstract
Carbamate insecticides mediate their neurotoxicity by acetylcholinesterase (AChE) inactivation. Male Sprague-Dawley rats acutely intoxicated with the carbamate insecticide carbofuran (1.5 mg/kg, sc) developed hypercholinergic signs within 5-7 min of exposure, with maximal severity characterized by seizures within 30-60 min, lasting for about 2 h. At the time of peak severity, compared with controls, AChE was maximally inhibited (by 82-90%), radical oxygen species (ROS) markers (F(2)-isoprostanes, F(2)-IsoPs; and F(4)-neuroprostanes, F(4)-NeuroPs) were elevated 2- to 3-fold, and the radical nitrogen species (RNS) marker citrulline was elevated 4- to 8-fold in discrete brain regions (cortex, amygdala, and hippocampus). In addition, levels of high-energy phosphates (HEPs) were significantly reduced (ATP, by 43-56%; and phosphocreatine, by 37-48%). Values of total adenine nucleotides and total creatine compounds declined markedly (by 41-56% and 35-45%, respectively), while energy charge potential remained unchanged. Quantitative morphometric analysis of pyramidal neurons of the hippocampal CA1 region revealed significant decreases in dendritic lengths (by 64%) and spine density (by 60%). Pretreatment with the N-methyl-D-aspartate (NMDA) receptor antagonist memantine (18 mg/kg, sc), in combination with atropine sulfate (16 mg/kg, sc), significantly attenuated carbofuran-induced changes in AChE activity and levels of F(2)-IsoPs and F(4)-NeuroPs, declines in HEPs, as well as the alterations in morphology of hippocampal neurons. MEM and ATS pretreatment also protected rats from carbofuran-induced hypercholinergic behavioral activity, including seizures. These findings support the involvement of ROS and RNS in seizure-induced neuronal injury and suggest that memantine by preventing carbofuran-induced neuronal hyperactivity blocks pathways associated with oxidative damage in neurons.