General
Preferred name
dizocilpine
Synonyms
(+)-MK 801 maleate ()
(+)-MK-801 hydrogen maleate ()
(+)-MK 801 (Maleate) ()
Dizocilpine hydrogen maleate ()
MK 801 ()
DIZOCILPINE MALEATE ()
(+)-MK 801 (Maleate)(+)-MK 801 maleate(+)-Mk-801 Hydrogen Maleate ()
Dizocilpine (Maleate) ()
MK-801 (maleate) ()
(+)-Dizocilpine (MK 801) Maleate ()
(+)-MK-801 maleate ()
MK-801 ()
(+)-MK-801 (hydrogen maleate) ()
P&D ID
PD010545
CAS
77086-22-7
77086-21-6
Tags
drug candidate
natural product
available
Drug indication
Cerebrovascular ischaemia
Neuroprotective
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Potent vanilloid receptor agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Highly potent and selective non-competitive NMDA glutamate receptor antagonist
(LOPAC library)
DESCRIPTION
Non-competitive NMDA antagonist, acts at ion channel site
(Tocriscreen Total)
DESCRIPTION
Non-competitive NMDA antagonist; acts at ion channel site
(Tocriscreen Plus)
DESCRIPTION
(-)-MK-801 maleate is a potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM that acts at the NMDA receptor-operated ion channel as an open channel blocker. It blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. It anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions in test rats. It were used to treat hyperalgesia in the diabetic neuropathic pain (DNP). It is used in various ischemia treatments. It has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
4
Compound Sets
20
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
44
Molecular Weight
221.12
Hydrogen Bond Acceptors
1
Hydrogen Bond Donors
1
Rotatable Bonds
0
Ring Count
4
Aromatic Ring Count
2
cLogP
3.15
TPSA
12.03
Fraction CSP3
0.25
Chiral centers
2.0
Largest ring
6.0
QED
0.72
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Selectivity
NMDA
Pathway
Neuroscience
Membrane Transporter/Ion Channel
Neuronal Signaling
Target
NMDA Receptor
GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D
iGluR
Primary Target
NMDA Receptors
MOA
NMDAR
Antagonist
glutamate receptor antagonist
Solubility
DMSO: > 20 mg/mL, H2O: 6 mg/mL
Source data
