Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C16H15N |
Molecular Weight | 221.297 |
Optical Activity | ( + ) |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@]12N[C@H](CC3=CC=CC=C13)C4=CC=CC=C24
InChI
InChIKey=LBOJYSIDWZQNJS-CVEARBPZSA-N
InChI=1S/C16H15N/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16/h2-9,15,17H,10H2,1H3/t15-,16+/m1/s1
Molecular Formula | C16H15N |
Molecular Weight | 221.297 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Dizocilpine (MK-801) is an antagonist of the N-methyl-D-aspartate (NMDA) receptor in the glutamate category involved with the central nervous system (CNS). The drug displays a variety of physiological actions, many of which involve the CNS, such as anesthetic and anticonvulsant properties. It penetrates readily into CNS and was described as the agent with central sympathomimetic properties. Co-administration of dizocilpine with psychostimulants, such as cocaine, amphetamine and nicotine, has been reported to prevent the development of behavioural sensitization to these drugs as well as associated neuroadaptations in rodents. However, studies with bromocriptine have suggested that co-administration of dizocilpine might merely cause sensitization to become state-dependent. A single injection of MK-801 to rats models both positive and negative symptoms of schizophrenia. Treatment of mice with dizocilpine induced learning impairment.
CNS Activity
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Low doses of N-methyl-D-aspartate antagonists in superficial laminae of medulla oblongata facilitate wind-up of convergent neurones. | 2001 |
|
Generalisation of ethanol with drug mixtures containing a positive modulator of the GABA(A) receptor and an NMDA antagonist. | 2001 |
|
[3H]acetycholine release in rat striatal slices is not subject to dopamine heteroreceptor supersensitivity 30 months after 6-hydroxydopamine lesion of the substantia nigra. | 2001 Apr |
|
NMDA antagonists produce site-selective impairment of accuracy in a delayed nonmatch-to-sample task in rats. | 2001 Dec |
|
Comparative studies on the memory-enhancing actions of captopril and losartan in mice using inhibitory shock avoidance paradigm. | 2001 Feb |
|
N-methyl-D-aspartate receptor antagonists potentiate the antinociceptive effects of morphine in squirrel monkeys. | 2001 Jul |
|
Two distinct oscillatory states determined by the NMDA receptor in rat inferior olive. | 2001 Jul 1 |
|
Excitatory mechanisms in neuroleptic-induced vacuous chewing movements (VCMs): possible involvement of calcium and nitric oxide. | 2001 Jun |
|
Dizocilpine but not ketamine reduces the volume of ischaemic damage after acute subdural haematoma in the rat. | 2001 May |
|
Glufosinate ammonium induces convulsion through N-methyl-D-aspartate receptors in mice. | 2001 May 18 |
|
Microdialysates of amines and metabolites from core nucleus accumbens of freely moving rats are altered by dizocilpine. | 2001 May 25 |
|
Possible mechanism of anticonvulsant effect of ketamine in mice. | 2001 Oct |
|
Delayed sclerosis, neuroprotection, and limbic epileptogenesis after status epilepticus in the rat. | 2002 |
|
Endogenous excitatory amino acid neurotransmission regulates thyroid-stimulating hormone and thyroid hormone secretion in conscious freely moving male rats. | 2002 Apr |
|
Protection of methylmercury effects on the in vivo dopamine release by NMDA receptor antagonists and nitric oxide synthase inhibitors. | 2002 Apr |
|
Sexually dimorphic effects of morphine and MK-801: sex steroid-dependent and -independent mechanisms. | 2002 Feb |
|
Potentiation of nuclear activator protein-1 DNA binding following brief exposure to N-methyl-D-aspartate in immature cultured rat hippocampal neurons. | 2002 Feb 15 |
|
Prenatal choline supplementation protects against postnatal neurotoxicity. | 2002 Jan 1 |
|
N-Methyl-D-aspartate receptor blockade by dizocilpine prevents stress-induced sudden death in cardiomyopathic hamsters. | 2002 Jul 19 |
|
Cerebral glucose utilization in transgenic mice overexpressing heat shock protein 70 is altered by dizocilpine. | 2002 Mar |
|
Nitric-oxide-synthase-mediated cyclic guanosine monophosphate production in neonatal rat cerebellar prisms is resistant to calcineurin inhibition. | 2002 Mar 29 |
|
Repetitive spreading depression induces nestin protein expression in the cortex of rats and mice. Is this upregulation initiated by N-methyl-D-aspartate receptors? | 2002 Mar 8 |
|
Involvement of dopaminergic system in the nucleus accumbens in the discriminative stimulus effects of phencyclidine. | 2002 May |
|
Relative reinforcing strength of three N-methyl-D-aspartate antagonists with different onsets of action. | 2002 May |
|
NMDA receptor involvement in imipramine withdrawal-associated effects on swim stress, GABA levels and NMDA receptor binding in rat hippocampus. | 2002 May 24 |
|
SR146131, a cholecystokinin-A receptor agonist, antagonizes prepulse inhibition deficits produced by dizocilpine and DOI. | 2002 Nov |
|
Differential effects of direct and indirect dopamine agonists on prepulse inhibition: a study in D1 and D2 receptor knock-out mice. | 2002 Nov 1 |
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 17:58:16 GMT 2025
by
admin
on
Mon Mar 31 17:58:16 GMT 2025
|
Record UNII |
7PY8KH681I
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
EPA PESTICIDE CODE |
605204
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
||
|
WIKIPEDIA |
Designer-drugs-Dizocilpine
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
||
|
WIKIPEDIA |
NMDA receptor antagonist
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
||
|
NCI_THESAURUS |
C264
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
DTXSID3048447
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
SUB06341MIG
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
180081
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
7641
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
7PY8KH681I
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
C65450
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
176788
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
34725
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
m4700
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | Merck Index | ||
|
CHEMBL284237
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
77086-21-6
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
100000081843
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
6320
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY | |||
|
DIZOCILPINE
Created by
admin on Mon Mar 31 17:58:16 GMT 2025 , Edited by admin on Mon Mar 31 17:58:16 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR | |||
|
TRANSPORTER -> INHIBITOR |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|