| Identification | Back Directory | [Name]
Dizocilpine | [CAS]
77086-21-6 | [Synonyms]
C13737
Dizocilpine
MK-801 (Dizocilpine)
Dizocilpine USP/EP/BP
Dizocilpine free base(MK801)
(5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine
[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-
[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5α,10α-imine | [Molecular Formula]
C16H15N | [MDL Number]
MFCD06412575 | [MOL File]
77086-21-6.mol | [Molecular Weight]
221.3 |
| Hazard Information | Back Directory | [Uses]
Neuroprotective. | [Definition]
ChEBI: Dizocilpine is an organic heterotetracyclic compound that is 1-methyl-8-azabicyclo[3.2.1]octane ortho-fused to two benzene rings at positions 2-3 and 6-7 (the 5S,10R-stereoisomer). It is a non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor and affects cognitive function, learning, and memory. It has a role as a NMDA receptor antagonist, an anaesthetic, an anticonvulsant, a nicotinic antagonist and a neuroprotective agent. It is a secondary amino compound and a tetracyclic antidepressant. It is a conjugate base of a dizocilpine(1+). | [in vivo]
Dizocilpine maleate can be used to create schizophrenia models. An intraperitoneal injection of 0.2 mg/kg in SD rats results in a half-life of 52.31 minutes, an AUC of 3185.48 nM·min, and a clearance rate of 34 mL/min/kg[2].
Induction of Schizophrenia
Background
The specific mechanism of schizophrenia induction is unclear. One hypothesis is that, Dizocilpine maleateleads to dysregulation of glutamatergic system through NMDA inhibition[2].
Specific Modeling Methods
Rat: Sprague-Dawley ? male ? adult with weight of 250-300 g
Administration: 0.4 mg/kg ? i.p. ? single dose.
Note
Dizocilpine maleate is dissolved in 0.9% sterile saline.
Modeling Indicators Behavior: Increased spontaneous activity with obvious anxiety-like behavior, increased motor activity in longer diatance (hyperactivity), reduced time staying in central area (avoidance of central area).
Prepulse Inhibition (PPI): Decreased PPI significantly.
maze test:Avoided open arm entries in elevated plus maze test and reduced number of novel arm entries in Y maze test.
Correlated Product(s): Phencyclidine Opposite Product(s): Clozapine (HY-14539); Haloperidol (HY-14538) | [IC 50]
NMDA Receptor |
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