ChemicalBook CAS DataBase List 77086-21-6

77086-21-6

Name	Dizocilpine
CAS	77086-21-6
Molecular Formula	C16H15N
MDL Number	MFCD06412575
Molecular Weight	221.3
MOL File	77086-21-6.mol

Chemical Properties

Melting point	68.5-69°
alpha	20589 +161.4° (c = 0.038 g/2 ml ethanol)
Boiling point	320.3±11.0 °C(Predicted)
density	1.144±0.06 g/cm3(Predicted)
solubility	Soluble in DMSO > 10 mM
form	Powder
pka	7.96±0.40(Predicted)
color	White to off-white
EPA Substance Registry System	5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)- (77086-21-6)

Safety Data

Hazardous Substances Data

77086-21-6(Hazardous Substances Data)

Hazard Information

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

Spectrum Detail

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