Dizocilpine

Product Name: Dizocilpine
CAS No.: 77086-21-6
Chemical Name: Dizocilpine
Synonyms: C13737;Dizocilpine;MK-801 (Dizocilpine);Dizocilpine (MK-801);Dizocilpine USP/EP/BP;Dizocilpine free base;Dizocilpine, 10 mM in DMSO;Dizocilpine free base(MK801);(5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine;(5S,10R)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene
CBNumber: CB81075436
Molecular Formula: C16H15N
Formula Weight: 221.3
MOL File: 77086-21-6.mol

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Dizocilpine Property

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)

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Safety

Hazardous Substances Data: 77086-21-6(Hazardous Substances Data)

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Hazard and Precautionary Statements (GHS)

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Dizocilpine Chemical Properties,Usage,Production

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

Dizocilpine Preparation Products And Raw materials

Raw materials

Preparation Products

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Dizocilpine Suppliers

China 67 Germany 1 India 1 United States 7 Global 76

Target molecule Corp.

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View Lastest Price from Dizocilpine manufacturers

Career Henan Chemical Co

Product: Dizocilpine 77086-21-6
Price: US $1.00/KG
Min. Order: 1KG
Purity: 99%HPLC
Supply Ability: 100KG
Release date: 2020-02-05

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(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

[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5α,10α-imine

C13737

MK-801 (Dizocilpine)

5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-

Dizocilpine

Dizocilpine free base(MK801)

Dizocilpine USP/EP/BP

Dizocilpine (MK-801)

noncompetitive,MK 801,Dizocilpine,Ionotropic glutamate receptors,voltage,inhibit,MK801,hyperlocomotion,Inhibitor,iGluR,ambulation,neurotransmitter,anticonvulsant

Dizocilpine free base

(5S,10R)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene

Dizocilpine, 10 mM in DMSO

77086-21-6

Inhibitors