Basic information Safety Supplier Related

Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI)

Basic information Safety Supplier Related

Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI) Basic information

Product Name:
Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI)
Synonyms:
  • Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI)
  • Eglumegad
  • Eglumetad
  • LY 354740
  • (1S,2S,5R,6S)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
  • Bicyclo[3.1.0]hexane-2,6-dicarboxylicacid, 2-aMino-, [1S-(1a,2b,5a,6a)]-
  • Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid,2-amino-,(1S,2S,5R,6S)-
  • Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S...
CAS:
176199-48-7
MF:
C8H11NO4
MW:
185.18
Product Categories:
  • CYCLOPENTANE
  • Glutamate
Mol File:
176199-48-7.mol
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Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI) Chemical Properties

Melting point:
270-271 °C
Boiling point:
376.4±32.0 °C(Predicted)
Density 
1.569
storage temp. 
Keep in dark place,Sealed in dry,2-8°C
solubility 
H2O : 6.33 mg/mL (34.18 mM; Need ultrasonic and warming)
form 
Powder
pka
2.06±0.40(Predicted)
color 
White to off-white
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Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI) Usage And Synthesis

Uses

Treatment ofgeneral anxiety disorders and smoking cessation (metabotropic glutamate agonist).

Uses

LY 354740 is a highly selective and potent agonist of group II mGluR.

Definition

ChEBI: Eglumetad is a L-alpha-amino acid.

Biological Activity

Highly selective and potent agonist of group II mGlu receptors (EC 50 values are 5.1 and 24.3 nM at mGlu 2 and mGlu 3 receptors respectively and > 100000 nM at mGlu 4 , mGlu 7 , mGlu 1a and mGlu 5a receptors). Displays antianxiety and antiaddictive activity in vivo . Orally and systemically active.

in vivo

Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) has no effect on spatial working memory performance in Gria1 / or WT mice, and it has no effect on rewarded alternation testing with a short inter-trial interval in Gria1 / and WT mice at concentration of 30 mg/kg. Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) reduces spontaneous locomotor activity in wild-type and Gria1 / mice[1]. Eglumegad (LY354740) (15 mg/kg, i.p.) dreases novelty-induced hyperlocomotion in naive GluA1-KO and pre-handled GluA1-KO males, but not in females. Eglumegad (LY354740) (15 mg/kg, i.p.) significantly reduces the increased c-Fos expression of GluA1-KO males to the level of WT males, but not in of females[3]. Eglumegad (LY354740) (10 mg/kg, i.p.) attenuates the immobilization stress-induced increase in BDNF mRNA expression in the rat mPFC[4].

IC 50

mGluR2R: 5 nM (IC50); mGluR3R: 24 nM (IC50)

storage

+4°C

Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)- (9CI)Supplier

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