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116765 Adenosine A2A/A₁ Receptor Antagonist - Calbiochem

116765
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₂₂N₄O₃ •2HCl

Products

Catalogue NumberPackaging Qty/Pack
116765-10MG Glass bottle 10 mg
Description
OverviewA blood-brain barrier-permeant indenopyrimidinone that acts as a dual A1/A2A antagonist (Ki = 48.2 and 6.5 nM, respectively, against agonist-induced cAMP response in A1- or A2A-expressing CHO-K1 cells) and effectively reverses D2 antagonist haloperidol- (1 mg/kg; s.c.) induced catalepsy in both rats and mice (ED50 = 0.3 and <0.1 mg/kg, respectively) in vivo by simultaneously reversing A1-mediated inhibition of DA (Dopamine) release and A2A-dependent inhibition of D2 receptor response to DA.
Catalogue Number116765
Brand Family Calbiochem®
Synonyms2-Amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]-pyrimidin-5-one, diHCl
References
ReferencesShook, B.C., et al. 2012. J. Med. Chem. 55, 1402.
Product Information
FormLight yellow solid
Hill FormulaC₂₃H₂₂N₄O₃ •2HCl
Chemical formulaC₂₃H₂₂N₄O₃ •2HCl
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Adenosine A2A/A₁ Receptor Antagonist - Calbiochem Certificates of Analysis

TitleLot Number
116765

References

Reference overview
Shook, B.C., et al. 2012. J. Med. Chem. 55, 1402.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision24-September-2012 JSW
Synonyms2-Amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]-pyrimidin-5-one, diHCl
DescriptionA blood-brain barrier-permeant indenopyrimidinone compound that acts as a dual A1/A2A antagonist (Ki = 48.2 and 6.5 nM, respectively, against agonist-induced cAMP response in A1- or A2A-expressing CHO-K1 cells) and effectively reverses neuroleptic D2 receptor antagonist haloperidol- (1 mg/kg; s.c.) induced catalepsy in both mice (by 85% and 100%, respectively, with 0.1 mg/kg or 1 mg/kg oral dosage 30 min after haloperidol) and rats (by 88% and 97%, respectively, with 1 mg/kg or 10 mg/kg oral dosage) in vivo by simultaneously reversing A1-mediated inhibition of DA (Dopamine) release and A2A-dependent inhibition of D2 receptor response to DA.
FormLight yellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₃H₂₂N₄O₃ •2HCl
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml; clear, yellow solution)
Storage +2°C to +8°C
Hygroscopic
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesShook, B.C., et al. 2012. J. Med. Chem. 55, 1402.