116765 Adenosine A2A/A₁ Receptor Antagonist - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₃H₂₂N₄O₃ •2HCl

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116765-10MG
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      Glass bottle 10 mg
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      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.