Regadenoson

SKU: orb1225339

Description

Regadenoson is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 313348-27-5
• MW: 390.35
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₈N₈O₅
• SMILES: CNC(=O)C1=CN(N=C1)C2=NC3=C(C(=N2)N)N=CN3[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O
• Target: Adenosine Receptor
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  Animal model: Mongrel dogs (23-27 kg). Dosage: 0.1, 0.175, 0.25, 0.5, 1.0, 2.5, 5 μg/kg. Administration: Peripheral intravenous injection; single. Result: Increased mean CBF (coronary blood flow) in a dose-dependent manner, with an ED50 of 0.34 μg/kg and resulted in a maximal increase of 154 mL/min from baseline (45 mL/min). Caused a dose-dependent decrease in mean coronary resistance with a maximal decrease of 73 and 75 % at 2.5 and 5 μg/kg, respectively. Animal model: Mongrel dogs (23-27 kg). Dosage: 2.5 μg/kg. Administration: Peripheral intravenous injection; single in 30 s. Result: Reached 84% of the peak reactive hyperemia flow following a 20-s-long coronary occlusion (201 mL/min). Animal model: Female F344 rats (150-170 g). Dosage: 0.5 μg/kg. Administration: Intravenous injection; single (60 or 90 min after Temozolomide administration). Result: Increaseed levels of Temozolomide by 60 % in normal brain without affecting plasma concentrations.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CVT-3146 | Lexiscan

Quick Database Links

Gene Symbol

Adenosine Receptor