Regadenoson

Regadenoson
Clinical data

AHFS/Drugs.com	Multum Consumer Information
License data	US FDA: Regadenoson
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Intravenous
ATC code	C01EB21 (WHO)
Legal status
Legal status	US: ℞-only
Identifiers
IUPAC name 2-{4-[(methylamino)carbonyl]- 1H-pyrazol-1-yl}adenosine
Synonyms	1-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]- N-methylpyrazole-4-carboxamide
CAS Number	313348-27-5^Y
PubChem CID	219024
IUPHAR/BPS	5596
DrugBank	DB06213^N
ChemSpider	189859^N
UNII	7AXV542LZ4
KEGG	D05711^Y
ChEMBL	CHEMBL1201750^N
ECHA InfoCard	100.218.278
Chemical and physical data
Formula	C₁₅H₁₈N₈O₅
Molar mass	390.354 g/mol
3D model (Jmol)	Interactive image
SMILES CNC(=O)C1=CN(N=C1)C2=NC(=C3C(=N2)N(C=N3)[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)N
InChI InChI=1S/C15H18N8O5/c1-17-13(27)6-2-19-23(3-6)15-20-11(16)8-12(21-15)22(5-18-8)14-10(26)9(25)7(4-24)28-14/h2-3,5,7,9-10,14,24-26H,4H2,1H3,(H,17,27)(H2,16,20,21)/t7-,9-,10-,14-/m1/s1^N Key:LZPZPHGJDAGEJZ-AKAIJSEGSA-N^N
^NY (what is this?)

Regadenoson (CVT-3146, Lexiscan) is an A_2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing. It produces hyperemia quickly and maintains it for a duration that is useful for radionuclide myocardial perfusion imaging. The selective nature of the drug makes it preferable to other stress agents such as adenosine, which are less selective and therefore cause more side-effects.

Regadenoson was approved by the United States Food and Drug Administration on April 10, 2008 and is marketed by Astellas Pharma under the tradename Lexiscan. It is approved for use in the European Union and under the name of Rapiscan. It is currently being marketed by GE Healthcare and is being sold in both the United Kingdom and Germany.

Regadenoson has a 2 to 3 minute biological half-life, as compared with adenosine's 10-second half-life. As a result, regadenoson stress protocols use a single bolus, instead of a 4-6 minute continuous infusion, which was needed with adenosine. Another difference is that adenosine infusion is weight based (140mcg/kg/minute), while with regadenoson, a 0.4mg/5mL preloaded syringe dose is standard for all weights. Regadenoson stress tests are not affected by the presence of beta blockers, as regadenoson vasodilates via the adenosine pathway without stimulating beta adrenergic receptors.

One side effect of regadenoson is that it can temporarily disrupt the integrity of the blood-brain barrier by inhibiting P-glycoprotein function.

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