Adenosine

Adenosine Receptor Agonist — CARDIOVASCULAR SYSTEM

Key facts

Adenosine is an ofp drug in the Adenosine Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1989. Its mechanism of action is classified as Adenosine Receptor Agonists. DrugCentral lists 18 molecular targets, including Adora2b|Adora2a, Adora1 and Adora2a. Recorded indications include Myocardial Perfusion Imaging Adjunct and Paroxysmal supraventricular tachycardia.

• Approval status: ofp (first approved 1989 by the FDA).
• Drug class: Adenosine Receptor Agonist.
• Mechanism of action: Adenosine Receptor Agonists.
• Molecular targets: Adora2b|Adora2a, Adora1, Adora2a and Adora3 (18 listed in DrugCentral).
• Indications: Myocardial Perfusion Imaging Adjunct and Paroxysmal supraventricular tachycardia.
• ATC code: C01EB10 (Other cardiac preparations).
• Molecular formula: C10H13N5O4; molecular weight 267.25 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Myocardial Perfusion Imaging Adjunct
• Paroxysmal supraventricular tachycardia

Off-label uses (1)

• Supraventricular tachycardia

Contraindications (20)

• Acute cerebrovascular insufficiency
• Acute coronary syndrome
• Aortic valve stenosis
• Asthma
• Chronic obstructive lung disease
• Complete atrioventricular block
• Disorder of autonomic nervous system
• Hypovolemia
• Left main coronary artery disease
• Left to right cardiovascular shunt
• Low blood pressure
• Mitral valve stenosis
• Pericarditis
• Pulmonary emphysema
• Respiratory alkalosis
• Respiratory insufficiency
• Second degree atrioventricular block
• Sick sinus syndrome
• Syncope due to Bradycardia
• Transplantation of heart

Mechanism & targets

• Mechanism of action (MoA): Adenosine Receptor Agonists
• Established pharmacologic class: Adenosine Receptor Agonist

Molecular targets (18)

Target	Gene	Action	Activity
Adenosine A2 receptor	Adora2b|Adora2a	unknown	Ki 8.30
Adenosine receptor A1	Adora1	unknown	Ki 8.29
Adenosine receptor A2a	Adora2a	unknown	Ki 7.52
Adenosine receptor A3	Adora3	unknown	Ki 7.00
Adenosine receptor A3	ADORA3	agonist	Ki 6.54
Adenosine receptor A1	ADORA1	agonist	EC50 6.51
Adenosine receptor A2a	ADORA2A	agonist	EC50 6.16
Adenosine kinase	ADK	unknown	IC50 6.00
Adenosylhomocysteinase	AHCY	unknown	Km 5.80
Mitogen-activated protein kinase kinase kinase 7	MAP3K7	unknown	Kd 5.36
Adenosine kinase	AK	unknown	Ki 5.05
Phosphatidylinositol 4-kinase type 2-alpha	PI4K2A	inhibitor	IC50 5.00
Phosphatidylinositol 4-kinase type 2-beta	PI4K2B	inhibitor	IC50 5.00
cAMP-dependent protein kinase A	PRKAR2A|PRKACA|PRKACB|PRKAR2B	unknown	Ki 4.82
Adenosine receptor A2b	ADORA2B	agonist	EC50 4.62
Adenosine deaminase	ADA	unknown	Kd 4.60
Glyceraldehyde-3-phosphate dehydrogenase liver	GAPDH	unknown	IC50 4.46
Histone-lysine N-methyltransferase, H3 lysine-79 specific	DOT1L	unknown	IC50 4.00

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1989-10-30	FDA	—	ASTELLAS

ATC classification

ATC code	Therapeutic hierarchy
C01EB10	CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › OTHER CARDIAC PREPARATIONS › Other cardiac preparations

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Drug ineffective	247.4
Bronchospasm	113.8
Supraventricular tachycardia	110.7
Ventricular fibrillation	95.0
Ventricular tachycardia	94.8
Arteriospasm coronary	79.4
Cardiac arrest	72.7
Drug ineffective for unapproved indication	72.5
Bradycardia	60.9
Pemphigoid	56.8
Atrioventricular block	55.8
Oesophageal ulcer haemorrhage	53.3

Chemical structure

• Molecular formula: C₁₀H₁₃N₅O₄
• Molecular weight: 267.25 g/mol
• CAS number: —
• InChIKey: OIRDTQYFTABQOQ-KQYNXXCUSA-N
• PubChem CID: 60961

NC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C2=NC=N1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Adenosine used for?

DrugCentral lists the following indications for Adenosine: Myocardial Perfusion Imaging Adjunct and Paroxysmal supraventricular tachycardia.

How does Adenosine work?

Adenosine is classified as Adenosine Receptor Agonists; its molecular targets in DrugCentral include Adora2b|Adora2a, Adora1, Adora2a and Adora3.

When was Adenosine first approved?

Adenosine was first approved by the FDA in 1989.

What drug class does Adenosine belong to?

Adenosine is in the Adenosine Receptor Agonist class.

What is the chemical formula of Adenosine?

Adenosine has the molecular formula C10H13N5O4 and a molecular weight of 267.25 g/mol.

Sources

• DrugCentral drug card 90 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL477 — compound record and bioactivity
• PubChem CID 60961 — chemical identifiers
• DrugBank DB00640 — drug record
• FDA UNII K72T3FS567 — substance identity
• DailyMed: FDA labels for Adenosine — current prescribing information (label search)
• UniProt P0DMS8 (ADORA3) — target protein
• UniProt P30542 (ADORA1) — target protein
• UniProt P29274 (ADORA2A) — target protein
• UniProt P55263 (ADK) — target protein
• UniProt P23526 (AHCY) — target protein
• UniProt O43318 (MAP3K7) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.