Investigational Drug Details
| Drug ID: | D183 |
| Drug Name: | Adenosine |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00640 |
| DrugBank Description: | A nucleoside that is composed of adenine and d-ribose. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter. |
| PubChem ID: | 60961 |
| CasNo: | 58-61-7 |
| Repositioning for NAFLD: | Yes |
| SMILES: | NC1=C2N=CN([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)C2=NC=N1 |
| Structure: |
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| InChiKey: | OIRDTQYFTABQOQ-KQYNXXCUSA-N |
| Molecular Weight: | 267.2413 |
| DrugBank Targets: | Adenosine receptor A1; Adenosine receptor A2a; Adenosine receptor A2b; Adenosine receptor A3 |
| DrugBank MoA: | Adenosine slows conduction time through the AV node and can interrupt the reentry pathways through the AV node, resulting in the restoration of normal sinus rhythm in patients with paroxysmal supraventricular tachycardia (PSVT), including PSVT associated with Wolff-Parkinson-White Syndrome. This effect may be mediated through the drug's activation of cell-surface A<sub>1</sub> and A<sub>2</sub> adenosine receptors. Adenosine also inhibits the slow inward calcium current and activation of adenylate cyclase in smooth muscle cells, thereby causing relaxation of vascular smooth muscle. By increasing blood flow in normal coronary arteries with little or no increase in stenotic arteries (with little to no increase in stenotic arteries), adenosine produces a relative difference in thallous (thallium) chloride TI 201 uptake in myocardium supplied by normal verus stenotic coronary arteries. |
| DrugBank Pharmacology: | Adenosine is an endogenous nucleoside occurring in all cells of the body and is not chemically related to other antiarrhythmic drugs. Adenosine may exert its pharmacologic effects by activation of purine (cell surface A<sub>1</sub> and A<sub>2</sub> adenosine) receptors, as well as relax vascular smooth muscles through the reduction in calcium uptake by inhibition of slow inward calcium current and activation of adenylate cyclase in smooth muscle cells. Adenosine may reduce vascular tone by modulation of sympathetic neurotransmission. The drug also has negative chronotropic, dromotropic, and inotropic effects on the heart by slowing conduction time throught he AV node and interrupting AV nodal reentry pathways. Adenosine is a potent vasodilator in most vascular beds, but vasoconstriction is produced in renal afferent arterioles and hepatic veins. The drug produces a net mild to moderate reduction in systolic, diastolic, and mean arterial blood pressure and a reflex increase in heart rate. Adenosine is antagonized competitively by methylxanthines such as caffeine and theophylline, and potentiated by blockers of nucleoside transport such as dipyridamole. Adenosine is not blocked by atropine. |
| DrugBank Indication: | Used as an initial treatment for the termination of paroxysmal supraventricular tachycardia (PVST), including that associated with accessory bypass tracts, and is a drug of choice for terminating stable, narrow-complex supraventricular tachycardias (SVT). Also used as an adjunct to thallous chloride TI 201 myocardial perfusion scintigraphy (thallium stress test) in patients who are unable to exercise adequately, as well as an adjunct to vagal maneuvers and clinical assessment to establish a specific diagnosis of undefined, stable, narrow-complex SVT. |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0140 | NCT02427594 | PHASE1 | COMPLETED | NO | 2015-04 | 2017-08-30 | Details |
| L0521 | NCT01663103 | PHASE4 | COMPLETED | YES | 2012-08 | 2016-09-12 | Details |
| L0693 | NCT01439867 | PHASE2 | TERMINATED | YES | 2012-06-22 | 2020-06-17 | Details |
| L1075 | NCT04143581 | PHASE2 | WITHDRAWN | NO | 2021-09-03 | 2021-09-13 | Details |
| L1480 | NCT02598635 | PHASE4 | UNKNOWN | NO | 2015-10 | 2017-03-24 | Details |
| L1583 | NCT01214395 | PHASE2 | COMPLETED | YES | 2010-06 | 2012-08-03 | Details |
| L4427 | NCT02497313 | COMPLETED | NO | 2015-07 | 2017-05-03 | Details | |
| L4560 | NCT02481141 | COMPLETED | YES | 2014-07 | 2018-05-22 | Details | |
| L5837 | NCT01494987 | PHASE3 | COMPLETED | YES | 2012-01 | 2014-11-18 | Details |
| L6093 | NCT02111096 | PHASE2 | TERMINATED | YES | 2014-04 | 2019-10-09 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T03 | Angiotensin-converting enzyme | ACE | INHIBITOR | Target is a single protein chain | P12821 | ACE_HUMAN | Details |
| T13 | Renin | REN | INHIBITOR | Target is a single protein chain | P00797 | REN_HUMAN | Details |
| T06 | Sulfonylurea receptor 1 | ABCC8 | Target is a single protein chain | Q09428 | ABCC8_HUMAN | Details | |
| T15 | Steryl-sulfatase | STS | INHIBITOR | Hydrolase | P08842 | STS_HUMAN | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00058 | 14960743 | N Engl J Med | Impaired mitochondrial activity in the insulin-resistant offspring of patients with type 2 diabetes. | Details |
| A00076 | 16142453 | Hum Genet | Mitochondrial polymorphisms and susceptibility to type 2 diabetes-related traits in Finns. | Details |
| A00107 | 18025464 | Proc Natl Acad Sci U S A | Increased ATPase activity produced by mutations at arginine-1380 in nucleotide-binding domain 2 of ABCC8 causes neonatal diabetes. | Details |
| A00110 | 18323454 | Science | Hepatic glucose sensing via the CREB coactivator CRTC2. | Details |
| A00113 | 18596924 | J Clin Invest | Clinical characteristics and biochemical mechanisms of congenital hyperinsulinism associated with dominant KATP channel mutations. | Details |
| A00174 | 29471960 | Nefrologia (Engl Ed) | Overview of autosomal dominant polycystic kidney disease in the south of Spain. | Details |