Investigational Drug Details
| Drug ID: | D045 |
| Drug Name: | Esmolol |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00187 |
| DrugBank Description: | Esmolol, commonly marketed under the trade name Brevibloc, is a cardioselective beta-1 receptor blocker. It has a rapid onset but short duration of action without causing significant intrinsic sympathomimetic or membrane stabilizing activities at recommended therapeutic doses. It works by blocking beta-adrenergic receptors in the heart, which leads to decreased force and rate of heart contractions. Esmolol prevents the action of two naturally occurring substances: epinephrine and norepinephrine. |
| PubChem ID: | 59768 |
| CasNo: | 81147-92-4 |
| Repositioning for NAFLD: | Yes |
| SMILES: | COC(=O)CCC1=CC=C(OCC(O)CNC(C)C)C=C1 |
| Structure: |
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| InChiKey: | AQNDDEOPVVGCPG-UHFFFAOYSA-N |
| Molecular Weight: | 295.374 |
| DrugBank Targets: | Beta-1 adrenergic receptor |
| DrugBank MoA: | Similar to other beta-blockers, esmolol blocks the agonistic effect of the sympathetic neurotransmitters by competing for receptor binding sites. Because it predominantly blocks the beta-1 receptors in cardiac tissue, it is said to be cardioselective. In general, so-called cardioselective beta-blockers are relatively cardioselective; at lower doses they block beta-1 receptors only but begin to block beta-2 receptors as the dose increases. At therapeutic dosages, esmolol does not have intrinsic sympathomimetic activity (ISA) or membrane-stabilizing (quinidine-like) activity. Antiarrhythmic activity is due to blockade of adrenergic stimulation of cardiac pacemaker potentials. In the Vaughan Williams classification of antiarrhythmics, beta-blockers are considered to be class II agents. |
| DrugBank Pharmacology: | |
| DrugBank Indication: | For the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Also used in noncompensatory sinus tachycardia where the rapid heart rate requires specific intervention. |
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