Repositioning Candidate Details
| Candidate ID: | R0337 |
| Source ID: | DB01136 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Carvedilol |
| Synonyms: | |
| Molecular Formula: | C24H26N2O4 |
| SMILES: | COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=C1C1=CC=CC=C1N2 |
| Structure: |
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| DrugBank Description: | Carvedilol is a racemic mixture where the S(-) enantiomer is a beta adrenoceptor blocker and the R(+) enantiomer is both a beta and alpha-1 adrenoceptor blocker.[L7889,L7892] It is currently used to treat heart failure, left ventricular dysfunction, and hypertension.[L7889,L7892] The dual action of carvedilol is advantageous in combination therapies as moderate doses of 2 drugs have a decreased incidence of adverse effects compared to high dose monotherapy in the treatment of moderate hypertension.[A182306] Carvedilol was granted FDA approval on 14 September 1995.[L7889] |
| CAS Number: | 72956-09-3 |
| Molecular Weight: | 406.4742 |
| DrugBank Indication: | Carvedilol is indicated to treat mild to severe heart failure, left ventricular dysfunction after myocardial infarction with ventricular ejection fraction ≤40%, or hypertension.[L7889,L7892] |
| DrugBank Pharmacology: | Carvedilol reduces tachycardia through beta adrenergic antagonism and lowers blood pressure through alpha-1 adrenergic antagonism.[L7889,L7892] It has a long duration of action as it is generally taken once daily and has a broad therapeutic index as patients generally take 10-80mg daily.[L7889,L7892] Patients taking carvedilol should not abruptly stop taking this medication as this may exacerbate coronary artery disease.[L7889,L7892] |
| DrugBank MoA: | Carvedilol inhibits exercise induce tachycardia through its inhibition of beta adrenoceptors.[A182306] Carvedilol's action on alpha-1 adrenergic receptors relaxes smooth muscle in vasculature, leading to reduced peripheral vascular resistance and an overall reduction in blood pressure.[A1929,A182306] At higher doses, calcium channel blocking and antioxidant activity can also be seen.[A1929] The antioxidant activity of carvedilol prevents oxidation of low density lipoprotein and its uptake into coronary circulation.[A1929] |
| Targets: | Beta-1 adrenergic receptor; Alpha-1A adrenergic receptor; Alpha-1 adrenergic receptors; NADH dehydrogenase [ubiquinone] 1 subunit C2; Beta-2 adrenergic receptor; Vascular endothelial growth factor A; Natriuretic peptides B; Gap junction alpha-1 protein; Potassium voltage-gated channel subfamily H member 2; Vascular cell adhesion protein 1; Alpha-1D adrenergic receptor; Alpha-1B adrenergic receptor; Alpha-2C adrenergic receptor; Alpha-2B adrenergic receptor; Alpha-2A adrenergic receptor; E-selectin; Hypoxia-inducible factor 1-alpha; Inward rectifier potassium channel 4; Inward rectifier potassium channel 2 |
| Inclusion Criteria: |
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