Repositioning Candidate Details
| Candidate ID: | R0943 |
| Source ID: | DB06204 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Tapentadol |
| Synonyms: | Tapentadol |
| Molecular Formula: | C14H23NO |
| SMILES: | CC[C@H]([C@@H](C)CN(C)C)C1=CC(O)=CC=C1 |
| Structure: |
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| DrugBank Description: | Opioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008. |
| CAS Number: | 175591-23-8 |
| Molecular Weight: | 221.3385 |
| DrugBank Indication: | The immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy. |
| DrugBank Pharmacology: | Tapentadol is a centrally-acting synthetic analgesic that is 18 times less potent than morphine in binding mu-opioid receptors. It also increases norepinephrine concentrations in the brains of rats via inhibition of norepinephrine reuptake. Selective mu-opioid antagonists like naloxone can block analgesia from tapentadol. It also has not effect on the QT interval. |
| DrugBank MoA: | Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition. |
| Targets: | Mu-type opioid receptor agonist; Sodium-dependent noradrenaline transporter inhibitor; Kappa-type opioid receptor; Delta-type opioid receptor; 5-hydroxytryptamine receptor 3A; Sodium-dependent serotonin transporter inhibitor |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I05 | 9352 | Type 2 diabetes mellitus | A diabetes that is characterized by chronic hyperglycaemia with disturbances of carbohydrate, fat and protein metabolism resulting from defects in insulin secretion, insulin action, or both. A diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. http://en.wikipedia.org/wiki/Diabetes, http://en.wikipedia.org/wiki/Diabetes_mellitus_type_2 | disease of metabolism/inherited metabolic disorder/ carbohydrate metabolic disorder/glucose metabolism disease/diabetes/ diabetes mellitus | Details |