Repositioning Candidate Details
| Candidate ID: | R0127 |
| Source ID: | DB00455 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Loratadine |
| Synonyms: | |
| Molecular Formula: | C22H23ClN2O2 |
| SMILES: | CCOC(=O)N1CCC(CC1)=C1C2=C(CCC3=C1N=CC=C3)C=C(Cl)C=C2 |
| Structure: |
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| DrugBank Description: | Loratadine is a second generation antihistamine used to manage symptoms of allergic rhinitis.[A176435] A lack of sedative and CNS adverse effects make loratadine, along with other second generation antihistamines, preferable over their 1st generation counterparts in many clinical situations.[A176441] |
| CAS Number: | 79794-75-5 |
| Molecular Weight: | 382.883 |
| DrugBank Indication: | Loratadine is a 2nd generation antihistamine and is used to manage symptoms of allergic rhinitis, wheal formation, urticaria, and other allergic dermatologic conditions.[A176435][A176438][L8486] |
| DrugBank Pharmacology: | Like other 2nd generation antihistamines, loratadine is selective for peripheral H1 receptors.[A5506] Loratadine does not penetrate effectively into the central nervous system and has poor affinity for CNS H1-receptors.[A5506] These qualities result in a lack of CNS depressant effects such as drowsiness, sedation, and impaired psychomotor function.[A5506] |
| DrugBank MoA: | Histamine release is a key mediator in allergic rhinitis and urticaria.[A185312][A176441][A175060] As a result, loratadine exerts it's effect by targeting H1 histamine receptors. Loratadine binds to H1 histamine receptors found on the surface of epithelial cells, endothelial cells, eosinophils, neutrophils, airway cells, and vascular smooth muscle cells among others.[A176441] H1 histamine receptors fall under the wider umbrella of G-protein coupled receptors, and exist in a state of equilibrium between the active and inactive forms.[A176441][A175060] Histamine binding to the H1-receptor facilitates cross linking between transmembrane domains III and V, stabilizing the active form of the receptor.[A176441][A175060] On the other hand, antihistamines bind to a different site on the H1 receptor favouring the inactive form.[A176441][A175060] Hence, loratadine can more accurately be classified as an "inverse agonist" as opposed to a "histamine antagonist", and can prevent or reduce the severity of histamine mediated symptoms.[A176441][A175060][L8486] |
| Targets: | Histamine H1 receptor; Potassium voltage-gated channel subfamily H member 2 |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I02 | 1184 | nephrotic syndrome | "A nephrosis characterized by marked increase in glomerular protein permeability resulting in marked elevation of urine protein levels, hypoalbuminemia, hyperlipidemia, and hypercoagulability." [url:https\://en.wikipedia.org/wiki/Nephrotic_syndrome, url:https\://www.niddk.nih.gov/health-information/kidney-disease/nephrotic-syndrome-adults] | Details |