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deptropine
- Development stage
- Unknown
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Deptropine is a first-generation tricyclic antihistamine with anticholinergic properties. It acts primarily as an antagonist at the histamine H1 receptor and also exhibits muscarinic receptor antagonism[3][4][7]. Deptropine is used mainly for the management of allergic conditions such as allergic rhinitis and urticaria[1][6]. Historically prescribed for asthma due to its bronchodilatory effects via antimuscarinic action, its use has declined in favor of inhaled beta-2 adrenergic agonists and glucocorticosteroids[4]. Deptropine readily crosses the blood-brain barrier and can cause central nervous system side effects such as sedation[6]. Recent research has explored its potential anti-cancer activity in breast cancer stem cells and hepatocellular carcinoma by interfering with autophagy pathways leading to cell death[4][5].
- Brand names
- BrontinaNoleptanPiridolanBrontineDeptrin
- Other names
- deptropinaDIBENZHEPTROPINE CITRATE
02
Targets
mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)
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