Drug intelligence / Profile preview

tolpropamine

Development stage
Unknown
Lead developer
Hoechst
Modality
Small Molecules
Administration
Topical
01

Overview

Tolpropamine is a first-generation antihistamine of the alkylamine class with anticholinergic properties, primarily used as an antipruritic and topical antihistaminic. It acts as an H1 receptor antagonist, blocking the action of histamine at H1 receptors to reduce allergic symptoms such as itching and inflammation. Tolpropamine is noted for its rapid onset and minimal sedative effects compared to older antihistamines. Its mechanism involves interfering with histamine-induced signaling pathways, stabilizing mast cells, reducing pro-inflammatory cytokine expression via NF-κB inhibition, and decreasing further histamine release. It is mainly indicated for conditions like allergic rhinitis, urticaria (hives), and other dermatological allergies[1][3][4][5][6].

Other names
tolpropaminatolpropaminum
02

Targets

HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)

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