Drug intelligence / Profile preview

lidocaine + histamine + cowhage

Development stage
Preclinical
Modality
Small Molecules
Administration
Topical
01

Overview

This is a compounded topical or experimental combination of three agents—lidocaine, histamine, and cowhage—primarily used in research settings to study mechanisms of itch (pruritus) and pain.\n- **Lidocaine** is a local anesthetic that blocks voltage-gated sodium channels on sensory neurons, inhibiting nerve signal transmission and providing analgesic and antipruritic effects.\n- **Histamine** is an endogenous compound that acts as an agonist at multiple histamine receptors (H1, H2, H3, H4), mediating vasodilation, increased vascular permeability, smooth muscle contraction/relaxation, gastric acid secretion, and pruritus when applied to the skin[5].\n- **Cowhage** refers to spicules from the plant *Mucuna pruriens*, which contain mucunain—a protease that activates proteinase-activated receptors (PAR2/4) on sensory nerves to induce non-histaminergic itch.\n\nThis specific combination does not correspond to any approved pharmaceutical product but has been used in experimental models for inducing or modulating different types of itch (histaminergic via histamine; non-histaminergic via cowhage) with lidocaine included for its modulatory effect on neural responses[1][2][4]. The mixture allows researchers to compare mechanisms underlying different forms of pruritus and assess the efficacy of local anesthetics like lidocaine in suppressing these sensations.

02

Targets

PAR4 (Protease-activated receptor 4)HRH1 (Histamine H1 Receptor)NaV (Voltage-gated sodium channels)HRH2 (Histamine H2 Receptor)PAR2 (Protease-activated receptor 2)

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