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

HRH1 (Histamine H1 Receptor)HRH2 (Histamine H2 Receptor)PAR2 (Protease-activated receptor 2)PAR4 (Protease-activated receptor 4)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)

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