Articaine (hydrochloride)

Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC₅₀ of 15.8 μM for open-state Na⁺ channels, and IC₅₀ of 40.6 μM and 378 μM for inactivated and resting-state Na⁺ channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na⁺ influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury)^[1][2][3]. In Vivo:Articaine (20 mg/kg, 40 mg/kg; intraperitoneal injection; single dose) hydrochloride can significantly reduce serum urea nitrogen, creatinine and cystatin C levels, alleviate renal tissue pathological damage, inhibit the release of inflammatory factors such as TNF-α, IL-6, and IL-1β, and exert anti-inflammatory effects by inhibiting NF-κB activation and NLRP3 inflammasome pathway in the lipopolysaccharide (LPS)-induced acute kidney injury model of Swiss albino mice^[2].
Articaine hydrochloride (0.5 mM, 1 mM; immersion for 1 h) can enhance the anesthetic effect in the zebrafish model, inhibiting the tactile response rate by 100% and reducing the heart rate by 60%. In combination with nanolipid carriers (NLCs), it can prolong the duration of anesthesia^[3].