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Benzocaine Sodium Channel inhibitor

Cat.No.S4210

Benzocaine(ethyl 4-aminobenzoate) is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.
Benzocaine Sodium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 165.19

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Quality Control

Batch: S421001 DMSO]33 mg/mL]false]Ethanol]33 mg/mL]false]Water]Insoluble]false Purity: 99.93%
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99.93

Solubility

In vitro
Batch:

DMSO : 33 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 165.19 Formula

C9H11NO2

 Storage (From the date of receipt)
CAS No. 94-09-7 Download SDF Storage of Stock Solutions

Synonyms ethyl 4-aminobenzoate Smiles CCOC(=O)C1=CC=C(C=C1)N

Mechanism of Action

Targets/IC50/Ki
Sodium channel
In vitro

Benzocaine blocks µ1 wild-type Na+ currents in a dose-dependent manner with IC50 of 0.8 mM in HEK293T cells. This compound (1 mM) blocks about 55% of wild-type Na+ current but about 95% of µ1-N1584A mutant current. It (1 mM) blocks about 55% of wild-type µ1 currents, but about 80% of µ1-I1575A mutant current. This chemical results in a biphasic (protective/inductive) concentration-dependent hemolytic effect upon rat erythrocytes, with an effective Benzocaine:lipid molar ratio in the membrane for protection (RePROT), onset of hemolysis (ReSAT) and 100% membrane solubilization (ReSOL) of 1.0:1, 1.1:1 and 1.3:1, respectively. It and 4-hydroxybenzoate interact with the open and inactivated channels during repetitive pulses, but during the interpulse the complex dissociates too fast to accumulate sufficient use-dependent block of Na+ currents. This compound (500 μM) reduces the peak and steady-state currents and increases the amplitude of the inactivating component from 21.7% to 30.2% (n=7, P<0.05), so that benzocaine-induced block at the end of pulses to +60 mV averaged 30.9% (n=7). It (500 μM) significantly accelerates the initial phase of deactivation (τf=27.2±2.6 ms, n=7, P<0.01), but does not modify the slow phase of tail current decline. This chemical binds with high affinity to an intracellular binding site to produce 'agonist' effects and to a low affinity subsite, which is also located in the inner mouth, to produce the blocking effects. It and extracellular K(+) interact to modify the voltage-dependence of channel opening.

In vivo

Benzocaine is absorbed rapidly and similarly through both viable and nonviable skin of the hairless guinea pig, the absorption of the two acidic compounds, benzoic acid and PABA, is greater through nonviable skin.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12237171/
  • [5] https://pubmed.ncbi.nlm.nih.gov/2293213/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06165432 Completed
Pain
B.P. Koirala Institute of Health Sciences
 March 19 2021 Phase 4
NCT03116737 Completed
Pain|Acute Otitis Media
Lachlan Pharma Holdings
 January 3 2017 Phase 3
NCT02092454 Completed
Pain|Acute Otitis Media
Otic Therapy LLC
 September 2013 Phase 2

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