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Anesthetics Benzocaine Pharmaceutical Intermediate CAS 94-09-7

Chemical name    Common names and synonyms      CAS number    EC number   Concentration
benzocaine benzocaine 94-09-7 none         100%

Precautions for safe handling

Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Avoid exposure - obtain special instructions before use.Provide appropriate exhaust ventilation at places where dust is formed. For precautions see section 2.2.

Conditions for safe storage, including any incompatibilities

Benzocaine topical creams and ointments should be stored in tight containers and protected from light; prolonged exposure to temperatures greater than 30°C should be avoided.

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  • 94-09-7
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 Names

Name benzocaine

 Benzocaine Biological Activity

Description Benzocaine shares a common receptor with all other local anesthetics (LAs) in the voltage-gated Na+ channel, with an IC50 of 0.8 mM tested with a potential of +30 mV.
Related Catalog
Target

IC50: 0.8 mM (Na+ channel)[1].

In Vitro Benzocaine blocks μ1 wild-type Na+ currents in a dose-dependent Manner. The Benzocaine concentration that inhibits 50% of Na+ currents (IC50) is estimated to be about 0.8 mM when a test potential of +30 mV is applied. The slope of the h∞ curve is also significantly reduced by benzocaine (from 6.6 to 9.9 mV). Mutation of μ1-N1584A also significantly increases the potency of Benzocaine. At 1 mM, Benzocaine blocks about 55% of wild-type Na+ current but about 95% of μ1-N1584A mutant current. Benzocaine also appears to bind more strongly to its LA receptor in the N1584A mutant than in the wild type[1]. The inhibition of Ca2+ uptake occurres at lower Benzocaine concentration (IC50=40.3±1.2mM) than that affecting the enzymatic activity[2].
In Vivo A common Benzocaine-containing anesthetic is topically applied to the following species: dogs, domestic shorthair cats, Long-Evans rats, Sprague-Dawley rats, ferrets, rhesus monkeys, cynomolgus monkeys, owl monkeys, New Zealand White rabbits, miniature pigs, ICR mice, C3H mice, and C57BL/10SnJ mice. All animals, except mice and rats, receive a 2-second spray to the mucous membranes of the nasopharynx for an estimated dose of 56 mg. A 2-second spray to rodents' oral mucous membranes delivers too great a volume of fluid for these animals. The study is repeated in dogs several months later to confirm low response. Response to Benzocaine spray is observed in most animals tested, with response peaking between 15 and 30 minutes after dosing[3].

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 310.7±15.0 °C at 760 mmHg
Melting Point 88-90 °C
Molecular Formula C9H11NO2
Molecular Weight 165.189
Flash Point 164.2±17.9 °C
Exact Mass 165.078979
PSA 52.32000
LogP 1.95
Vapour Pressure 0.0±0.7 mmHg at 25°C
Index of Refraction 1.555
Storage condition 0-6°C
Stability Stable. Combustible. Incompatible with strong oxidizing agents.

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