Description | Benzocain 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 |
Signaling Pathways
>>
Membrane Transporter/Ion Channel
>>
Sodium Channel
Research Areas
>>
Neurological Disease
|
||||||||||||
Target |
IC50: 0.8 mM (Na+ channel)[1]. |
||||||||||||
In Vitro | Benzocain blocks μ1 wild-type Na+ currents in a dose-dependent Manner. The Benzocain 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 benzocain (from 6.6 to 9.9 mV). Mutation of μ1-N1584A also significantly increases the potency of Benzocain. At 1 mM, Benzocain blocks about 55% of wild-type Na+ current but about 95% of μ1-N1584A mutant current. Benzocain 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 Benzocain concentration (IC50=40.3±1.2mM) than that affecting the enzymatic activity[2]. | ||||||||||||
In Vivo | A common Benzocain-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 Benzocain spray is observed in most animals tested, with response peaking between 15 and 30 minutes after dosing[3]. | ||||||||||||
Solvent |
In Vitro:
DMSO : ≥ 100 mg/mL (605.36 mM) H 2 O : 2 mg/mL (12.11 mM; ultrasonic and warming and heat to 60°C) * "≥" means soluble, but saturation unknown. In Vivo: 1.Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution 2.Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution 3.Add each solvent one by one: 10% DMSO 90% corn oil Solubility: ≥ 2.5 mg/mL (15.13 mM); Clear solution |
||||||||||||
Solubility |
|
||||||||||||
Storage |
4°C, protect from light |
||||||||||||
Shipping | Room temperature in continental US; may vary elsewhere | ||||||||||||
SMILES | O=C(OCC)C1=CC=C(N)C=C1 |
Density | 1.1±0.1 g/cm3 |
---|---|
Boiling Point | 310.7±15.0 °C at 760 mmHg |
Melting Point | 88-90 °C |
Molecular Formula | C 9 H 11 NO 2 |
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. |
Name | CAS | Appearance |
Ethyl 2-phenylacetoacetate | 5413-05-8 | White powder |
Diethyl(phenylacetyl)malonate | 20320-59-6 | White powder |
BMK methyl glycidate | 80532-66-7 | Yellow liquid |
3-OXO-4-PHENYL-BUTYRIC ACID ETHYL ESTER | 718-08-1 | Clear liquid |
1-(benzo[d][1,3]dioxol-5-yl)-2-bromopropan-1-one | 52190-28-0 | Brown powder |
PMK ethyl glycidate | 28578-16-7 | Brown liquid |
2-Benzylamino-2-methyl-1-propanol | 10250-27-8 | White powder |
2-iodo-1-p-tolyl-propan-1-one | 236117-38-7 | Yellow powder |
1-(Benzyloxycarbonyl)-4-piperidinone | 19099-93-5 | White powder |
1-BOC-4-(4-FLUORO-PHENYLAMINO)-PIPERIDINE | 288573-56-8 | White powder |
1-BOC-4-(4-BROMO-PHENYLAMINO)-PIPERIDINE | 443998-65-0 | White powder |
1-Phenyl-2-nitropropene | 705-60-2 | Yellow diamond crystal |
docosyltrimethylammonium methyl sulphate | 81646-13-1 | White flake |
2-Amino-4-phenylbutane | 22374-89-6 | Transparent crystal |
Tetramisole hydrochloride | White powder Contained crystal | |
N-Isopropylbenzylamine | 102-97-6 | Clear crystal pink blue |
Valerophenone | 1009-14-9 | Clear liquid or Yellow liquid |
4'-Methylpropiophenone | 5337-93-9 | Clear liquid or Yellow liquid |
Tryptamine | 61-54-1 | White powder |
Dimethyl terephthalate | 120-61-6 | Colorless rhombic crystal system crystal |
Valerophenone | 1009-14-9 | White liquid |
N-(2,6-Dimethylphenl)-2-Piperidine Carboxamide | 15883-20-2 | White powder |
4-Methylpropiophenone | 5337-93-9 | Yellow liquid |
Benzylisopropylamine | 102-97-6 | Transparent crystal, transparent column, pink, blue |
5-Nitro-2-(bromoacetamido)benzophenone | 2011-70-3 | |
Nitazoxanide | 55981-09-4 | White powder |
1H-Indole-5,6-diol | 3131-52-0 | White powder |
D-Tartaric acid | 147-71-7 | White powder |
L-(+)-Tartaric acid | 526-83-0 | White powder |
L(+)-Tartaric acid | 87-69-4 | White powder |
DL-Tartaric acid | 133-37-9 | White powder |
1-Boc-3-Piperidinone | 98977-36-7 | Yellow powder |
tert-butyl 4-(4-bromoanilino)piperidine-1-carboxylate | 443998-65-0 | White powder |
tert-butyl 4-(4-fluoroanilino)piperidine-1-carboxylate | 288573-56-8 | White powder |
N-Benzyl-4-piperidone | 3612-20-2 | Yellow liquid |
4-oxopiperidinium chloride | 41979-39-9 | Yellow powder |
N-Phenyl-4-biphenylamine | 32228-99-2 | White powder |
N-BOC-aniline | 3422/1/3 | White powder |
4'-Methoxypropiophenone | 121-97-1 | White powder |
2-iodo-1-p-tolylpropan-1-one | 236117-38-7 | Yellow powder |
2-bromo-1-phenylhexan-1-one | 59774-06-0 | Yellow liquid |
2-iodo-1-phenyl-pentane-1-one | 124878-55-3 | Yellow liquid |
hexanophenone | 942-92-7 | White liquid |
2-(2-chlorophenyl)cyclohexan-1-one | 91393-49-6 | Yellow liquid |
2-Oxiranecarboxylicacid, 3-(1,3-benzodioxol-5-yl)-2-methyl-, ethyl ester | 28578-16-7 | Yellow liquid,Yellow powder,White powder |
1-Bromocyclopentyl-o-chlorophenyl ketone | White powder | |
Nicotinamide riboside chloride | 23111-00-4 | White powder |
1,4-Dimethoxy-2-(2-nitroethenyl) benzene | 40276-11-7 | Brown red color,White powder |
1-Phenyl-2-nitropropene | 705-60-2 | Yellow powder |
Loperamide hydrochloride | 34552-83-5 | White powder |
N-Benzyl-4-piperidone | 3612-20-2 | Yellow liquid |
1-Boc-3-Piperidinone | 98977-36-7 | Yellow powder |
Diethyl(phenylacetyl)malonate | 20320-59-6 | Brown red liquid |
(2S)-2-Ethylbutyl 2-(((perfluorophenoxy)(phenoxy)phosphoryl)amino)propanoate | 1911578-98-7 | White powder |
Tetramisole hydrochloride | White powder | |
Piperidin-4-one hydrochloride | 41979-39-9 | White powder |
5-(2-Fluorophenyl)-1H-pyrrole-3-carbonitrile | 1240948-77-9 | White powder |
5-(2-Fluorophenyl)-1H-pyrrole-3-carbaldehyde | 881674-56-2 | White powder |
5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrole-3-carbaldehyde | 881677-11-8 | White powder |
Pyridine-3-sulfonyl chloride | 16133-25-8 | White powder |
1-Boc-3-piperidone | 98977-36-7 | Yellow powder |
(R)-7-(Benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione | 1985607-70-2 | White powder |
Loperamide hydrochloride | 34552-83-5 | White powder |
3-Benzyloxy-4-oxo-4H-pyran-2-carboxylic acid | 119736-16-2 | White powder |
methyl-2-methyl-3-phenylglycidate | 80532-66-7 | White powder |
N-Carbethoxy-4-piperidone | 29976-53-2 | Yellow liquid |
N-[(S)-(4-nitrophenoxy)phenoxyphosphinyl]-L-Alanine 2-ethylbutyl ester | 1354823-36-1 | White powder |
Benzyl alcohol | 100-51-6 | White liquid,White powder |
2-Bromo-4-fluoroaniline | 1003-98-1 | Yellow liquid |
Albendazole | 54965-21-8 | White powder |
Cysteamine Hydrochloride | 156-57-0 | White powder |
Olmesartan medoxomil | 144689-63-4 | White powder |
Florfenicol | 76639-94-6 | White powder |
Sulfanilamide | 63-74-1 | White grain |
Nafamostat mesylate | 82956-11-4 | White powder |
Dexmedetomidine | 113775-47-6 | White powder |
Bromadol | 77239-98-6 | White powder |
Cedrol | 77-53-2 | White powder |
Ferrous sulfate heptahydrate | 7782-63-0 | Light green powder |
1-Bromo-3,5-dimethyladamantane | 941-37-7 | Clear liquid |
1,3-Dimethyladamantane | 702-79-4 | Clear liquid |
docosyl-trimethyl-azanium; sulfonatooxymethane | 81646-13-1 | White flake |
Anethole | 4180-23-8 | Clear liquid |
3-Amino-1-hydroxyadamantane | 702-82-9 | White powder |
Furosemide | 54-31-9 | White powder |
2-Piperidone | 675-20-7 | White powder |
Levobupivacaine hydrochloride | 27262-48-2 | White powder |
8-ETHYL-5,8-DIHYDRO-5-OXO-2-[1-PIPERAZINYL]PYRIDO[2,3-D]-PYRIMIDINE-6-CARBOXYLIC ACID | 51940-44-4 | White powder |
Dihydroxyacetone (1,3-Dihydroxyacetone) | 96-26-4 | White powder |
Denatonium | 3734-33-6 | White powder |
Benzoate | 532-32-1 | White powder |
2-ethylhexanol | 104-76-7 | White powder,Clear liquid |
Cesium chloride (Caesium chloride) | 7647-17-8 | White powder |