Tetracaine hydrochloride (Pontocaine) is a hydrochloride salt form of tetracaine which is a potent local anaesthetic and a channel function allosteric inhibitor. Tetracaine hydrochloride (Pontocaine) is used to block temporarily the pain "message" that is sent along the nerves that connect the eyes to the brain. Tetracaine hydrochloride (Pontocaine) is mainly used topically in ophthalmology and as an antipruritic, and it has been used in spinal anesthesia. In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. In addition, tetracaine serves as an allosteric blocker of channel function. At low concentrations, tetracaine gives rise to an initial prevention of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely.
| Molecular Weight | 300.82 |
| Formula | C15H24N2O2.HCl |
| CAS Number | 136-47-0 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Calcium Channel Products |
|---|
| ω-Agatoxin TK
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca2+ channel blocker. |
| SNX-482
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. |
| ω-Conotoxin MVIIC
ω-Conotoxin MVIIC is a N- and P/Q-type Ca2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release. |
| ω-Conotoxin GVIA
ω-Conotoxin GVIA is an inhibitor of the N-type Ca2+ channel. |
| ω-Conotoxin CnVIIA
ω-Conotoxin CnVIIA, a 27 amino acid neuropeptide toxin, is a N-type calcium current blocker. |
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