Dibucaine (Cinchocaine) 是一种钠通道抑制剂。
| Cas No. | 85-79-0 |
| 别名 | 辛可卡因,Cinchocaine |
| 化学名 | 2-butoxy-N-[2-(diethylamino)ethyl]quinoline-4-carboxamide |
| Canonical SMILES | CCCCOC1=NC2=CC=CC=C2C(=C1)C(=O)NCCN(CC)CC |
| 分子式 | C20H29N3O2 |
| 分子量 | 343.46 |
| 溶解度 | ≥ 16.45mg/mL in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Dibucaine is a local anesthetic of the amide type now generally used for surface anesthesia.Target: Sodium ChannelDibucaine is an amide local anesthetic. Dibucaine reduced the degradation of BSA-gold complex in the reservosomes, which was not caused either by an inhibition of the whole proteolytic activity of the parasite or by a reduction on the expression levels of cruzipain [1].Dibucaine, a quaternary ammonium compound, inhibited SChE to a minimum within 2 min in a reversible manner. The inhibition was very potent. It had an IC(50) of 5.3 microM with BuTch or 3.8 microM with AcTch. The inhibition was competitive with respect to BuTch with a K(i) of 1.3 microM and a linear-mixed type (competitive/noncompetitive) with respect to AcTch with inhibition constants, K(i) and K(I) of 0.66 and 2.5 microM, respectively. Dibucaine possesses a butoxy side chain that is similar to the butryl group of BuTch and longer by an ethylene group from AcTch [2]. References:
[1]. Souto-Padron, T., A.P. Lima, and O. Ribeiro Rde, Effects of dibucaine on the endocytic/exocytic pathways in Trypanosoma cruzi. Parasitol Res, 2006. 99(4): p. 317-20.
[2]. Elamin, B., Dibucaine inhibition of serum cholinesterase. J Biochem Mol Biol, 2003. 36(2): p. 149-53. |
