Dibucaine hydrochloride
目录号 : GC35860
Dibucaine 盐酸盐 (Cinchocaine hydrochloride) 有局部麻醉活性。
Cas No.:61-12-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dibucaine hydrochloride (Cinchocaine hydrochloride) is a local anesthetic of the amide type now generally used for surface anesthesia.Target: Sodium ChannelDibucaine hydrochloride (Cinchocaine hydrochloride) is an amide local anesthetic. Dibucaine hydrochloride (Cinchocaine hydrochloride) 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 hydrochloride (Cinchocaine hydrochloride), 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 hydrochloride (Cinchocaine hydrochloride) possesses a butoxy side chain that is similar to the butryl group of BuTch and longer by an ethylene group from AcTch [2].
[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.
| Cas No. | 61-12-1 | SDF | |
| Canonical SMILES | O=C(C1=CC(OCCCC)=NC2=CC=CC=C12)NCCN(CC)CC.Cl | ||
| 分子式 | C20H30ClN3O2 | 分子量 | 379.92 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6321 mL | 13.1607 mL | 26.3213 mL |
| 5 mM | 0.5264 mL | 2.6321 mL | 5.2643 mL |
| 10 mM | 0.2632 mL | 1.3161 mL | 2.6321 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[Ionic strength influences hemolytic action of Dibucaine hydrochloride]
Masui 2003 Nov;52(11):1174-80.PMID:14661561doi
Background: Little is known about effect of ionic strength on local anesthetic toxicity. Using human erythrocytes, hemolytic action of dibucaine in solutions of various ionic strength was investigated. Methods: The critical micellar concentration (CMC) of dibucaine and the dibucaine level that causes destruction of half of the red blood cells in vitro (EC50 value) were determined in solutions of various ionic strength. Results: The mean CMC values of the dibucaine solutions adjusted to ionic strength 0.15, 0.30, 0.45 and 0.90 with NaCl, were 35.3, 22.6, 15.9 and 9.6 mM, respectively. The mean EC50 values of these solutions measured at 5 sec were 22.5, 16.0, 12.6 and 8.2 mM, respectively, and those at 30 min were 4.9, 4.5, 4.5 and 2.6 mM, respectively. There was a significant correlation between mean CMC values and mean EC50 values at 5 sec but not at 30 min in the solution of the same ionic strength. Conclusions: These findings indicated that the mechanism of dibucaine-induced hemolysis within a few seconds is through membrane lysis, whereas dibucaine-induced hemolysis at 30 min is caused by another mechanism. Because each mechanism is enhanced by high ionic strength, dibucaine dissolved in salt solution should not be administered intrathecally.
The Effect of Trigger Point Injections on Pain in Patients with Advanced Cancer
Korean J Fam Med 2019 Sep;40(5):344-347.PMID:31487973DOI:10.4082/kjfm.18.0065.
Background: It has been reported that in 62.5% of cases of incurable cancer pain, the complaint is due to myofascial pain syndrome. Trigger point injections using Dibucaine hydrochloride help patients with such cancer pain. This study evaluated the efficacy of trigger point injections for alleviating pain in patients with advanced cancer. Methods: Twenty patients with advanced cancer who had a life expectancy of 6 months or less and had been diagnosed with myofascial pain syndrome were treated with trigger point injections. Prior to treatment, a Visual Analog Scale (VAS) was used to measure the resting pain level and discomfort upon application of pressure on the site of pain. These values were compared with last treatment measurements. Results: The mean pre-treatment VAS scores for pain at rest and upon application of pressure on the pain site were 7.3 and 9.0, respectively. These scores decreased significantly to 1.95 and 3.2, respectively, after the treatment (P<0.05). Conclusion: Trigger point injection is an alternative and effective pain control modality for advanced cancer patients with myofascial pain syndrome.
Design of a rate- and time-programming drug release device using a hydrogel: pulsatile drug release from kappa-carrageenan hydrogel device by surface erosion of the hydrogel
Colloids Surf B Biointerfaces 2001 Apr;20(4):355-359.PMID:11166546DOI:10.1016/s0927-7765(00)00207-1.
We have found that a repetitive pulsatile drug release with a certain time interval is observed from a monolithic hydrogel device by surface erosion of the hydrogel. As a model system of pulsatile drug release, Dibucaine hydrochloride and kappa-carrageenan hydrogel were chosen as a drug and a device, respectively. Electrostatic interactions between Dibucaine hydrochloride and kappa-carrageenan polymer segments are strong, since Dibucaine hydrochloride is positively charged and each disaccharide repeating unit of kappa-carrageenan chains has one sulfate group. Dibucaine hydrochloride was loaded into the hydrogel by immersing dry kappa-carrageenan hydrogel disks in a Dibucaine hydrochloride solution for 24 h. The pulsed release of Dibucaine hydrochloride from the device was observed every 50 min between 30 and 250 min after the release starts. The weight of kappa-carrageenan hydrogel decreases in an oscillatory manner with time in distilled water. The oscillatory changes observed in the hydrogel weight in distilled water are considered to be caused by influx and efflux of water molecules into and from the surface and core of the hydrogel and by polymer liberation from the hydrogel. This phenomenon was well explained by our kinetic model [Colloids and Surfaces B 8 (1996) 93-100]. The time interval between pulses observed in drug release coincides with that observed in the oscillatory weight change of the hydrogel. From these, it was concluded that the pulsatile release of Dibucaine hydrochloride from the device was caused by the pulsatile liberation of swollen kappa-carrageenan hydrogel from the surface of the device.
Photosensitivity reaction to dibucaine. Case report and experimental induction
Arch Dermatol 1979 Aug;115(8):986-7.PMID:464631doi
In a 13-year-old girl, photoallergic dermatitis was caused by Dibucaine hydrochloride, which was used as a local anesthetic in the treatment of her dental caries. The action spectrum for the photosensitivity reaction was in the long-wave ultraviolet (UVA) range. Spectrophotometrically, dibucaine absorbed UVA up to 380 nm, and in the vitro irradiated chemical showed an altered absorption spectrum. The agent is fluorescent under UVA light. The allergic photocontact sensitization could be experimentally induced in guinea pigs. The chemical properties and high sensitization rate of experimental induction suggested that dibucaine may be a potent photosensitizing chemical. Dibucaine should be included in routine photopatch test materials.
Preparation and properties of carrageenan microspheres containing allopurinol and local anesthetic agents for the treatment of oral mucositis
Colloids Surf B Biointerfaces 2009 Jun 1;71(1):27-35.PMID:19181495DOI:10.1016/j.colsurfb.2009.01.003.
For the treatment of oral mucositis, carrageenan microspheres containing allopurinol and local anesthetic agents, such as lidocaine hydrochloride, Dibucaine hydrochloride and tetracaine hydrochloride were prepared using a spray-drying method. As base materials, kappa-carrageenan and iota-carrageenan were evaluated, since carrageenan mitigates bitter taste of lidocaine hydrochloride, Dibucaine hydrochloride and tetracaine hydrochloride. The microspheres were spherical and their average diameters were about 10 microm. The drug loading efficiency was more than 70%. Allopurinol and local anesthetic agents became amorphous by the spray drying. Allopurinol and the local anesthetic agents were released from the microspheres for at least 400 min when iota-carrageenan was used as a base material. On the other hand, the release was prolonged to 600 min when kappa-carrageenan was used. The microspheres were spread and made membranes at the air/water interfaces immediately after dropped on the water surfaces. The properties of the microspheres such as dispersing efficacy and membrane production on the water surfaces suggest that the microspheres can uniformly cover inner surfaces of oral cavity to prevent and treat oral mucositis.