Butacaine
(Synonyms: 二丁氨卡因) 目录号 : GC33725
Butacaine是一种局部麻醉剂。
Cas No.:149-16-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Butacaine is a local anesthetic.
| Cas No. | 149-16-6 | SDF | |
| 别名 | 二丁氨卡因 | ||
| Canonical SMILES | CCCCN(CCCOC(C1=CC=C(N)C=C1)=O)CCCC | ||
| 分子式 | C18H30N2O2 | 分子量 | 306.44 |
| 溶解度 | DMSO : ≥ 125 mg/mL (407.91 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2633 mL | 16.3164 mL | 32.6328 mL |
| 5 mM | 0.6527 mL | 3.2633 mL | 6.5266 mL |
| 10 mM | 0.3263 mL | 1.6316 mL | 3.2633 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。
The effect of Butacaine on adenine nucleotide binding and translocation in rat liver mitochondria
Biochem J 1975 Jun;148(3):527-31.PMID:128352DOI:10.1042/bj1480527.
The effect of the local anaesthetic, Butacaine, on adenine nucleotide binding and translocation in rat liver mitochondria partially depleted of their adenine nucleotide content was investigated. The range of Butacaine concentrations that inhibit adenine nucleotide translocation and the extent of the inhibition are similar to the values obtained for native mitochondria. Butacaine does not alter either the total number of atractyloside-sensitive binding sites of depleted mitochondria, or the affinity of these sites for ADP or ATP under conditions where a partial inhibition of the rate of adenine nucleotide translocation is observed. The data are consistent with an effect of Butacaine on the process by which adenine nucleotides are transported across the mitochondrial inner membrane rather than on the binding of adenine nucleotides to sites on the adenine nucleotide carrier. The results are briefly discussed in relation to the use of local anaesthetics in investigations of the mechanism of adenine nucleotide translocation.
Phospholipids as ionophores
J Biol Chem 1976 Mar 10;251(5):1326-32.PMID:1254569doi
The ionophoretic capabilities of phospholipids have been examined by direct measurement in a Pressman cell of the phospholipid-mediated translocation of cations across an organic phase separating two aqueous phases. Cardiolipin and phosphatidic acid were the most active inonophores among the phospholipids tested, with activities comparable to that of X537A in respect to the translocation of divalent cations. Cardiolipin translocates both divalent and monovalent cations at approximately equal rates. The ionophoretic activity of cardiolipin could be modulated by other phospholipids (inhibition), by Butacaine (stimulation), by complexation with cytochrome c (inhibition), and by ruthenium red and lanthanum (inhibition). The rate of translocation of cations mediated by cardiolipin was independent of pH over a wide pH range (5.4 to 8.3). The same general pattern of properties observed for cardiolipin applied to phosphatidic acid except for stimulation by Butacaine. Complexation of phospholipid mixtures, such as asolectin or mitochondrial lipid, with reduced cytochrome c, enhanced the ionophoretic capability of these phospholipids by 1 order of magnitude. The complex thus formed has the properties of a polyionophore. The possible physiological significance of this enormous ionophoretic potential of phospholipids is examined.
[Effect of procaine, nicotinoylprocaine and Butacaine on mammalian cells in culture]
Arzneimittelforschung 1984;34(10):1250-3.PMID:6240271doi
The tertiary amines, procaine and nicotinoylprocaine, cause an increase in the specific activities of two glycohydrolases, alpha-fucosidase and beta-N-acetylhexosaminidase, which are involved in membrane metabolism. The specific activity of alkaline phosphatase, a plasma membrane enzyme, is lowered in muscle cells after addition of procaine or nicotinoylprocaine to the culture medium. The specific activities of two transferases, aspartate-amino-transferase and creatine phosphokinase, are increased by 10(-5) mol/l Butacaine. A combined addition of Butacaine and nicotinoylprocaine causes less effects on the transferases. The specific activities of neutral alpha-glucosidase and beta-N-acetylhexosaminidase are scarcely influenced by Butacaine alone. Only Butacaine and nicotinoylprocaine together lead to an increase of the activities of these hydrolases. These results suggest two different mechanism of action at least concerning these substances: 1. a specific binding of tertiary amines and 2. a coordinated mechanism on the membrane fluidity.
Inhibition by local anaesthetics of adenine nucleotide translocation in rat liver mitochondria
Biochem J 1974 Jun;140(3):413-22.PMID:4280910DOI:10.1042/bj1400413.
1. The mechanism of adenine nucleotide translocation in mitochondria isolated from rat liver was further examined by using the local anaesthetics procaine, Butacaine, nupercaine and tetracaine as perturbators of lipid-protein interactions. Each of these compounds inhibited translocation of ADP and of ATP; Butacaine was the most effective with 50% inhibition occurring at 30mum for 200mum-ATP and at 10mum for 200mum-ADP. The degree of inhibition by Butacaine of both adenine nucleotides was dependent on the concentration of adenine nucleotide present; with low concentrations of adenine nucleotide, low concentrations of butacaine-stimulated translocation, but at high concentrations (greater than 50mum) low concentrations of Butacaine inhibited translocation. Butacaine increased the affinity of the translocase for ATP to a value which approached that of ADP. 2. Higher concentrations of nupercaine and of tetracaine were required to inhibit translocation of both nucleotides; 50% inhibition of ATP translocation occurred at concentrations of 0.5mm and 0.8mm of these compounds respectively. The pattern of inhibition of ADP translocation by nupercaine and tetracaine was more complex than that of ATP; at very low concentrations (less than 250mum) inhibition ensued, followed by a return to almost original rates at 1mm. At higher concentrations inhibition of ADP translocation resulted. 3. That portion of ATP translocation stimulated by Ca(2+) was preferentially inhibited by each of the local anaesthetics tested. In contrast, inhibition by the anaesthetics of ADP translocation was prevented by low concentrations of Ca(2+). 4. The data provide further support for our hypothesis that lipid-protein interactions are important determinants in the activity of the adenine nucleotide translocase in mitochondria.
Solubility-excipient classification gradient maps
Pharm Res 2007 Mar;24(3):530-45.PMID:17245653DOI:10.1007/s11095-006-9169-0.
This study assessed the effect of excipients (sodium taurocholate, 2-hydroxypropyl-f-cyclodextrin, potassium chloride, propylene glycol, 1-methyl-2-pyrrolidone, and polyethylene glycol 400) on the apparent intrinsic solubility properties of eight sparingly soluble drugs (four bases, two neutrals, and two acids): astemizole, Butacaine, clotrimazole, dipyridamole, griseofulvin, progesterone, glibenclamide, and mefenemic acid. Over 1,200 UV-based solubility measurements (pH 3-10) were made with a high-throughput instrument. New equations, based on the "shift-in-pKa" method, were derived to interpret the complicated solubility-pH dependence observed, and poorly predicted by the Henderson-Hasselbalch equation. An intrinsic solubility-excipient classification gradient map visualization tool was developed to rank order the compounds and the excipients. In excipient-free solutions, all of the ionizable compounds formed either uncharged or mixed-charge aggregates. Mefenamic acid formed anionic dimers and trimers. Glibenclamide displayed a tendency to form monoanionic dimers. Dipyridamole and Butacaine tended to form uncharged aggregates. With strong excipients, the tendency to form aggregates diminished, except in the case of glibenclamide. We conclude that a low-cost, compound-sparing, and reasonably accurate high-throughput assay which can be used in early screening to prioritize candidate molecules by their eventual developability via the excipient route is possible with the aid of the "self-organized" intrinsic solubility-excipient classification gradient maps.