Procaine (hydrochloride)
(Synonyms: Novocaine) 目录号 : GC44685
Procaine (hydrochloride) is an analytical reference standard categorized as a local anesthetic that is used as an adulterant.
Cas No.:51-05-8
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
Procaine hydrochloride is a local anesthetic drug of the amino ester group.Target: OthersProcaine hydrochloride is a local anesthetic of the ester type that has a slow onset and a short duration of action.Procaine (0.01-100 microM) inhibited the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. Procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM [1]. Procaine is a DNA-demethylating agent that produces a 40% reduction in 5-methylcytosine DNA content as determined by high-performance capillary electrophoresis or total DNA enzyme digestion. Procaine can also demethylate densely hypermethylated CpG islands. Procaine also has growth-inhibitory effects in these cancer cells, causing mitotic arrest [2]. Procaine functions as an excitant of limbic system cells, and that procaine alters synaptic transmission in some, but not all, output pathways from the amygdale [3].
References:
[1]. Fan, P. and F.F. Weight, Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons. Neuropharmacology, 1994. 33(12): p. 1573-9.
[2]. Villar-Garea, A., et al., Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer Res, 2003. 63(16): p. 4984-9.
[3]. Adamec, R.E. and C. Stark-Adamec, The effects of procaine HCl on population cellular and evoked response activity within the limbic system of the cat. Evidence for differential excitatory action of procaine in a variety of limbic circuits. Prog Neuropsychopharmacol Biol Psychiatry, 1987. 11(4): p. 345-64.
| Cas No. | 51-05-8 | SDF | |
| 别名 | Novocaine | ||
| Canonical SMILES | NC1=CC=C(C(OCCN(CC)CC)=O)C=C1.Cl | ||
| 分子式 | C13H20N2O2•HCl | 分子量 | 272.8 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 14 mg/ml,Ethanol: 16 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | 4°C, protect from light ,unstable in solution, ready to use. |
| 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 | 3.6657 mL | 18.3284 mL | 36.6569 mL |
| 5 mM | 0.7331 mL | 3.6657 mL | 7.3314 mL |
| 10 mM | 0.3666 mL | 1.8328 mL | 3.6657 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。
Pharmacological and toxicological aspects of combination of beta-lactam and aminoglycoside antibiotic, prednisolone and Procaine hydrochloride on the example of Vetramycin
Pol J Vet Sci 2003;6(4):279-96.PMID:14703874doi
Vetramycin is an injectable veterinary compound for animal use only. In veterinary medicine, it has been used for a long time as a bactericidal beta-lactam and aminglycoside antibiotics combination, extending the bactericidal spectrum of these substances. This compound, in addition to bactericidal Procaine penicillin and dihydrostreptomycin (DHS), contains also prednisolone acetate and Procaine hydrochloride, two biologically active substances. Prednisolone, a glucocorticoide, has an antiinflammatory, antiallergic, antiitchical and analgesic effect. Procaine hydrochloride, in turn, has a local anaesthetic effect and attenuates pain caused by irritable properties of antibiotics at the injection sites. The average dosage of, respectively, Procaine benzylpenicillin (I.U./kg(-1) b.w.), DHS (microg/kg(-1) b.w.), prednisolone acetate (microg/kg(-1) b.w.) and Procaine hydrochloride (mg/kg(-1) b.w.) in horses, cattle, pigs is 6000-15000, 10-11, 0.24-0.6 and 1.2-3.0; s.i.d., in sheep, foals, calves, piglets is 20000-40000, 10, 0.8-1.6 and 4-8; s.i.d., in dogs and cats is 30000-200000, 10, 0.8-1.6 and 4-8; s.i.d.. Intramammary injection dose (Vetramycin antimastitis ointment in syringe) in cows is 1000000 I.U. of Procaine benzylpenicillin + 1000000 I.U. of dihydrostreptycin sulphate per quarter of udder, s.i.d., during 3 successive days.
Effect of local anesthetic drug Procaine hydrochloride on the conformational stability of bovine hemoglobin: Multi-spectroscopic and computational approaches
J Biomol Struct Dyn 2022;40(19):8938-8948.PMID:33970817DOI:10.1080/07391102.2021.1920465.
The interaction between bovine hemoglobin (BHb) and local anesthetic drug Procaine hydrochloride (PCH) was examined by spectroscopic and computational studies. Intrinsic fluorescence analysis explored the ground-state complex formation in the binding of PCH with BHb through static quenching mechanism. The binding constants (Kb) are 29.38 × 103, 22.54 × 103 and 17.99 × 103 M-1 at 288, 298 and 308 K, respectively, and the ratio of BHb:PCH was 1:1 in the interaction mechanism of PCH and BHb. The acquired thermodynamic parameters (ΔH0, ΔG0 and ΔS0) demonstrated that interaction mechanism is spontaneous and enthalpy driven. The van der Waals forces and hydrogen bonding have been played a predominant role in the binding mechanism. The UV-vis spectroscopy validates the ground-state complexation between PCH and BHb and the binding constant (Kb) has been evaluated utilizing Benesi-Hildebrand equation. Fluorescence resonance energy transfer (FRET) results have demonstrated that the distance between donor (BHb) and acceptor (PCH) is very short (2.34 nm) suggesting a significant probability to energy transfer from BHb to PCH. Synchronous fluorescence results revealed that the alteration in the micro-environment of Tyrosine (Tyr) is more than tryptophan (Trp) residues suggesting that PCH molecule is close to Tyr residue. The secondary structure alterations were confirmed by CD, 3-D fluorescence and FT-IR spectroscopic measurements. Moreover, computational analyses further corroborated that PCH molecules are closer to Tyr residues as compared to Trp residues of BHb during the interaction process. The BHb-PCH complexes may contribute to a deeper understanding of the metabolism of drug, blood circulation process and may help to illustrate the relationship between functions and structure of BHb.Communicated by Ramaswamy H. Sarma.
Procaine hydrochloride fails to relieve pain in patients with acute pancreatitis
Digestion 2004;69(1):5-9.PMID:14755147DOI:10.1159/000076541.
Background: Several analgesics are in use for pain control in patients with acute pancreatitis. Procaine hydrochloride (Procaine) has a long tradition and is recommended by the German Society of Gastroenterology and Metabolic Diseases for pain treatment in patients with acute pancreatitis. There is no controlled trial showing that Procaine could be effective for pain treatment. Methods: In an open, randomized, controlled trial, 107 patients (76 male, 31 female; mean age 45 +/- 12 years) were included and randomized either to receive Procaine (n = 55) or pentazocine (n = 52) for pain relief. Procaine 2 g/ 24 h was administered by continuous intravenous infusion, pentazocine 30 mg was administered every 6 h as a bolus intravenous injection. Pentazocine was additionally administered on demand whenever required in patients of both treatment groups and its total consumption was recorded. Pain scores were assessed twice daily on a visual analogue scale. Results: Patients receiving Procaine were significantly more likely to request additional analgesics compared to patients treated with pentazocine alone, 98 vs. 44%, respectively (p < 0.001). Procaine did not reduce the amount of pentazocine required for pain control. The amount of pentazocine given in both groups was not statistically significantly different. Recorded pain scores were significantly lower (p < 0.001) in patients in the pentazocine group during the first 3 days of analgesic treatment. From day 4 on there was no significant difference in pain scores among the two groups. Conclusion: Thus, intravenous Procaine treatment is not effective for pain control in patients with acute pancreatitis.
Procaine hydrochloride as a monoamine oxidase inhibitor: implications for Geriatric therapy
J Am Geriatr Soc 1977 Feb;25(2):90-3.PMID:833415DOI:10.1111/j.1532-5415.1977.tb00237.x.
The results of in vitro experiments showed that inhibition by Procaine hydrochloride of monoamine oxidase (MAO) from either rat brain or liver was substrate-dependent. Procaine was more effective in inhibiting serotonin oxidation than phenylethylamine oxidation and had an intermediate effect on tryptamine oxidation. MAO activity in tissue homogenates from rats treated with Procaine (150 mg/kg intraperitoneally) was inhibited most in liver, less in heart, and only very slightly brain for a duration of up to 8 hours. Procaine injected in that dose did not alter brain norepinephrine levels and elevated only slightly the brain serotonin levels. It did not protect against the degradation of exogenous radioactive tryptamine in brain. These data confirm and extend prior observations on in vitro inhibition of MAO by Procaine and suggest that in high doses Procaine may inhibit MAO weakly in vivo. If the reported usefulness of Procaine preparations in treating geriatric patients indeed depends upon MAO inhibition, more effective inhibitors would seem to be available.
Colorimetric determination of Procaine hydrochloride in pharmaceutical preparations
J Pharm Sci 1980 Mar;69(3):346-8.PMID:7381718DOI:10.1002/jps.2600690326.
A new rapid, specific, and convenient colorimetric method for the determination of Procaine hydrochloride in pharmaceutical preparations is described. This method is based on measurement of the intensity of the orange-red color developed when Procaine hydrochloride is allowed to react with 1,2-naphthoquinone-4-sulfonic acid sodium salt in aqueous solution. Beer's law is followed over 6.0--20.0 micrograms/ml. The method was applied to the determination of Procaine hydrochloride in Procaine hydrochloride, Procaine hydrochloride injection with or without epinephrine, penicillin G Procaine, penicillin G Procaine injection, and fortified Procaine penicillin injection (BP). The results were comparable to those obtained by official procedures. Because of its simplicity, sensitivity, and accuracy, this method is particularly suited for routine analysis of official preparations of Procaine hydrochloride.