Endogenous Metabolite; alpha7 nicotinic receptors

氯化胆碱（0 或 70 μM，4 天）有利于证明细胞存活并保持细胞活力 [1]。

氯化胆碱（皮下注射，0.2 和 100 mg/kg/h，24 或 48 小时）可以有效降低巨噬细胞释放肿瘤因子 (TNF)，并减轻女性 C57/Bl6 研究中的有害反应 [2]。

细胞活力测定[1]
细胞类型：大鼠嗜铬细胞瘤细胞 PC12
测试浓度： 0 或 70 μM
孵育时间： 4 天
实验结果： 70 μM 时细胞活力为 94%，0 μM 时细胞活力为 83%。与未处理组相比，70 μM 时显示 DNA 碎片（细胞凋亡特征）的细胞数量减少了 8.5%。

Animal/Disease Models: Female C57/Bl6 mouse postoperative pain model [2]
Doses: 0.2 and 100 mg/kg/h
Route of Administration: subcutaneous injection, 24 or 48 hrs (hrs (hours))
Experimental Results: Heat allergy was diminished after surgery, and maximum efficacy was achieved after 48 hrs (hrs (hours)) of treatment . The ED50 value of the choline dose is 1.7 mg/kg/h. Allergic responses to punctate mechanical stimulation were diminished in a dose-dependent manner with an ED50 value of 4.7 mg/kg/h at 48 hrs (hrs (hours)) but not at 24 hrs (hrs (hours)) after infusion.

Absorption, Distribution and Excretion
A study of choline pharmacokinetics was undertaken in four patients receiving long-term total parenteral nutrition. On consecutive days, 7, 14, 28, and 56 mmol choline chloride were intravenously infused over a 12-hour period in each subject. The choline concentration was determined in plasma at baseline, 1/4, 1, 3, 6, and 12 hours, and 3 and 12 hours after the infusion ended, and in daily 24-hour urine collections. Analysis of variance showed the data fit a two-compartment model in which elimination from the central compartment was saturable significantly better than a one-compartment model in all four subjects (p < 10-8 in all cases), and significantly better than a nonsaturating model in three of the four subjects (p = 1.0 x 10-9, 7.5 x 10-6, 9.4 x 10-11, respectively). The model allowed estimates of the rate constant for choline elimination at ambient levels, first-order rate constants for transfer between central and peripheral compartments, the dissociation constant for the saturable elimination process, the apparent volume of distribution in the central compartment, the steady-state volume of distribution, and the quantities of choline in the central compartment and in the readily exchangeable pool.
Choline chloride, a strong base, was surprisingly well absorbed at pH 7, but absorption was less at lower ph values.
Choline is absorbed from diet as such or as lecithin. Latter is hydrolyzed by intestinal mucosa to glycerophosphoryl choline, which either passes to liver to liberate choline or to peripheral tissues via intestinal lymphatics. /Choline/
Choline chloride (1-2 g, 4 times daily, increasing every 2 days, reaching max of 2-5 g 4 times daily, orally) dose-dependently incr serum choline levels in patients with Huntington's Disease, & incr cerebrospinal fluid choline levels not related to serum levels.
For more Absorption, Distribution and Excretion (Complete) data for CHOLINE CHLORIDE (11 total), please visit the HSDB record page.

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Metabolism / Metabolites
Free choline is not fully absorbed, especially after large doses, & intestinal bacteria metabolize choline to trimethylamine. /Choline/
/The/ ability to form choline /de novo via the methylation of phosphatidylethanolamine using S-adenosylmethionine as the methyl donor, mostly in the liver,/ means that some of the demand for choline can ... be met using methyl groups derived from 1-carbon metabolism (via methyl-folate and methionine). Several vitamins (folate, vitamin B12, vitamin B6, and riboflavin) and the amino acid methionine interact with choline in 1-carbon metabolism ... Methionine, methyl-tetrahydrofolate (THF), and choline can be fungible sources of methyl groups. /Choline/
Before choline can be absorbed in the gut, some is metabolized by bacteria to form betaine and methylamines (which are not methyl donors) ... Although some free choline is excreted with urine, most is oxidized in the kidney to form betaine ... /Choline/
Acetylcholine is one of the most important neurotransmitters used by neurons in the memory centers of the brain (hippocampus and septum). Choline accelerates the synth and release of acetylcholine in nerve cells. Choline used by brain neurons is largely derived from membrane lecithin /(phosphatidylcholine)/, or from dietary intake of choline and lecithin ... Choline derived from lecithin may be especially important when extracellular choline is in short supply, as might be expected to occur in advanced age because of decr brain choline uptake ... /Choline/
For more Metabolism/Metabolites (Complete) data for CHOLINE CHLORIDE (6 total), please visit the HSDB record page.

Maximum Drug Dose
The tolerable upper limit for choline has been set at 3 g/day.
Coates, P.M., Blackman, M.R., Cragg, G.M., Levine, M., Moss, J., White, J.D. (Ed), Encyclopedia of Dietary Supplements. Marcel Dekker, New York, NY, p. 109 (2005)

The Tolerable Upper Intake Level (UL) for adults is 3.5 g/day.

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Interactions
Repeated admin of choline chloride to female rats incr liver necrosis caused by carbon tetrachloride. LEDDA GM ET AL; RASS MED SARDA 80(4) 215 (1977)

Lithium admin potentiates effect of exogenous choline on brain acetylcholine levels.

[1]. Apoptosis is induced by choline deficiency in fetal brain and in PC12 cells. Brain Res Dev Brain Res. 1997 Jul 18;101(1-2):9-16.

[2]. Antinociceptive and anti-inflammatory effects of choline in a mouse model of postoperative pain. Br J Anaesth. 2010 Aug;105(2):201-7.

Choline chloride appears as white crystals. Practically neutral aqueous solution. (NTP, 1992)
Choline chloride is a quaternary ammonium salt with choline cation and chloride anion. It has a role as an animal growth promotant. It is a chloride salt and a quaternary ammonium salt. It contains a choline.
A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.

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Mechanism of Action
Choline has several roles in body. It is an important component of phospholipids, affects mobilization of fat from liver (lipotropic action), acts as methyl donor, & is essential for formation of neurotransmitter acetylcholine. /Choline/
Several mechanisms are suggested for the cancer-promoting effect of a choline-devoid diet. These incl incr cell proliferation related to regeneration after parenchymal cell death occurs in the choline deficient liver, hypomethylation of DNA (alters expression of genes), reactive oxygen species leakage from mitochondria with incr lipid peroxidation in liver, activation of protein kinase C signaling due to accumulation of diacylglycerol in liver, mutation of the fragile histidine triad (FHIT) gene, which is a tumor suppressor gene, and defective cell-suicide (apoptosis) mechanisms. Loss of phposphatidylethanolamine N-methyl-transferase (PEMT) function may also contribute to malignant transformation of hepatocytes. /Choline/
Acetylcholine is one of the most important neurotransmitters used by neurons in the memory centers of the brain (hippocampus and septum). Choline accelerates the synth and release of acetylcholine in nerve cells. /Choline/
Female Sprague-Dawley rats received approximately 300 mg/kg per day of choline chloride through their drinking water on days 11 of pregnancy through birth and the level of nerve growth factor (NGF) in the hippocampus and frontal cortex of their male offspring was measured at 20 and 90 days of age. Prenatal choline supplementation caused significant increases in hippocampal NGF levels at 20 and 90 days of age, while levels of NGF in the frontal cortex were elevated in choline-supplemented rats at 20 days of age, but not 90 days of age. These results suggest that increases in NGF levels during development or adulthood may be one mechanism underlying improvements in spatial and temporal memory of adult rats exposed to elevated levels of choline chloride perinatally.

C5H14CLNO

139.6238

139.076

67-48-1

Choline bitartrate;87-67-2;Choline Fenofibrate;856676-23-8;Choline-d4 chloride;285979-70-6;Choline-d9 chloride;61037-86-3;Choline Chloride-13C3;Choline theophyllinate;4499-40-5;Glycerophosphoinositol choline;425642-32-6;Choline-d6 chloride;Choline-d13 chloride;352438-97-2;Choline-13C2 chloride;202190-49-6; 425642-32-6 (choline); 129830-95-1 (free); 425642-29-1 (potassium); 425642-30-4 (sodium)

6209

White to off-white solid powder

1.205 g/cm3

302-305 °C (dec.)(lit.)

20.23

1

2

2

8

46.5

0

SGMZJAMFUVOLNK-UHFFFAOYSA-M

InChI=1S/C5H14NO.ClH/c1-6(2,3)4-5-7;/h7H,4-5H2,1-3H3;1H/q+1;/p-1

2-hydroxyethyl(trimethyl)azanium;chloride

CHOLINE CHLORIDE; 67-48-1; Hepacholine; Lipotril; Paresan; 2-Hydroxy-N,N,N-trimethylethanaminium chloride; Hormocline; (2-Hydroxyethyl)trimethylammonium chloride;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 140 mg/mL (~1002.72 mM)
H2O : ≥ 100 mg/mL (~716.23 mM)

配方 1 中的溶解度: ≥ 3.5 mg/mL (25.07 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 35.0 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 3.5 mg/mL (25.07 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 35.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 3.5 mg/mL (25.07 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 35.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 130 mg/mL (931.10 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。