L-Hyoscyamine sulfate
(Synonyms: L-莨菪碱硫酸盐; Daturine sulfate) 目录号 : GC39130
L-Hyoscyamine sulfate (Daturine sulfate) 是一种莨菪烷生物碱，是茄科某些植物的次生代谢物。体外实验表明它是一种 mAChR 受体的拮抗剂。
Cas No.:620-61-1
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
L-Hyoscyamine sulfate (Daturine sulfate) is a tropane alkaloid that is a secondary metabolite found in certain plants of the solanaceae family. In vitro it has been shown to be an antagonist of mAChR[1].
[1]. Jones JB, et al. Sublingual hyoscyamine sulfate in combination with ketorolac tromethamine for ureteral colic: a randomized, double-blind, controlled trial. Ann Emerg Med. 2001 Feb;37(2):141-6.
| Cas No. | 620-61-1 | SDF | |
| 别名 | L-莨菪碱硫酸盐; Daturine sulfate | ||
| Canonical SMILES | CN1[C@@H]2C[C@@H](OC([C@@H](C3=CC=CC=C3)CO)=O)C[C@H]1CC2.[0.5H2SO4] | ||
| 分子式 | C17H24NO5S0.5 | 分子量 | 338.41 |
| 溶解度 | DMSO : 25 mg/mL (73.87 mM; Need ultrasonic) | 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 | 2.955 mL | 14.775 mL | 29.55 mL |
| 5 mM | 0.591 mL | 2.955 mL | 5.91 mL |
| 10 mM | 0.2955 mL | 1.4775 mL | 2.955 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。
MIL-53(Fe)-derived ant nest structured porous carbon nanospheres CuFeS2 /C for the determination of atropine enantiomeric impurity L-Hyoscyamine
Chirality 2022 Dec;34(12):1526-1537.PMID:36190759DOI:10.1002/chir.23500.
In this work, an ant nest structured porous carbon nanosphere had been developed for the recognition detection of the atropine (ATP) enantiomers D-hyoscyamine (D-HSM) and L-Hyoscyamine (L-HSM). Firstly, Fe-based organic framework was used as the substrate, and Cu ions and sulfur ions were separately introduced to obtain CuFeS2 with ant nest structure by hydrothermal incubation. Then CuFeS2 /C porous nanospheres (PNSs) were obtained by high-temperature calcination. The composite-modified electrode exhibited superior electrochemical performance for L-HSM due to the synergistic effect of CuFeS2 cubic crystals and porous carbon, which has the high specific surface area of the ant nest structure. In addition, the molecularly imprinted polymer (MIP) about L-HSM formed with sulfonated-β-cyclodextrin (S-β-CD) and L-arginine (L-Arg) by cyclic voltammetry showed strong chiral recognition of D/L-HSM (ATP). Therefore, a novel electrochemical sensor was constructed based on CuFeS2 /C PNSs and MIP to detect L-HSM by differential pulse voltammetry. Under the optimal conditions, the peak current density of L-HSM showed a good linearity in the concentration range of 0.02-4.6 μM with LOD and LOQ of 0.45 and 1.5 nM, respectively. The oxidation peaks of L-HSM and D-HSM were successfully identified from the racemic ATP, and the oxidation peak potential difference (ΔEp ) between them was 0.138 V. In conclusion, the sensor showed excellent reproducibility, repeatability, and stability and had been applied to the determination of L-HSM in human serum, saliva, and ATP sulfate tablets with satisfactory results.
Determination of L-Hyoscyamine in atropine and D-hyoscyamine in L-Hyoscyamine by chiral capillary electrophoresis as an alternative to polarimetry
Electrophoresis 2003 Aug;24(15):2687-92.PMID:12900883DOI:10.1002/elps.200305492.
A method for the separation of atropine enantiomers, D- and L-Hyoscyamine by capillary electrophoresis (CE) has been developed and validated. The advantages of the CE method compared with polarimetry include smaller amounts of analytes and a lower limit of detection of the unwanted enantiomer. Moreover, the present method enables a baseline separation of the analytes and tropic acid, one of the typical impurities of atropine. The developed enantioseparation of atropine was performed using a commercially available sulfated beta-cyclodextrin and was validated for the determination of L-Hyoscyamine in atropine as well as for the enantiomeric purity of L-Hyoscyamine.
Pharmacokinetics of atropine in dogs after i.m. injection with newly developed dry/wet combination autoinjectors containing HI 6 or HLö 7
Arch Toxicol 1996;70(5):293-9.PMID:8852700DOI:10.1007/s002040050276.
To cope with the rapid onset of the life-threatening cholinergic crisis after poisoning with organophosphorus compounds, atropine-oxime preparations should be available in autoinjectors allowing i.m. administration also in the absence of a physician. Such a scenario is conceivable in the battlefield, when nerve agents are disseminated, and can no longer be excluded in civilian areas, as demonstrated most recently in Tokyo. In addition, autoinjectors may be of value in agriculture when medical care is remote. The use of second generation oximes with broad antidotal spectrum, e.g., HI 6 (1-(((4-(aminocarbonyl)pyridinio)methoxy)methyl)-2-((hydr oxyimino)methyl) pyridinium dichloride monohydrate; CAS 34433-31-3) and HLö 7 (1-(((4-(aminocarbonyl)pyridinio)methoxy)methyl) 2,4-bis((hydroxyimino)methyl) pyridinium dimethanesulfonate; CAS 145613-73-6) is only possible in dry/wet autoinjectors because their stability is limited in concentrated solution. To detect a possible delay in atropine absorption by the two oximes, the pharmacokinetics of atropine after "autoinjection" in beagle dogs were determined. Commercially available autoinjectors from two manufacturers [STI International Ltd (BJ) and Astra Tech (AT)] were filled with atropine sulfate, either alone (2 mg) or in combination with HI 6 (500 mg) and HLö 7 (200 mg), respectively, and injected according to a complete cross-over design. Atropine concentration was determined as L-Hyoscyamine equivalents in a radioreceptor assay (RRA). In the range of 0.1-6.9 ng/ml, atropine sulfate displaced [N-methyl-3H]-scopolamine methyl chloride ([3H]NMS) competitively from rat cerebral cortex membranes. At 200 pmol/l [3H]NMS, IC50 was 1.4 +/- 0.1 x 10(-9) M atropine (CV = 8.1%). The intra-assay deviation was about 6%; day-to-day deviation in determination of 1 nM (0.695 ng/ml) atropine was 2.6% (CV = 5.2%). AT autoinjectors containing HI 6 delivered only 1.81 mg atropine sulfate while 2.14 mg was released by the other injectors. According to the manufacturer, the reduced delivery was caused by a defective Teflon-coated O-ring as detected later on in the batch used. To allow comparison of the bioavailability of atropine from various autoinjectors, the AUCs were normalized to a constant dose. The atropine absorption half-time (7 min) was not affected either by the autoinjector type or by the combination with oximes. The other pharmacokinetic data likewise did not reveal any differences between the groups. Maximal plasma concentration was 33 ng ml-1, elimination half-life 52 min, Vapp 3.2 l kg-1 and Clpl 44 ml min-1 kg-1. The relatively high clearance of L-Hyoscyamine is discussed.
Purification of the muscarinic acetylcholine receptor from porcine atria
Proc Natl Acad Sci U S A 1984 Aug;81(15):4993-7.PMID:6589642DOI:10.1073/pnas.81.15.4993.
The muscarinic acetylcholine receptor from porcine atria has been purified 100,000-fold to homogeneity by solubilization in digitonin/cholate and sequential chromatography on wheat germ agglutinin-agarose, diethylaminoethylagarose, hydroxylapatite, and 3-(2'-aminobenzhydryloxy)tropane-agarose. The yield of purified receptor was 4.3% of that found in the membrane fraction, and the purified receptor bound 11.1-12.8 nmol of L-[3H]quinuclidinyl benzilate per mg of protein, corresponding to a binding component Mr of 78,400-90,000. The purified receptor preparation consisted of two polypeptides in approximately equimolar amounts when examined on silver-stained sodium dodecyl sulfate/polyacrylamide gels. The larger polypeptide (Mr 78,000 on 8% polyacrylamide gels) was specifically alkylated with [3H]propylbenzilylcholine mustard, whereas the smaller polypeptide (Mr 14,800) was not labeled. The possibility that the small polypeptide is a contaminant fortuitously appearing in equimolar amounts with the large polypeptide cannot be ruled out at this time. The purified preparation was highly stable, with no measurable change in the number of ligand binding sites or the gel pattern after 1 month's storage on ice. Scatchard analysis showed a single class of binding sites for the antagonist L-[3H]quinuclidinyl benzilate with a dissociation constant of 61 +/- 4 pM. Equilibrium titration experiments demonstrated that the antagonist L-Hyoscyamine displaced L-[3H]quinuclidinyl benzilate from a single class of sites (Kd = 475 +/- 30 pM), whereas the agonist carbamoylcholine interacted at two populations of sites (53% +/- 3% high affinity, Kd = 1.1 +/- 0.3 microM; 47% +/- 3% low affinity, Kd = 67 +/- 14 microM). The ligand binding data were very similar to that for the membrane-bound receptor, suggesting that the receptor has not been altered radically during purification.