Tigloidin (Tigloyl pseudotropine)
(Synonyms: 惕各酰托品因,Tigloyl pseudotropine; Tiglylpseudotropine; Tiglyssin) 目录号 : GC30442Tiglodin (Tigloyl pseudotropine) 是阿托品的类似物,具有抗胆碱能活性。
Cas No.:495-83-0
Sample solution is provided at 25 µL, 10mM.
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Tigloidin is an analogue of atropine, with anticholinergic activity.
Tigloidine hydrobromide (20-60 mg/kg, i.p.) fails to protect the mice against the lethal effect of physostigmine, but at 100 mg/kg and above, it protects 80% of the animals against the lethal effect. Tigloidine markedly prevents tremor and salivation produced by tremorine at 80-100 mg/kg, but fails to prevent these effects in doses up to 40 mg/kg. Tigloidine (up to 100 mg/kg, i.p) does not significantly affects reserpine and tetrabenazine induced sedation and ptosis in mice. Tigloidine (25-50 mg/kg, i.p.) also fails to cause any behavioral changes in the cats[1].
[1]. Sanghvi I, et al. Pharmacology of a potential anti-Parkinson agent: tigloidine. Eur J Pharmacol. 1968 Oct;4(3):246-53.
Cas No. | 495-83-0 | SDF | |
别名 | 惕各酰托品因,Tigloyl pseudotropine; Tiglylpseudotropine; Tiglyssin | ||
Canonical SMILES | C/C=C(C)/C(O[C@H]1C[C@@H](N2C)CC[C@@H]2C1)=O | ||
分子式 | C13H21NO2 | 分子量 | 223.31 |
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。 |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.4781 mL | 22.3904 mL | 44.7808 mL |
5 mM | 0.8956 mL | 4.4781 mL | 8.9562 mL |
10 mM | 0.4478 mL | 2.239 mL | 4.4781 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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Specificities of the enzymes of N-alkyltropane biosynthesis in Brugmansia and Datura
The enzymes N-methylputrescine oxidase (MPO), the tropine-forming tropinone reductase (TRI), the pseudotropine-forming tropinone reductase (TRII), the tropine:acyl-CoA transferase (TAT) and the pseudotropine:acyl-CoA transferase (PAT) extracted from transformed root cultures of Datura stramonium and a Brugmansia candida x aurea hybrid were tested for their ability to accept a range of alternative substrates. MPO activity was tested with N-alkylputrescines and N-alkylcadaverines as substrates. TRI and TRII reduction was tested against a series of N-alkylnortropinones, N-alkylnorpelletierines and structurally related ketones as substrates. TAT and PAT esterification tests used a series of N-substituted tropines, pseudotropines, pelletierinols and pseudopelletierinols as substrates to assess the formation of their respective acetyl and tigloyl esters. The results generally show that these enzymes will accept alien substrates to varying degrees. Such studies may shed some light on the overall topology of the active sites of the enzymes concerned.
Factors regulating tropane-alkaloid production in a transformed root culture of a Datura candida × D. aurea hybrid
Using in combination an analysis of (i) the levels of enzyme activities present, (ii) the pool sizes of metabolic intermediates and end products and (iii) the effects of feeding metabolic intermediates, the limitations ? flux into tropane alkaloids in a Datura root culture have been examined. This culture, produced by transforming a Datura candida × D. aurea hybrid with Agrobacterium rhizogenes, is found to be highly competent in the biosynthesis of both hyoscyamine and scopolamine as well as a wide range of other hygrine-derived alkaloids. It has been found that, of six enzymes which are involved in this pathway, the two initial activities, ornithine decarboxylase (EC 4.1.1.17) and arginine decarboxylase (EC 4.1.1.19), are present at potentially flux-limiting levels, in contrast to those other enzymes assayed which act further down the pathway. An additional limitation to flux, involving the supply of activated acids for condensation with tropine to form the identified tropoyl and tigloyl derivatives, is also indicated from the observed effect of feeding free acids. The relative contribution to flux limitation caused by these two interacting phenomena is inferred from an analysis of the changing relative levels of metabolic intermediates and end products as cultures mature.