Timepidium bromide (Sesden)
(Synonyms: 噻哌溴铵,Sesden; SA504) 目录号 : GC32666
Timepidium bromide (Sesden) (Sesden; SA504) 是一种抗胆碱能药物。
Cas No.:35035-05-3
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
Animal experiment: | Rabbits[1]Timepidium bromide (200 μg/kg) is injected into the femoral vein 5 min prior to 131I-MAA. To evaluate the effects of Timepidium bromide on gastric and duodenal blood flow in cholinergic drug-treated animals, Timepidium bromide is administered in a dose of 200 μg/kg through the femoral vein 3 min before ACh or 5 min after Neost. 131I-MAA is given into the left ventricle of the animals 2 min after ACh and 10 min after Neost. |
References: [1]. Naito K, et al. Effect of timepidium bromide, an anticholinergic agent, on gastric and duodenal blood flow distribution in rabbits. Jpn J Pharmacol. 1982 Feb;32(1):73-80. | |
Timepidium bromide (Sesden; SA504) is an anticholinergic agent.
Effects of Timepidium bromide (TB), acetylcholine (ACh) and neostigmine (Neost) on gastric and duodenal blood flow distribution are studied by the use of 131I-labeled macroaggregated human serum albumin (MAA) in rabbits. In normal rabbits, gastric blood flow is found to be uneven in various regions of the stomach: anterior corpus (50% of total gastric blood flow) greater than posterior corpus (40%) greater than pyloric antrum (7%). Intravenous administration of Timepidium bromide (200 μg/kg) to normal rabbits produces a slight increase in total gastric blood flow, but the increase in the mucosal layer of the pyloric antrum is considerable[1].
[1]. Naito K, et al. Effect of timepidium bromide, an anticholinergic agent, on gastric and duodenal blood flow distribution in rabbits. Jpn J Pharmacol. 1982 Feb;32(1):73-80.
| Cas No. | 35035-05-3 | SDF | |
| 别名 | 噻哌溴铵,Sesden; SA504 | ||
| Canonical SMILES | C[N+]1(C)C/C(CC(OC)C1)=C(C2=CC=CS2)\C3=CC=CS3.[Br-] | ||
| 分子式 | C17H22BrNOS2 | 分子量 | 400.4 |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4975 mL | 12.4875 mL | 24.975 mL |
| 5 mM | 0.4995 mL | 2.4975 mL | 4.995 mL |
| 10 mM | 0.2498 mL | 1.2488 mL | 2.4975 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。
Therapeutic importance of synthetic thiophene
Chem Cent J 2018 Dec 19;12(1):137.PMID:30564984DOI:10.1186/s13065-018-0511-5.
Thiophene and its substituted derivatives are very important class of heterocyclic compounds which shows interesting applications in the field of medicinal chemistry. It has made an indispensable anchor for medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules. It has been reported to possess a wide range of therapeutic properties with diverse applications in medicinal chemistry and material science, attracting great interest in industry as well as academia. It has been proven to be effectual drugs in present respective disease scenario. They are remarkably effective compounds both with respect to their biological and physiological functions such as anti-inflammatory, anti-psychotic, anti-arrhythmic, anti-anxiety, anti-fungal, antioxidant, estrogen receptor modulating, anti-mitotic, anti-microbial, kinases inhibiting and anti-cancer. Thus the synthesis and characterization of novel thiophene moieties with wider therapeutic activity is a topic of interest for the medicinal chemist to synthesize and investigate new structural prototypes with more effective pharmacological activity. However, several commercially available drugs such as Tipepidine, Tiquizium Bromides, Timepidium bromide, Dorzolamide, Tioconazole, Citizolam, Sertaconazole Nitrate and Benocyclidine also contain thiophene nucleus. Therefore, it seems to be a requirement to collect recent information in order to understand the current status of the thiophene nucleus in medicinal chemistry research.
Effect of Timepidium bromide, an anticholinergic agent, on gastric and duodenal blood flow distribution in rabbits
Jpn J Pharmacol 1982 Feb;32(1):73-80.PMID:7087265DOI:10.1254/jjp.32.73.
Effects of Timepidium bromide (TB; anticholinergic agent), acetylcholine (ACh) and neostigmine (Neost) on gastric and duodenal blood flow distribution were studied by the use of 131I-labeled macroaggregated human serum albumin (MAA) in rabbits. In normal rabbits, gastric blood flow was found to be uneven in various regions of the stomach: anterior corpus (50% of total gastric blood flow) greater than posterior corpus (40%) greater than pyloric antrum (7%). Intravenous administration of TB (200 microgram/kg) to normal rabbits produced a slight increase in total gastric blood flow, but the increase in the mucosal layer of the pyloric antrum was considerable. On the other hand, ACh (10 microgram/kg, i.v.) and Neost (50 microgram/kg. i.v.) significantly reduced the total gastric blood flow, in particular, the mucosal blood flow in the anterior and posterior corpus. This reduction in blood flow was virtually abolished by TB and was restored to the normal level. These results suggest that these cholinergic or anticholinergic drugs affect the gastric blood flow and that these effects may be mediated through muscarinic receptors. Blood flow in the duodenum was only slightly changed by these drugs.
Effects of Timepidium bromide, hyoscine-N-butylbromide and atropine on the isolated guinea pig gallbladder and sphincter of Oddi
Jpn J Pharmacol 1980 Jun;30(3):317-23.PMID:7452982DOI:10.1254/jjp.30.317.
Effects of Timepidium bromide (TB), hyoscine-N-butylbromide (HB) and atropine (Atr) were studied on the isolated guinea pig gallbladder and sphincter of Oddi. In the isolated gallbladder, the contraction induced by methacholine was competitively antagonized with TB, HB and Atr: pA2 values for TB, HB and Atr were 8.44, 7.55 and 9.11, respectively. Contraction of gallbladder after field stimulation at 5 Hz was also inhibited by TB, HB and Atr as well as by tetrodotoxin (TTX). On the other hand, TB had no significant influence on the electrically evoked (30 Hz) contraction which remained after treatment with TTX. It was estimated that the inhibitory activity of TB on the contraction of gallbladder was 1/5-1/6 that of Atr and 7 times as potent as HB. In the isolated sphincter of Oddi, TB, HB and Atr reduced the perfusion pressure increased by acetylcholine (ACh), the activity of TB being 1/4 that of Atr and 3 times of HB. The contractile responses to field stimulation (5 Hz) were also inhibited by TB, HB and Atr. The inhibitory activity of TB was 1/5 that of Atr and 12 times of HB. It was also demonstrated that TB produced no significant effect on the noradrenaline (Nor)-induced contraction and isoproterenol (Iso)-induced relaxation in the gallbladder or Nor-induced increase of the perfusion pressure in the sphincter of Oddi. It is suggested that TB acts on the gallbladder and sphincter of Oddi by virtue of its anticholinergic activity.
Effect of Timepidium bromide on the motor activity of the sphincter of Oddi: manometric evaluation of intracholedochal pressure
Curr Med Res Opin 1987;10(9):596-600.PMID:3436156DOI:10.1185/03007998709112413.
The intracholedochal pressure changes induced by Timepidium bromide were studied in 12 patients who had undergone surgery because of gall bladder stones and were receiving transient external bile drainage by the Kehr method. Cholangiomanometric examination, carried out under basal conditions and after an intravenous dose of 15 mg Timepidium bromide, revealed a statistically significant decrease in mean intracholedochal pressure in all 12 patients. It is concluded that Timepidium bromide is likely to exert a direct action on the sphincter of Oddi, decreasing its basal tone and thus causing a decrease in intracholedochal pressure.
Metabolic fate of Timepidium bromide (SA-504)--Unstable metabolities in the rats
Radioisotopes 1977 Apr;26(4):238-44.PMID:578322DOI:10.3769/radioisotopes.26.4_238.
The colored substances excreted in bile or urine have bee investigated after adminstration of a high dose of SQ-504 to rats. A reddish-violet colored substance and a bluish-violet colored substance were dominant. Their chemical structures were not assigned because of their small quantity and instability. It was recognized that the colored substances were metabolites of SA-504 from the studies with 3H and 14C labelled SA-504 and the derivatives of SA-504.