Scopolamine hydrobromide trihydrate
(Synonyms: 东莨菪碱氢溴酸盐三水合物; Hyoscine hydrobromide trihydrate) 目录号 : GC63182
An Analytical Reference Standard
Cas No.:6533-68-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
Scopolamine is a tropane alkaloid that can be found in many plants of the Solanaceae (nightshade) family.1 It is a muscarinic receptor antagonist that can be used to induce memory impairment in animals.2,3,4 Scopolamine prevents motion sickness, nausea, and vomiting in animals.3,5
1.Ziegler, J., and Facchini, P.J.Alkaloid biosynthesis: Metabolism and traffickingAnnu. Rev. Plant Biol.59735-769(2008) 2.Woods, S., Clarke, N.N., Layfield, R., et al.5-HT(6) receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanismsBr. J. Pharmacol.167436-449(2012) 3.Soto, E., and Vega, R.Neuropharmacology of vestibular system disordersCurr. Neuropharmacol.8(1)26-40(2010) 4.Shannon, H.E., Hart, J.C., Bymaster, F.P., et al.Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in ratsJ. Pharmacol. Exp. Ther.290(2)901-907(1999) 5.Grynkiewicz, G., and Gadzikowska, M.Tropane alkaloids as medicinally useful natural products and their synthetic derivatives as new drugsPharmacol. Rep.60(4)439-463(2008)
| Cas No. | 6533-68-2 | SDF | |
| 别名 | 东莨菪碱氢溴酸盐三水合物; Hyoscine hydrobromide trihydrate | ||
| 分子式 | C17H28BrNO7 | 分子量 | 438.31 |
| 溶解度 | DMSO : 88mg/mL; Water : 88mg/mL | 储存条件 | Store at 4°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 | 2.2815 mL | 11.4075 mL | 22.8149 mL |
| 5 mM | 0.4563 mL | 2.2815 mL | 4.563 mL |
| 10 mM | 0.2281 mL | 1.1407 mL | 2.2815 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。
NTP Toxicology and Carcinogenesis Studies of Scopolamine hydrobromide trihydrate (CAS No. 6533-68-2) in F344 Rats and B6C3F1 Mice (Gavage Studies)
Natl Toxicol Program Tech Rep Ser 1997 Mar;445:1-277.PMID:12594530doi
Scopolamine hydrobromide trihydrate is used in ophthalmic preparations and as a preanesthetic sedative. Its major use is in transdermal patches for the treatment of motion sickness. Scopolamine hydrobromide trihydrate was selected for study because of considerable human exposure resulting from its use in prescription and over-the-counter preparations. Scopolamine was a suspect carcinogen because it contains an aliphatic epoxide moiety which may act as a biological alkylating agent. Male and female F344/N rats and B6C3F1 mice received Scopolamine hydrobromide trihydrate (89% pure) in distilled water by gavage for 16 days, 14 weeks, or 2 years. Genetic toxicology studies were conducted in Salmonella typhimurium, cultured Chinese hamster ovary cells, and mouse peripheral blood erythrocytes. 16-DAY STUDY IN RATS: Groups of five male and five female rats were administered 0, 75, 150, 300, 600, or 1,200 mg Scopolamine hydrobromide trihydrate/kg body weight in distilled water by gavage for 16 days. All rats survived to the end of the study. The final mean body weights and body weight gains of males receiving 600 and 1,200 mg/kg and the mean body weight gain of males receiving 300 mg/kg were significantly lower than those of the control group. Clinical findings included bilateral pupillary dilation in all dosed animals and red eyelids in males and females receiving 1,200 mg/kg. There were no significant treatment-related gross or microscopic lesions. 16-DAY STUDY IN MICE: Groups of five male and five female mice were administered 0, 150, 250, 450, 900, or 1,800 mg Scopolamine hydrobromide trihydrate/kg body weight in distilled water by gavage for 16 days. One male and two females receiving 1,800 mg/kg and one female receiving 150 mg/kg died during the study. The final mean body weights and body weight gains of dosed mice were similar to those of the control groups. Clinical findings related to Scopolamine hydrobromide trihydrate administration included bilateral pupillary dilation and squinting in all dosed males and females. The relative liver weights of males receiving 1,800 mg/kg and of females in all dosed groups were significantly greater than those of the control groups. There were no significant treatment-related gross or microscopic lesions. 14-WEEK STUDY IN RATS: Groups of 10 male and 10 female rats were administered 0, 15, 45, 135, 400, or 1,200 mg Scopolamine hydrobromide trihydrate/kg body weight in distilled water by gavage for 14 weeks. One female receiving 45 mg/kg, one male and one female receiving 135 mg/kg, six males and one female receiving 400 mg/kg, and eight males and seven females receiving 1,200 mg/kg died during the study. The final mean body weights and mean body weight gains of all dosed males and females were significantly lower than those of the control groups. Clinical findings included bilateral pupillary dilation in all dosed males and females and reddening of the eyes in 15 mg/kg males and 135, 400, and 1,200 mg/kg males and females. Hematocrit, hemoglobin concentration, and/or erythrocyte count in male and female rats receiving 45 mg/kg or greater were slightly higher than those of the control groups. In general, these changes were most prominent in rats in the 400 and 1,200 mg/kg groups. Higher hematocrit, hemoglobin concentration, and erythrocyte count were likely due to hemoconcentration from dehydration (relative erythrocytosis). A minimal to mild mature neutrophilia, evidenced by higher segmented neutrophil numbers than in the control group, occurred in all dosed male rats. Sperm morphology and vaginal cytology parameters in dosed rats were similar to those in the control groups. Nine male and five female dosed rats died from esophageal obstructions consisting of feed and bedding material in the posterior pharynx. Tracheal obstruction occurred concurrently with esophageal obstruction as a result of food build-up in the oropharyngeal region. This condition is considered to be secondary to the inhibitory effects of Scopolamine hydrobromide trihydrate on salivary gland secretions and on esopon esophageal smooth muscle involved in swallowing. There were no other significant treatment-related gross or microscopic findings. 14-WEEK STUDY IN MICE: Groups of 10 male and 10 female mice were administered 0, 15, 45, 135, 400, or 1,200 mg Scopolamine hydrobromide trihydrate/kg body weight in distilled water by gavage for 14 weeks. One male receiving 135 mg/kg and two males and one female receiving 1,200 mg/kg died during the study. The final mean body weights and mean body weight gains of all dosed male groups and females receiving 45 mg/kg and above were significantly lower than those of the control groups. Clinical observations included bilateral pupillary dilation, hyperactivity, and hypoactivity. A minimal to mild mature neutrophilia, similar to that which occurred in the 14-week rat study, occurred in male mice receiving 45 mg/kg or greater. As in the rat study, there was no microscopic evidence of inflammation that could account for the neutrophilia. The estrous cycle length of 1,200 mg/kg females was significantly greater than that in the control group. There were no significant treatment-related gross or microscopic lesions. 2-YEAR STUDY IN RATS: Groups of 60 male and 60 female rats were administered 0, 1, 5, or 25 mg Scopolamine hydrobromide trihydrate/kg body weight in distilled water by gavage for 104 weeks. Ten males and ten females from each dose group, excluding the 1 mg/kg female group, were evaluated at 15 months. Survival, Body Weights, Clinical Findings, and Ophthalmic Examination Findings: The survival rates of female rats receiving 1 and 25 mg/kg were significantly lower than that of the control group. Mean body weights of 1 and 5 mg/kg males and females were similar to those of the controls throughout the study. However, mean body weights of 25 mg/kg males and females were generally lower than those of the control groups after about week 25. Clinical findings included bilateral pupillary dilation in all dosed males and females. Ophthalmic examination revealed no significant findings. Hematology: Compared to controls, hematocrit was slightly higher in the 25 mg/kg male rats, similar to the effects observed in the 14-week study; this is consistent with dehydration resulting in hemoconcentration. Reticulocyte numbers in the 25 mg/kg female rats were slightly lower than those in the controls. This result is consistent with the lower body weights, and thus a decreased nutritional status, exhibited by these animals. Plasma Scopolamine Determinations: The serum scopolamine concentrations were 6 ng scopolamine/mL serum for the 5 mg/kg female sample and 12 and 28 ng/mL for the 25 mg/kg male and female samples, respectively. The amounts of scopolamine in the other serum samples were below the minimum detection limit (4 ng/mL) of the analysis method. Neurobehavioral Findings: Horizontal motor activity of 25 mg/kg females was significantly greater than that of the control group on days 90, 180, and 360. Startle response of 5 and 25 mg/kg females was significantly lower than that of the control group on day 90. On day 180, passive avoidance of 25 mg/kg males was significantly lower than that of the control group. Pathology Findings: The incidences of adenoma of the pituitary gland pars distalis decreased with increasing dose in both male and female rats; however, this trend was only significant in males (males: vehicle control, 19/49; 1 mg/kg, 17/49; 5 mg/kg, 13/50; 25 mg/kg, 10/50; females: 20/50, 13/60, 14/50, 10/50). The incidences of adenoma of the pituitary gland pars distalis in 25 mg/kg males and all groups of dosed females were below the NTP historical control range. The incidences of hyperplasia were not significantly different from those in the control groups. The incidences of mononuclear cell leukemia in 25 mg/kg males and females were significantly lower than those of the control groups (males: 33/50, 21/50, 26/50, 24/50; females: 20/50, 6/60, 13/50, 4/50). The incidence of mononuclear cell leukemia in females receiving 25 mg/kg was well below the NTP historical range. 2-YEAR STUDY IN MICE: Groups of 70 male and 70 female mice were administered 0, 1, 5, or 25 mg Scopolamine hydrobromide trihydrate/kg body weight in distilled water by gavage for 104 to 105 weeks. Ten control animals and ten animals from each dose level were evaluated at 15 months. Survival, Body Weights, Clinical Findings, and Ophthalmic Examination Findings Survival of dosed males and females was similar to that of the controls. The mean body weights of males and females receiving 1 mg/kg were similar to those of the control groups throughout the majority of the study. The mean body weights of 5 mg/kg males and females were slightly lower than those of the controls. The mean body weights of males and females receiving 25 mg/kg were lower than those of the control groups after week 13. Clinical findings included bilateral pupillary dilation in all dosed male and female groups. Ophthalmic examination revealed no significant findings. Hematology: Hematocrit, hemoglobin concentration, and erythrocyte count in 25 mg/kg female mice were slightly lower than those in the control group. These results are consistent with development of a minimal normocytic, normochromic nonresponsive anemia. The anemia may be related to the lower body weights exhibited by these animals and are presumed to be due to a decreased nutritional status. Pathology Findings: The combined incidences of hepatocellular neoplasms (adenoma or carcinoma) occurred with a significant negative trend in males and females (males: vehicle control, 30/50; 1 mg/kg, 33/50; 5 mg/kg, 14/50; 25 mg/kg, 15/50; females: 22/51, 21/50, 16/50, 9/51). The combined incidences of hepatocellular neoplasms in 5 and 25 mg/kg males were within the NTP historical control range. The incidences of clear cell foci and eosinophilic foci in dosed male groups, and eosinophilic foci in 25 mg/kg females, were significantly lower than those of the control groups. The incidences of many spontaneously occurring nonneoplastic lesions were significantly lower in dosed mice than in the control groups and usually decreased with increasing dose. These included kidney nephropathy, alveolar epithelial hyperplasia, hyperplasia of the pancreatic islets, bone marrow myelofibrosis, hyperplasia of the pituitary gland pars distalis, cystic hyperplasia of the uterus, and hematopoietic cell proliferation of the spleen. The decreased incidences of these spontaneous lesions were most likely a result of lower body weights in dosed animals. GENETIC TOXICOLOGY: Scopolamine hydrobromide trihydrate did not induce mutations in any of five strains of Salmonella typhi murium, with or without S9 metabolic activation enzymes, nor did it induce sister chromatid exchanges in cultured Chinese hamster ovary cells, with or without S9. A weakly positive response was obtained, however, in a chromosomal aberrations test conducted in cultured Chinese hamster ovary cells with very high doses of Scopolamine hydrobromide trihydrate in the presence of S9; without S9, no increase in aberrations was noted. Despite the evidence for chromosomal damage observed in vitro, no increase in the frequencies of micronucleated normochromatic erythrocytes was observed in peripheral blood samples of male or female mice exposed to Scopolamine hydrobromide trihydrate for 14 weeks by gavage. CONCLUSIONS: Under the conditions of these 2-year gavage studies, there was no evidence of carcinogenic activity of Scopolamine hydrobromide trihydrate in male or female F344/N rats or B6C3F1 mice administered 1, 5, or 25 mg/kg. Synonyms: Scopolamine hydrobromide, 6,7-epoxytropan-3-yl, euscopol, hydroscine hydrobromide, hyoscine bromide, (-)-hyoscine hydrobromide, hysco, isoscopil, scopolammonium bromide, (s)-tropate hydrobromide trihydrate, lα-tropyl-a-scopine
Neuroprotective role of medicinal plant extracts evaluated in a scopolamine-induced rat model of Alzheimer's disease
Biomarkers 2022 Dec;27(8):773-783.PMID:35950787DOI:10.1080/1354750X.2022.2112975.
Background:Alzheimer's disease is a debilitating neurological brain disease with memory impairment among the first signs. Scopolamine (SCO), a muscarinic receptor antagonist that disrupts cognition and memory acquisition, is considered a psychopharmacological AD model. We investigate the effectiveness of medicinal plants in mitigating the SCO-induced neurobehavioural damage in rats. Materials and Methods: Animals were injected with Scopolamine hydrobromide trihydrate (2.2 mg/kg IP.) daily for 2 months. Each treatment group was administered one of four medicinal spice extracts (Nigella sativa, 400 mg/kg; rosemary, 200 mg/kg; sage, 600 mg/kg and ginseng; 200 mg/kg 90 minutes after SCO injection. Animals were subjected to cognitive-behavioural tests (NOR, Y-maze and MWM). After the experiment, we extracted the brains for histopathological examination and biochemical assessment for oxidative stress (levels of TT, CAT and TBARS) and gene expression of acetylcholinesterase and brain monoamines. Results: As expected, SCO treatment impaired memory and cognition, increased oxidative stress, decreased neurotransmitters and caused severe neurodegenerative changes in the brain. Conclusion: Surprisingly, these effects were measurably moderated by the administration of all four plant extracts, indicating a neuroprotective action that we suggest could alleviate AD disease manifestations.
Effect of Dietary Restriction on Toxicology and Carcinogenesis Studies in F344/N Rats and B6C3F1 Mice
Natl Toxicol Program Tech Rep Ser 1997 Sep;460:1-414.PMID:12587016doi
Studies were conducted to compare outcomes when four chemicals were evaluated under typical NTP bioassay conditions as well as under protocols employing dietary restriction. Specific experiments were designed to evaluate the effect of diet restriction on the sensitivity of the bioassay toward chemical-induced chronic toxicity and carcinogenicity and to evaluate the effect of weight-matched control groups on the sensitivity of the bioassays. Two chemicals, butyl benzyl phthalate and t-butylhydroquinone, were administered in feed; one chemical, salicylazosulfapyridine, was administered in corn oil by gavage; and one chemical, Scopolamine hydrobromide trihydrate, was administered in distilled water by gavage. In each of four protocols, the effects of the chemical were assessed by a comparison between a group exposed to a single dose concentration of the study chemical and a nonexposed control group. F344/N rats and B6C3F1 mice were fed NIH-07 diet either ad libitum or in amounts that restricted mean body weights according to the following design requirements. For the core bioassay, groups of 50 to 60 ad libitum-fed animals were allotted to a control group and three dosed groups for approximately 104 weeks or up to 128 weeks (t-butylhydroquinone study). The comparison between the control group and the group receiving the highest dose was used to represent the outcome of the bioassay under ad libitum feeding protocols. In a second comparison, outcomes from the group receiving the highest dose were compared with a weight-matched group of 50 to 60 untreated controls; the weight-matched controls received feed in amounts restricted so that the mean body weight matched the mean body weight of the dosed group. Two additional groups of 48 to 60 animals (one control and one dosed group) were offered feed in amounts that limited the mean body weight of the control group to approximately 85% that of the controls fed ad libitum under the first protocol. Animals assigned to this dietary restriction paradigm were evaluated after 104 weeks or 130 weeks (t-butylhydroquinone). A fourth protocol was em- loyed to evaluate whether an additional period of exposure (up to 1 year) would influence the neoplasm profile of animals fed a restricted diet. Two groups of approximately 50 animals (one control and one dosed group) in the butyl benzyl phthalate, salicylazosulfapyridine, and Scopolamine hydrobromide trihydrate studies received restricted diets, as under the third protocol, for 3 years or until survival in either group was reduced to 20%. Butyl benzyl phthalate caused an increased incidence of pancreatic acinar cell neoplasms in ad libitum-fed male rats relative to ad libitum-fed and weight-m atched controls. This change did not occur in rats in the restricted feed protocol after 2 years; however, acinar cell adenomas were observed in three exposed, feed-restricted males at 30 months. Feed restriction is known to influence the incidence of pancreatic acinar cell neoplasms and may have prevented the full expression of this chemical-induced effect. Butyl benzyl phthalate also caused an increased incidence of urinary bladder neoplasms in female rats in the 32-month restricted feed protocol. The incidences of urinary bladder neoplasms were not significantly increased in female rats in any of the 2-year protocols, suggesting that the length of study, and not body weight, was the primary factor in the detection of this carcinogenic response. Salicylazosulfapyridine caused an increased incidence of urinary bladder papillomas in male rats fed ad libitum relative to ad libitum-fed and weight- matched controls. This increase was associated with an increased incidence of urinary bladder calculi; the incidences of urinary bladder concretions, dilatation, and hyperplasia were also increased in dosed males. The incidences of urinary bladder papillomas and calculi were not increased in male rats receiving salicylazosulfapyridine that were fed restricted diets. In male mice, salicylazosulfapyridine caused an increased incidence of liver neoplasms relative tsms relative to the ad libitum-fed and weight-matched controls. This increase did not occur in the restricted feed protocols. Liver neoplasms in mice are greatly influenced by body weight, and the marked mean body weight reduction observed in dosed male mice in the restricted feed protocols may have overridden the carcinogenic response. Neither t-butylhydroquinone nor scopolamine hydro bromide trihydrate caused increased neoplasm incidences under any of the experimental protocols. Results consistently show that feed restriction caused decreased incidences of neoplasms and nonneoplastic lesions at a variety of anatomic sites in control and dosed animals. Furthermore, the sensitivity of the bioassay to detect a carcinogenic response was altered by dietary restriction: two of the four chemicals caused increased incidences of neoplasms at three sites when evaluated under a standard ad libitum feeding protocol for 104 weeks. When control and dosed groups were subjected to dietary restriction, none of these three sites was detected as a target of carcinogenesis after 2 to 3 years. Rather, one different site of carcinogenesis was detected after 32 months. When dosed animals in the ad libitum feeding protocol were compared to weight-matched control groups, three sites were identified as targets of carcinogenesis and corresponded to the three sites discovered under the ad libitum feeding protocol. The magnitude of the response was greater when the weight-matched controls protocol was used. Dietary restriction of dosed and control animals decreased the sensitivity of these carcinogenesis bioassays. Regarding the future use of dietary restriction regimens in long-term studies, only limited conclusions can be drawn because only four chemicals were evaluated and none of these proved to be a strong carcinogen. However, the results of these studies are consistent with previous findings that dietary restriction increases survival rates and decreases the incidences of neoplasms and nonneoplastic lesions at a variety of sites in rats and mice. This association between reduced body weights and decreased neoplasm incidences underlines the necessity that the doses selected for chronic studies not exceed "minimally toxic doses" so that no marked body weight reductions (or increases) will occur in the dosed groups. Such body weight changes complicate the detection of carcinogenic effects. The following tables summarize and compare the findings from ad libitum-fed, weight-matched, and feed-restricted groups for each chemical. Tabular Summary of Dietary Restriction Study of Butyl Benzyl Phthalate is available in web version of this document. TabularSummary of the Dietary Restriction Study of t-Butylhydroquinone is available in web version of this document. TabularSummary of the Dietary Restriction Studies of Salicylazosulfapyridine is available in web version of this document. TabularSummary of the Dietary Restriction Study of Scopolamine hydrobromide trihydrate is available in web version of this document.