Morantel tartrate
(Synonyms: 酒石酸甲噻嘧啶) 目录号 : GC32285
A positive allosteric modulator of nAChRs
Cas No.:26155-31-7
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
Morantel is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs).1 It enhances channel gating of the α3β2 nAChR subtype by binding to non-canonical sites.2 Formulations containing morantel are used to treat nematode infections in livestock.3
1.Wu, T.Y., Smith, C.M., Sine, S.M., et al.Morantel allosterically enhances channel gating of neuronal nicotinic acetylcholine alpha 3 beta 2 receptorsMol. Pharmacol.74(2)466-475(2008) 2.Seo, S., Henry, J.T., Lewis, A.H., et al.The positive allosteric modulator morantel binds at noncanonical subunit interfaces of neuronal nicotinic acetylcholine receptorsJ. Neurosci.29(27)8734-8742(2009) 3.McKellar, Q.A., Scott, E.W., Baxter, P., et al.Pharmacodynamics, pharmacokinetics and faecal persistence of morantel in cattle and goatsJ. Vet. Pharmacol. Ther.16(1)87-92(1993)
| Cas No. | 26155-31-7 | SDF | |
| 别名 | 酒石酸甲噻嘧啶 | ||
| Canonical SMILES | CC1=C(/C=C/C2=NCCCN2C)SC=C1.O=C(O)[C@H](O)[C@@H](O)C(O)=O | ||
| 分子式 | C16H22N2O6S | 分子量 | 370.42 |
| 溶解度 | DMSO: 125 mg/mL (337.45 mM) | 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 | 2.6996 mL | 13.4982 mL | 26.9964 mL |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL |
| 10 mM | 0.27 mL | 1.3498 mL | 2.6996 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。
Morantel tartrate release from a long-acting intraruminal device in cattle: pharmacokinetics and gastrointestinal distribution
J Vet Pharmacol Ther 1992 Jun;15(2):117-23.PMID:1433473DOI:10.1111/j.1365-2885.1992.tb00998.x.
The pharmacokinetics and gastrointestinal distribution of Morantel tartrate release from a sustained release trilaminate bolus in cattle were investigated over a 98-day period post-treatment. Six Holstein calves (125-150 kg) had permanent indwelling fistulae surgically inserted into the rumen, abomasum and terminal ileum. Samples of jugular blood, feces and ruminal, abomasal and ileal fluids were taken on days -3, 1, 4, 7, 10, 14 and weekly up to 98 days post-bolus administration. Morantel tartrate concentrations were measured by HPLC after extraction and clean-up. Morantel was not detected in plasma at any time after bolus administration. High concentrations of Morantel tartrate were found in ruminal, abomasal and ileal fluids and feces over 98 days post-treatment. The morantel peak concentration (Cmax) was achieved at Day 1 post-administration in each of these compartments. The steady-state morantel concentration (Css) was achieved at approximately 10 days post-treatment and maintained for 91-98 days post-treatment in these gastrointestinal compartments. The morantel Cmax, Css, area under the zero (AUC) and first moment (AUMC) of the concentration-time curve were significantly higher (P less than 0.01) in feces than in other compartments. The in vivo drug release profile of this device has been determined. Steady-state concentrations for from 91 to 98 days have been confirmed.
Determination of depletion and statistical distribution of morantel-related residues in bovine milk following administration of Morantel tartrate to dairy cows
J Assoc Off Anal Chem 1986 Nov-Dec;69(6):935-8.PMID:3804945doi
Residue depletion studies were conducted in dairy cattle to monitor morantel-related residues in milk following oral administration of Morantel tartrate (Rumate. Eleven lactating cows of various ages, periods of lactation, and known milk production were orally dosed with the bolus formulation of Morantel tartrate with an actual dose range of 8.4-9.8 mg/kg body weight. Representative samples of milk were collected at 10-14 h intervals post-dose, and subsamples were assayed for the major and minor hydrolysis products of morantel-related residues, MAPA and CP-20,107. Residues assayed as precursors of MAPA peaked at the second milking (24 h post-dose) and were below 25 ppb (range: less than 12-24 ppb). Precursors of CP-20,107, which confirm the identity of morantel, also peaked at 24 h post-dose (range: 2.1-3.3 ppb) and declined rapidly thereafter. A statistical model was used to project the level of residues at the upper limit of 99% of the total target animal (i.e., dairy cattle) population with 95% confidence. The calculated peak levels from this model were 50 and 5.0 ppb for morantel-related residues convertible to MAPA and CP-20,107, respectively.
Effect of the morantel sustained-release bolus, used during one grazing season, on the sensitivity of Ostertagia and Cooperia to Morantel tartrate in calves
Am J Vet Res 1985 Feb;46(2):424-5.PMID:3994107doi
Infective 3rd-stage larvae of Ostertagia and Cooperia, obtained from the feces of nonmedicated and morantel sustained-release bolus (MSRB)-treated calves, were orally administered to 2 groups of parasite-free calves. After a 42-day maturation period, a therapeutic dose of Morantel tartrate was administered to half of the calves from each group. All calves were necropsied 7 days after treatment. After comparing the nematode counts for the nonmedicated and morantel-treated calves of each group, Morantel tartrate was demonstrated to be equally effective against the nonmedicated-derived and MSRB-derived nematode populations. The sensitivity of Ostertagia spp and Cooperia spp to Morantel tartrate, therefore, was not diminished after use of the MSRB for a single grazing season.
Pharmacodynamics, pharmacokinetics and faecal persistence of morantel in cattle and goats
J Vet Pharmacol Ther 1993 Mar;16(1):87-92.PMID:8479005DOI:10.1111/j.1365-2885.1993.tb00293.x.
Morantel could not be detected (< 0.05 microgram/ml) in the plasma of cattle or goats following the oral administration of Morantel tartrate at a dose rate of 10 mg/kg bodyweight. No morantel was detected in the milk of lactating goats except in one animal where a concentration of 0.092 microgram/ml was detected at 8 h after drug administration. Morantel was highly effective against Cooperia oncophora infections in calves treated 6, 9 or 18 days after infection; however, was highly effective against Ostertagia ostertagi only when treated 18 days after infection. Morantel did not affect the fecundity of adult O. ostertagi surviving treatment 18 days after infection which had similar average numbers of eggs in their uteri (range 13.4 +/- 0.73-16.8 +/- 0.98) as did parasites from control animals (range 12.0 +/- 0.70-13.6 +/- 0.66). Morantel could be detected at a concentration of 96 +/- 4.5 micrograms/g (dry weight) in the faeces of a calf 24 h after treatment with 10 mg/kg bodyweight of Morantel tartrate. The concentration of morantel in replicate samples of this faeces exposed to natural atmosphere, but not to soil or soil organisms, declined slowly over the following 322 days. At day 322 after the start of the experiment 8.8 micrograms/g of morantel could be measured in the remaining faecal material. Throughout the faecal degradation study the concentration of morantel in the crusts of the replicate sample pats was lower than the concentration in the core samples.
Further studies with a strain of Ostertagia ostertagi resistant to Morantel tartrate
Int J Parasitol 1991 Nov;21(7):867-70.PMID:1774123DOI:10.1016/0020-7519(91)90157-3.
Two experiments with a morantel resistant strain of Ostertagia ostertagi were carried out. In the first experiment five groups of five calves were infected with 60,000 larvae of this resistant strain. Calves of one group remained untreated, calves of the other groups were treated with Morantel tartrate, oxfendazole, levamisole or ivermectin in the recommended doses. It was demonstrated that there was side resistance to levamisole, but not to oxfendazole or ivermectin. Compared with the untreated controls the reduction percentages of the worm burdens were 45.3 (Morantel tartrate), 99.7 (oxfendazole), 83.5 (levamisole) and 100 (ivermectin). In the second experiment a comparison was made between the effect of levamisole against a morantel susceptible strain of O. ostertagi and the resistant strain. Two groups of five calves were infected with the susceptible strain and two groups with the resistant one. One group of each pair remained untreated, the other was treated with levamisole. The reduction percentages of the worm burdens were 99.6 (susceptible strain) and 63.6 (resistant strain). This result confirms the efficacy of levamisole to susceptible O. ostertagi and the side resistance of the morantel resistant strain.