Maropitant
(Synonyms: 马罗皮坦) 目录号 : GC36543
An NK1 receptor antagonist
Cas No.:147116-67-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Maropitant is an neurokinin-1 (NK1) receptor antagonist.1,2 It reduces motion sickness- or doxorubicin-induced emesis in dogs. Formulations containing maropitant have been used as antiemetics in dogs.
1.Benchaoui, H.A., Siedek, E.M., De La Puente-Redondo, V.A., et al.Efficacy of maropitant for preventing vomiting associated with motion sickness in dogsVet Rec.161(13)444-447(2007) 2.Rau, S.E., Barber, L.G., and Burgess, K.E.Efficacy of maropitant in the prevention of delayed vomiting associated with administration of doxorubicin to dogsJ. Vet. Intern. Med.24(6)1452-1457(2021)
| Cas No. | 147116-67-4 | SDF | |
| 别名 | 马罗皮坦 | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(OC)C(CN[C@@H]2[C@H](C(C3=CC=CC=C3)C4=CC=CC=C4)N5CCC2CC5)=C1 | ||
| 分子式 | C32H40N2O | 分子量 | 468.67 |
| 溶解度 | DMSO: 33.33 mg/mL (71.12 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 2.1337 mL | 10.6685 mL | 21.337 mL |
| 5 mM | 0.4267 mL | 2.1337 mL | 4.2674 mL |
| 10 mM | 0.2134 mL | 1.0668 mL | 2.1337 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。
Antinociceptive and analgesic effect of continuous intravenous infusion of Maropitant, lidocaine and ketamine alone or in combination in cats undergoing ovariohysterectomy
Acta Vet Scand 2021 Nov 27;63(1):49.PMID:34838084DOI:10.1186/s13028-021-00615-w.
Background: Multimodal analgesia consists of the combination of analgesic drugs at low doses to act in different places along the path of pain. Studies with continuous infusion of analgesic drugs in cats are not common. This study aimed to evaluate the analgesic effect of Maropitant, lidocaine and ketamine alone or in combination (intravenous bolus + subsequent continuous intravenous infusion) in the management of acute postoperative pain in cats undergoing ovariohysterectomy. Seventy healthy cats undergoing an ovariohysterectomy received a standard anesthetic protocol consisting of acepromazine and morphine, propofol (anesthesia induction), and isoflurane (anesthesia maintenance). The animals were stratified into seven groups (n = 10 in each group): control (CG), Maropitant (MG), lidocaine (LG), ketamine (KG), Maropitant + lidocaine (LMG), Maropitant + ketamine (KMG), and Maropitant + lidocaine + ketamine (LKMG). All drugs were injected first as an intravenous bolus and then by continuous intravenous infusion. During surgery, esophageal temperature, respiratory rate, heart rate, oxygen saturation, expired isoflurane concentration, and partial pressure of carbon dioxide at the end of expiration were evaluated at 7 time points. Postoperative pain was evaluated for 6 h after extubation using the visual analogue scale and the UNESP-Botucatu multidimensional composite pain scale for assessing postoperative pain in cats. Results: Adverse effects related to Maropitant, lidocaine and ketamine infusion were not observed. Pain scores were lower in the MG, KG and LG groups when compared to the CG group using both scales. Although pain scores were also lower in all combination groups than CG, more animals in these groups required rescue analgesia compared to MG. This indicates that the postoperative analgesic effect of all drugs, either alone or in combination, confers analgesia, although the combinations did not promote greater analgesia. Conclusions: Continuous intravenous infusion of Maropitant, lidocaine, and ketamine alone induces postoperative analgesic effect in cats undergoing ovariohysterectomy, but combinations of these drugs did not increase the analgesic effect. No adverse effect was observed with any drug or their combination.
Spotlight on the perioperative use of Maropitant citrate
Vet Med (Auckl) 2017 Aug 24;8:41-51.PMID:30050855DOI:10.2147/VMRR.S126469.
Neurokinin-1 (NK-1) receptors are present in both the central nervous system and peripheral tissues. Substance P (SP) is the major ligand and is involved in multiple processes including pain transmission, vasodilation, modulation of the inflammatory response, as well as the sensory neuronal transmission involved in stress, anxiety, and emesis. The involvement of NK-1 and SP in the vomiting reflex has led to the development of NK-1 antagonists to prevent and treat vomiting in human and veterinary medicine. Maropitant is a potent, selective neurokinin (NK-1) receptor antagonist that blocks the pharmacologic action of SP in the central nervous system. Maropitant is available in both an injectable and tablet formulation and approved for use in dogs and cats for the treatment and prevention of vomiting from a variety of clinical causes and motion sickness. When administered prior to anesthetic premedication, Maropitant prevents or significantly decreases the incidence of opioid-induced vomiting and signs of nausea in dogs and cats. Maropitant has also been shown to improve postoperative return to feeding and food intake in dogs. The minimum alveolar concentration of sevoflurage is decreased in both dogs and cats by Maropitant, indicating a potential role as an adjunct analgesic, especially for visceral pain. This article will review the background information and literature, including clinical recommendations with respect to the perioperative use of Maropitant in canine and feline veterinary patients.
Determination of the embryotoxic effect of Maropitant using an in ovo model
Pol J Vet Sci 2022 Jun;25(2):357-359.PMID:35861987DOI:10.24425/pjvs.2022.141821.
The aim of this research was to determine the embryotoxic and teratogenic effects and lethal dose (LD50) of Maropitant in ovo, using fertile chicken eggs. The study was designed in two stages, CHEST-I and CHEST-II. For CHEST-I, 210 fertile eggs were divided into seven equal groups; control, saline solution and 5 different doses of Maropitant (10, 5, 2.5, 1.25, 0.625 mg/kg) injected groups. For CHEST-II, 150 fertile eggs were divided into five equal groups; control, saline solution and 3 different doses of Maropitant (8, 6, 4 mg/kg)-injected groups. Eggs were opened on day 21 of incubation. Maropitant did not cause teratogenicity at any dose, while higher embryonic death rates were observed at doses above 4 mg/kg. The LD50 dose of Maropitant was determined as 7.24 mg/kg. In conclusion, Maropitant should only be used after full consideration of risks and benefits in pregnancy.
Anti-nausea effects and pharmacokinetics of ondansetron, Maropitant and metoclopramide in a low-dose cisplatin model of nausea and vomiting in the dog: a blinded crossover study
BMC Vet Res 2017 Aug 16;13(1):244.PMID:28814338DOI:10.1186/s12917-017-1156-7.
Background: Nausea is a subjective sensation which is difficult to measure in non-verbal species. The aims of this study were to determine the efficacy of three classes of antiemetic drugs in a novel low dose cisplatin model of nausea and vomiting and measure change in potential nausea biomarkers arginine vasopressin (AVP) and cortisol. A four period cross-over blinded study was conducted in eight healthy beagle dogs of both genders. Dogs were administered 18 mg/m2 cisplatin intravenously, followed 45 min later by a 15 min infusion of either placebo (saline) or antiemetic treatment with ondansetron (0.5 mg/kg; 5-HT3 antagonist), Maropitant (1 mg/kg; NK1 antagonist) or metoclopramide (0.5 mg/kg; D2 antagonist). The number of vomits and nausea associated behaviours, scored on a visual analogue scale, were recorded every 15 min for 8 h following cisplatin administration. Plasma samples were collected to measure AVP, cortisol and antiemetic drug concentrations. Results: The placebo treated group vomited an average number of 7 times (range 2-13). None of the dogs in either the ondansetron or Maropitant treated groups vomited during the observation period. The onset of nausea-like behaviour in the placebo-treated group occurred at t3.5h and peaked at t4.75h with nausea behaviour score of 58.5 ± 4.6 mm. Ondansetron and Maropitant reduced overall the area under the curve of nausea behaviour score by 90% and 25%, respectively. Metoclopramide had no effect on either vomiting or nausea. Cisplatin-induced nausea and vomiting caused concomitant increases in AVP and cortisol. In the placebo-treated group, AVP and cortisol increased from t2.5h, peaked at t5h (11.3 ± 2.9 pmol L-1 and 334.0 ± 46.7 nmol/L, respectively) and returned to baseline by t8h. AVP and cortisol increases were completely prevented by ondansetron and only partially by Maropitant, while metoclopramide had no effect. The terminal half-lives (harmonic mean ± pseudo SD) for ondansetron, Maropitant and metoclopramide were 1.21 ± 0.51, 5.62 ± 0.77 and 0.87 ± 0.17 h respectively. Conclusions: 5-HT3 receptor antagonist ondansetron demonstrates the greatest anti-emetic and anti-nausea efficacy of the three drugs. AVP and cortisol appear to be selective biomarkers of nausea rather than emesis, providing a means of objectively measuring of nausea in the dog.
Pharmacokinetics of Maropitant citrate in Rhode Island Red chickens (Gallus gallus domesticus) following subcutaneous administration
J Vet Pharmacol Ther 2022 Sep;45(5):495-500.PMID:35734891DOI:10.1111/jvp.13082.
Maropitant citrate is a synthetic neurokinin-1 receptor antagonist and substance P inhibitor used for control of emesis in dogs in cats. Maropitant citrate is used empirically in birds, despite a lack of pharmacokinetic data in avian species. The objective of this study was to determine the pharmacokinetic profile of a single dose of Maropitant citrate 1 and 2 mg/kg subcutaneously (SC) in eight Rhode Island Red hens (Gallus gallus domesticus). A crossover study design was used with 1-week washout between trials. Blood samples were collected over 36 h after drug administration. Plasma concentrations were measured using liquid chromatography-tandem mass spectrometry and pharmacokinetic parameters were determined via non-compartmental analysis. The mean maximum plasma concentration, time to maximum concentration, and elimination half-life following 1 and 2 mg/kg SC were 915.6 ± 312.8 ng/ml and 1195.2 ± 320.2 ng/ml, 0.49 ± 0.21 h and 1.6 ± 2.6 h, and 8.47 ± 2.24 h and 8.58 ± 2.6 h, respectively. Pharmacokinetic data suggests doses of 1 or 2 mg/kg SC may be administered every 12-24 h to maintain above target plasma concentration similar to dogs (90 ng/ml). These data provide a basis for further investigation of Maropitant citrate pharmacokinetics and pharmacodynamics in birds.