马罗匹坦(PVB)
Maropitant Citrate
CAS: 147116-67-4
Molecular Formula: C32H40N2O
马罗匹坦(PVB) - Names and Identifiers
马罗匹坦(PVB) - Physico-chemical Properties
| Molecular Formula | C32H40N2O |
| Molar Mass | 468.67 |
| Density | 1.11±0.1 g/cm3(Predicted) |
| Boling Point | 572.6±50.0 °C(Predicted) |
| Vapor Presure | 0-0Pa at 20-25℃ |
| Appearance | Solid:particulate/powder |
| pKa | 9.99±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vivo study | Treatment with 1 mg/kg Maropitant citrate, significantly reduces the size of ulcerative dermatitis (UD) lesions in mice. Intravenous Maropitant decreases MAC by 16%. In contrast, epidural administration of either saline or Maropitant does not change the MAC (2.17% and 1.92 %, respectively). |
马罗匹坦(PVB) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.134 ml | 10.668 ml | 21.337 ml |
| 5 mM | 0.427 ml | 2.134 ml | 4.267 ml |
| 10 mM | 0.213 ml | 1.067 ml | 2.134 ml |
| 5 mM | 0.043 ml | 0.213 ml | 0.427 ml |
Last Update：2024-01-02 23:10:35
马罗匹坦(PVB) - Reference Information
| LogP | 3.1-7.2 at pH2-7.5 |
| Overview | malopitant citrate is also known as CJ-11,972, and its trade name is Cerenia (anti-hypertension), originally developed by Pfizer. Maropitant citrate has a molecular weight of 678.82 and the chemical name is (2S,3S)-2-benzyl-n-(5-tert-butyl-2-methoxybenzyl)-3-amino-quinine citrate monohydrate. The synthetic method of marlopitant is reported in the literature. The synthetic route of this method requires 8 steps of reaction to achieve the preparation of marlopitant free base, it involves the Michael addition reaction, multi-step pressure hydrogenation reaction and the like in which the phenylmagnesium bromide format reagent and cuprous bromide dimethyl sulfide (CuBr •(CH)S) are difficult to control. The above method for synthesizing marlopitant free base not only has long route and low yield (the total yield of 8-step reaction is only about 10%), but also involves the use of many kinds of precious metals, such as Ti, pt, Pd, etc., are not only costly, but also require a large amount of solvent and adsorbent to remove these precious metal residues. For this reason, the development of a new method for the synthesis of malopitant is particularly important for the industrial production of the drug. |
| Application | maropitantcittrate citrate is a type 1 neurokinin (NK1) receptor anticoagulant, it can act on the central nervous system by inhibiting substance P, which causes Vomit of key neurotransmitters. Malopitant citrate is an alternative quinine drug, due to significant efficacy, Vomit FDA approved the drug for the prevention and treatment of dogs with acute, it was also subsequently approved for off-prescription use in cats. There are two dosage forms of malopitant citrate. Malopitant citrate for injection is used to prevent and treat acute Vomit in dogs; malopitant citrate tablets are used for the prevention of acute and Vomit due to motion sickness in dogs; Both can be used as an off-prescription medication in cats. China's Ministry of Agriculture approved the import registration of malopitant citrate in May 2016, which is also used for the prevention and treatment of acute Vomit in dogs. |
| biological activity | maropite is a selective orally active neurokinin (NK1) receptor antagonist. Maropite works by preventing the binding of the emetic center to substance P in the chemoreceptor trigger zone (CRTZ). Maropite is very effective in the prevention of Vomit. |
Last Update：2024-04-09 15:16:51
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