Chemistry:Mafoprazine
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| Trade names | Mafropan |
| AHFS/Drugs.com | Monograph |
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| Formula | C22H28FN3O3 |
| Molar mass | 401.482 g·mol−1 |
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Mafoprazine is an antipsychotic of the phenylpiperazine class which is used in veterinary medicine.[1] Intramuscular injections of mafoprazine mesylate are used for the sedation of pigs either on its own,[2] or in combination with sodium pentobarbital[3] or thiopental.[4]
Pharmacology
| Site | Ki (nM) | Species | Ref |
|---|---|---|---|
| D2 | 10.7 | Rat | [5][6] |
| α1 | 12.7 | Rat | [5][6] |
| α2 | 101.0 | Rat | [5][6] |
It demonstrates activity as a D2 dopamine receptor antagonist, an α1 adrenergic receptor antagonist, and an α2 adrenergic receptor agonist.[5]
The affinity of mafoprazine for D2 dopamine receptors is 6 and 16 times lower than that of chlorpromazine and haloperidol, respectively, but 2 times higher than that of azaperone.[5]
The Ki for various receptors was determined using rat neuronal receptor binding assays.[citation needed]
History
Mafoprazine was first synthesized in 1988.[5] It is sold as Mafropan® by DS Pharma Animal Health Co. Ltd., Osaka, Japan.
References
- ↑ "Mafoprazine | Chemical Substance Information | J-GLOBAL" (in en). https://jglobal.jst.go.jp/en/detail?JGLOBAL_ID=200907023639364356#%7B%22category%22%3A%227%22%2C%22fields%22%3A%5B%7B%22op%22%3A%22AND%22%2C%22nm%22%3A%22SNID%22%2C%22vals%22%3A%5B%7B%22v%22%3A%22J138.354J%22%2C%22m%22%3A1%7D%5D%7D%5D%7D.
- ↑ Heishima, Kazuki; Kuo, Kendon; Kimura, Masashi; Mori, Takashi (2019). Animal Lymphocyte Metaphase Chromosome Preparation. Methods in Molecular Biology. 1984. 7–22. doi:10.1007/978-1-4939-9432-8_2. ISBN 978-1-4939-9430-4.
- ↑ Azizi, AFN; Miyazaki, R; Yumito, T; Ohashi, Y; Uno, S; Miyajima, U; Kumamoto, M; Uchiyama, S et al. (1 January 2018). "Effect of maternal supplementation with seaweed powder on immune status of liver and lymphoid organs of piglets.". The Journal of Veterinary Medical Science 80 (1): 8–12. doi:10.1292/jvms.17-0537. PMID 29142150.
- ↑ Umeyama, Kazuhiro; Watanabe, Kota; Watanabe, Masahito; Horiuchi, Keisuke; Nakano, Kazuaki; Kitashiro, Masateru; Matsunari, Hitomi; Kimura, Tokuhiro et al. (14 April 2016). "Generation of heterozygous fibrillin-1 mutant cloned pigs from genome-edited foetal fibroblasts". Scientific Reports 6 (1): 24413. doi:10.1038/srep24413. PMID 27074716. Bibcode: 2016NatSR...624413U.
- ↑ 5.0 5.1 5.2 5.3 5.4 5.5 Fukuchi, Isao; Kawashima, Kazutaka; Matsuoka, Yuzo; Ishida, Ryuichi (1988). "Neurochemical study of mafoprazine, a new phenylpiperazine derivative.". The Japanese Journal of Pharmacology 47 (1): 51–61. doi:10.1254/jjp.47.51. PMID 3411821.
- ↑ 6.0 6.1 6.2 "NCATS Inxight Drugs — MAFOPRAZINE" (in en). https://drugs.ncats.io/drug/D7UUO54C6N.
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