Mafoprazine Explained
| Tradename: | Mafropan |
| Cas Number: | 80428-29-1 |
| Pubchem: | 71241 |
| Chemspiderid: | 64374 |
| Unii: | D7UUO54C6N |
| Kegg: | C18361 |
| Chembl: | 2105101 |
| Drug Name: | Mafoprazine |
| Iupac Name: | N-[4-[3-[4-(2-fluorophenyl)piperazin-1-yl]propoxy]-3-methoxyphenyl]acetamide |
| C: | 22 |
| H: | 28 |
| F: | 1 |
| N: | 3 |
| O: | 3 |
| Smiles: | COC1=C(OCCCN2CCN(CC2)C3=C(F)C=CC=C3)C=CC(NC(C)=O)=C1 |
| Stdinchi: | 1S/C22H28FN3O3/c1-17(27)24-18-8-9-21(22(16-18)28-2)29-15-5-10-25-11-13-26(14-12-25)20-7-4-3-6-19(20)23/h3-4,6-9,16H,5,10-15H2,1-2H3,(H,24,27) |
| Stdinchikey: | PHOCQBYGUQPMIB-UHFFFAOYSA-N |
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]
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Pharmacology
Mafoprazine!Site!Ki (nM)!Species!Ref| D2 | 10.7 | Rat | [5] |
| α1 | 12.7 | Rat | |
| α2 | 101.0 | Rat | | |
It demonstrates activity as a D2 dopamine receptor antagonist, an α1 adrenergic receptor antagonist, and an α2 adrenergic receptor agonist.[6]
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.[6]
The Ki for various receptors was determined using rat neuronal receptor binding assays.
History
Mafoprazine was first synthesized in 1988.[6] It is sold as Mafropan® by DS Pharma Animal Health Co. Ltd., Osaka, Japan.
Notes and References
- Web site: Mafoprazine Chemical Substance Information J-GLOBAL . jglobal.jst.go.jp . en.
- Book: Heishima . Kazuki . Kuo . Kendon . Kimura . Masashi . Mori . Takashi . Animal Lymphocyte Metaphase Chromosome Preparation . Radiation Cytogenetics . Methods in Molecular Biology . 2019 . 1984 . 7–22 . 10.1007/978-1-4939-9432-8_2. 31267415 . 978-1-4939-9430-4 . 195787061 .
- Azizi . AFN . Miyazaki . R . Yumito . T . Ohashi . Y . Uno . S . Miyajima . U . Kumamoto . M . Uchiyama . S . Yasuda . M . Effect of maternal supplementation with seaweed powder on immune status of liver and lymphoid organs of piglets. . The Journal of Veterinary Medical Science . 1 January 2018 . 80 . 1 . 8–12 . 10.1292/jvms.17-0537 . 29142150. 5797852 .
- Umeyama . Kazuhiro . Watanabe . Kota . Watanabe . Masahito . Horiuchi . Keisuke . Nakano . Kazuaki . Kitashiro . Masateru . Matsunari . Hitomi . Kimura . Tokuhiro . Arima . Yoshimi . Sampetrean . Oltea . Nagaya . Masaki . Saito . Masahiro . Saya . Hideyuki . Kosaki . Kenjiro . Nagashima . Hiroshi . Matsumoto . Morio . Generation of heterozygous fibrillin-1 mutant cloned pigs from genome-edited foetal fibroblasts . Scientific Reports . 14 April 2016 . 6 . 1 . 24413 . 10.1038/srep24413. 27074716 . 2016NatSR...624413U . 22352477 . free . 4830947 .
- Web site: NCATS Inxight Drugs — MAFOPRAZINE . drugs.ncats.io . en.
- Fukuchi . Isao . Kawashima . Kazutaka . Matsuoka . Yuzo . Ishida . Ryuichi . Neurochemical study of mafoprazine, a new phenylpiperazine derivative. . The Japanese Journal of Pharmacology . 1988 . 47 . 1 . 51–61 . 10.1254/jjp.47.51. 3411821 . 13158367 . free .
