| Identification | Back Directory | [Name]
thioperamide maleate salt | [CAS]
148440-81-7 | [Synonyms]
MR-12842 maleate
N-Cyclohexyl-4-(1H-imidazol-4-yl)-1-piperidinecarbothioamide maleate salt
MR-12842, N-Cyclohexyl-4-(1H-imidazol-4-yl)-1-piperidinecarbothioamide maleate salt
1-Piperidinecarbothioamide, N-cyclohexyl-4-(1H-imidazol-4-yl)-, (2Z)-2-butenedioate (1:1) | [Molecular Formula]
C15H24N4SC4H4O4 | [MDL Number]
MFCD00083209 | [MOL File]
148440-81-7.mol |
| Chemical Properties | Back Directory | [storage temp. ]
desiccated
under inert gas | [solubility ]
H2O: >10mg/mL | [form ]
solid | [color ]
white | [Water Solubility ]
H2O: >10mg/mL
DMSO: 12mg/mL
ethanol: 3mg/mL | [InChI]
1S/C16H25N3S.C4H4O4/c20-16(10-13-4-2-1-3-5-13)19-8-6-14(7-9-19)15-11-17-12-18-15;5-3(6)1-2-4(7)8/h11-14H,1-10H2,(H,17,18);1-2H,(H,5,6)(H,7,8)/b;2-1- | [InChIKey]
REZRBLGMJZZSID-BTJKTKAUSA-N | [SMILES]
OC(=O)\C=C/C(O)=O.S=C(CC1CCCCC1)N2CCC(CC2)c3c[nH]cn3 |
| Hazard Information | Back Directory | [Description]
Thioperamide (maleate) is a selective histamine H3 receptor antagonist that crosses the blood-brain barrier. This compound binds to rat cerebral cortical cells in vitro with a pKi value of 8.4 and inhibits histamine binding in vivo with an ED50 value of 1 mg/kg. At a dose of 5 mg/kg thioperamide (maleate) inhibits kindled seizures in rats by decreasing histamine and gamma-aminobutyric acid. | [Uses]
Thioperamide maleate salt was used to study the sympathetic and autonomic nerve activity in mammalian white adipose tissue. | [Biochem/physiol Actions]
Thioperamide is a potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier. It affects the central histaminergic system and decreases the duration of seizures and convulsions in mice. It also improves learning deficit induced by other drugs such as scopolamine. | [in vivo]
Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice[4]. | Animal Model: | Naive female C57BL/6J mice[4] | | Dosage: | 5, 10 or 20 mg/kg | | Administration: | Injections (i.p.) | | Result: | Facilitated reconsolidation of a contextually-conditioned fear memory. |
| [IC 50]
H3 Receptor | [References]
[1] GALINA MEIER . Influence of imidazole replacement in different structural classes of histamine H3-receptor antagonists[J]. European Journal of Pharmaceutical Sciences, 2001, 13 3: Pages 249-259. DOI: 10.1016/s0928-0987(01)00106-3
[2] CHIE HARADA. Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures[J]. Brain Research Bulletin, 2004, 63 2: Pages 143-146. DOI: 10.1016/j.brainresbull.2004.02.001 |
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