thioperamide maleate salt CAS#: 148440-81-7

thioperamide maleate salt Basic information

Product Name:

thioperamide maleate salt

Synonyms:

MR-12842, N-Cyclohexyl-4-(1H-imidazol-4-yl)-1-piperidinecarbothioamide maleate salt
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)
MR-12842 maleate
MR-12842,inhibit,Thioperamide maleate,MR 12842,MR12842,Histamine Receptor,Inhibitor,Thioperamide
Thioperamide maleate, H3 antagonist

CAS:

148440-81-7

MF:

C15H24N4SC4H4O4

MW:

0

Mol File:

148440-81-7.mol

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thioperamide maleate salt Chemical Properties

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

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Safety Information

Hazard Codes: Xi
Risk Statements: 36/37/38
Safety Statements: 26-36
WGK Germany: 3

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thioperamide maleate salt Usage And Synthesis

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 pK_i 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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