thioperamide maleate salt

Product Namethioperamide maleate salt
CAS148440-81-7
MFC15H24N4SC4H4O4
MW0
EINECS
MOL File148440-81-7.mol

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
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

Safety Information

Hazard Codes	Xi
Risk Statements	36/37/38
Safety Statements	26-36
WGK Germany	3
Storage Class	11 - Combustible Solids

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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