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Thioperamide maleate

SKU: orb1303137

Description

Thioperamide maleate (MR-12842 maleate) is a potent and selective histamine H3 receptor antagonist, with a Ki of 4.3 nM for receptor binding and 31 nM for inhibiting [³H]histamine synthesis. This compound is widely used in neuroscience research to study H3 receptor function in both in vitro and in vivo models of sleep, cognition, and energy homeostasis.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Thioperamide maleate

Key Properties

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CAS Number148440-81-7
MW408.52
Purity98.48% (May vary between batches)
FormulaC19H28N4O4S
SMILESOC(=O)\C=C/C(O)=O.S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1
TargetHistamine Receptor
SolubilityDMSO:55 mg/mL (134.63 mM)

Bioactivity

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Target IC50
H3 receptor:4.3 nM(Ki)|[3H]-Histamine synthesis:31 nM(Ki)
In Vivo
In C57BL/6J mice, Thioperamide (5-20 mg/kg; i.p.) facilitates reconsolidation of a contextually-conditioned fear memory.
In Vitro
Thioperamide maleate (0.01, 0.1, 1, 10, 100 μM) promotes the viability of NE-4C stem cells in a concentration-dependent manner. Thioperamide maleate displays similar potencies at human H4 and H3 receptors with Kis of 43 and 60 nM, respectively. Thioperamide maleate inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide maleate competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Histamine Receptor, HistamineReceptor, Inhibitor, H3 receptor, inhibit, MR12842, MR-12842, MR12842 Maleate, MR-12842 maleate, MR-12842 Maleate, MR 12842, MR 12842 Maleate, Thioperamide, Thioperamide maleate, Thioperamide Maleate
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
11211984 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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25 mg
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1 mg
$ 80.00
5 mg
$ 130.00
1 ml x 10 mM (in DMSO)
$ 140.00
10 mg
$ 170.00
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