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

Key Properties

• CAS Number: 148440-81-7
• MW: 408.52
• Purity: 99.88% (May vary between batches)
• Formula: C₁₉H₂₈N₄O₄S
• SMILES: OC(=O)\C=C/C(O)=O.S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1
• Target: Histamine Receptor
• Solubility: DMSO:55 mg/mL (134.63 mM)

Bioactivity

• 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

• Storage: Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

11211984