1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Thioperamide

Thioperamide (Synonyms: MR-12842)

Cat. No.: HY-12206
Handling Instructions

Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide inhibits [3H]histamine synthesis with a Ki of 31 nM.

For research use only. We do not sell to patients.

Thioperamide Chemical Structure

Thioperamide Chemical Structure

CAS No. : 106243-16-7

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Description

Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide inhibits [3H]histamine synthesis with a Ki of 31 nM[1].

IC50 & Target[1]

H3 Receptor

 

In Vitro

Thioperamide inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki of 4 nM[1].
Thioperamide (0.01-100 μM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner[2].

Cell Viability Assay[2]

Cell Line: NE-4C stem cells
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 24 hours
Result: The viability of NE-4C stem cells increased significantly to 150.83±6.91% when (1 μM) was administrated, and increased to 145.11±14.52% and 132.02%±25.65% when 10 μM and 100 μM were administrated respectively.
In Vivo

Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice[3].

Animal Model: Naive female C57BL/6J mice[3]
Dosage: 5, 10 or 20 mg/kg
Administration: Injections (i.p.)
Result: Facilitated reconsolidation of a contextually-conditioned fear memory.
Molecular Weight

292.44

Formula

C₁₅H₂₄N₄S

CAS No.

106243-16-7

SMILES

S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ThioperamideMR-12842MR12842MR 12842Histamine ReceptorH3receptorreleasehistaminesynthesisParkinsonInhibitorinhibitorinhibit

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