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Thioperamide maleate

Catalog No. T41247 CAS 148440-81-7

Synonyms: MR-12842 maleate

Thioperamide maleate (MR-12842 maleate) is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31 nM).

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Thioperamide maleate, CAS 148440-81-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
5 mg	In stock	$ 437.00
10 mg	In stock	$ 646.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,380.00
100 mg	In stock	$ 1,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 489.00

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Purity: 99.88%

Biological Description

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Description	Thioperamide maleate (MR-12842 maleate) is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31 nM).
Targets&IC50	H3 receptor:4.3 nM(Ki), [3H]-Histamine synthesis:31 nM(Ki)
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[1]. Thioperamide maleate displays similar potencies at human H4 and H3 receptors with Kis of 43 and 60 nM, respectively[2]. 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[4].
In vivo	In C57BL/6J mice, Thioperamide (5-20 mg/kg; i.p.) facilitates reconsolidation of a contextually-conditioned fear memory[3].

Synonyms	MR-12842 maleate
Molecular Weight	408.52
Formula	C19H28N4O4S
CAS No.	148440-81-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (134.63 mM)

References and Literature

1. Na Wang, et al. Histamine H3 Receptor Antagonist Enhances Neurogenesis and Improves Chronic Cerebral Hypoperfusion-Induced Cognitive Impairments. Front Pharmacol. 2020 Jan 21;10:1583. 2. Y Charlier, et al. Differential Effects of Histamine H(3) Receptor Inverse Agonist Thioperamide, Given Alone or in Combination With the N-methyl-d-aspartate Receptor Antagonist Dizocilpine, on Reconsolidation and Consolidation of a Contextual Fear Memory 3. Gbahou F, et al. Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br J Pharmacol. 2006;147(7):744-754. 4. J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.

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Keywords

Thioperamide maleate 148440-81-7 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor MR-12842 MR 12842 Maleate inhibit MR12842 Maleate MR-12842 maleate Thioperamide Maleate MR 12842 MR12842 MR-12842 Maleate Inhibitor Thioperamide inhibitor

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