A selective histamine H3 receptor antagonist
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Clobenpropit (hydrobromide)

Item No. 10011126

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(4-chlorophenyl)methyl]-carbamimidothioic acid, 3-(1H-imidazol-5-yl)propyl ester, dihydrobromide
CAS Number
145231-35-2
Synonyms
  • VUF 9153
Molecular Formula
C14H17ClN4S • 2HBr
Formula Weight
470.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/mlEthanol: 2.5 mg/mlWater: 20 mg/ml
λmax
221 nm
SMILES
N=C(SCCCc1cnc[nH]1)NCc1ccc(Cl)cc1
InChi Code
InChI=1S/C14H17ClN4S/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19)
InChi Key
UCAIEVHKDLMIFL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    25 mg

    $534

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    Product Description

    Clobenpropit is a selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes).1 Clobenpropit (0.3, 0.1, and 3 nM) reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by the H3 receptor agonist (R)-α-methylhistamine (Item No. 25601). It does not inhibit histamine-induced contractions in isolated guinea pig ileum or tachycardia in isolated right atria at concentrations up to 1 μM, indicating a lack of functional antagonist activity at H1 and H2 receptors, respectively. Clobenpropit (1 and 3 mg/kg) decreases the duration of the tonic, clonic, and convulsive coma phases of electrically induced convulsions in mice, an effect that can be blocked by (R)-α-methylhistamine or imetit (Item No. 29517).2 Clobenpropit (0.1 μM) also increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Solt, L.A., Kumar, N., Nuhant, P., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature 472(7344), 491-494 (2011).

    2. Yokoyama, H., Onodera, K., Maeyama, K., et al. Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur. J. Pharmacol. 260(1), 23-28 (1994).

    3. Dai, H., Fu, Q., Shen, Y., et al. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur. J. PHarmacol. 563(1-3), 117-123 (2007).