A histamine H3 receptor antagonist
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Iodophenpropit (hydrobromide)

Item No. 32850

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[2-(4-iodophenyl)ethyl]-carbamimidothioic acid, 3-(1H-imidazol-4-yl)propyl ester, dihydrobromide
CAS Number
145196-87-8
Molecular Formula
C15H19IN4S • 2HBr
Formula Weight
576.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/mlWater: 50 mg/ml
SMILES
IC1=CC=C(CCNC(SCCCC2=CN=CN2)=N)C=C1.Br.Br
InChi Code
InChI=1S/C15H19IN4S.2BrH/c16-13-5-3-12(4-6-13)7-8-19-15(17)21-9-1-2-14-10-18-11-20-14;;/h3-6,10-11H,1-2,7-9H2,(H2,17,19)(H,18,20);2*1H
InChi Key
BOSOGNBLIWPCMS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $50

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    5 mg

    $134

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    10 mg

    $195

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    Product Description

    Iodophenpropit is a histamine H3 receptor antagonist (pA2 = 9.6 in guinea pig intestine, which has a high endogenous expression of H3 receptors).1 It increases forskolin-induced cAMP production in SK-N-MC cells expressing the recombinant human H3 receptor (EC50 = 25.1 nM).2 It is also an inhibitor of NR1/NR2A, NR1/NR2B, NR1/NR2C, and NR1/NR2D subunit-containing NMDA receptors (IC50s = 1.3, 1.4, 9.7, and 14 µM, respectively, for the rat recombinant receptors).3 Iodophenpropit induces scratching behavior in mice when administered intradermally at a dose of 10 nmol and reduces amygdala-kindled seizure duration in rats (ED50 = 2.54 mg/kg).4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jansen, F.P., Wu, T.S., Voss, H.P., et al. Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain. Br. J. Pharmacol. 113(2), 355-362 (1994).

    2. Wieland, K., Bongers, G., Yamamoto, Y., et al. Constitutive activity of histamine H3 receptors stably expressed in SK-N-MC cells: Display of agonism and inverse agonism by H3 antagonists. J. Pharmacol. Exp. Ther. 299(3), 908-914 (2001).

    3. Hansen, K.B., Mullasseril, P., Dawit, S., et al. Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J. Pharmacol. Exp. Ther. 333(3), 650-662 (2010).

    4. Hossen, M.A., Inoue, T., Shinmei, Y., et al. Role of substance P on histamine H3 antagonist-induced scratching behavior in mice. J. Pharmacol. Sci. 100(4), 297-302 (2006).

    5. Harada, C., Fujii, Y., Hirai, T., et al. Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures. Brain Res. Bull. 63(2), 143-146 (2004).