A histamine H2 receptor agonist
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Dimaprit (hydrochloride)

Item No. 29418

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
carbamimidothioic acid, 3-(dimethylamino)propyl ester, dihydrochloride
CAS Number
23256-33-9
Molecular Formula
C6H15N3S • 2HCl
Formula Weight
234.2
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
NC(SCCCN(C)C)=N.Cl.Cl
InChi Code
InChI=1S/C6H15N3S.2ClH/c1-9(2)4-3-5-10-6(7)8;;/h3-5H2,1-2H3,(H3,7,8);2*1H
InChi Key
DFWCPLGXFMSUCW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 mg

    $74

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    100 mg

    $118

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    250 mg

    $274

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    Product Description

    Dimaprit is a histamine H2 receptor agonist with a Ki value of 44 µM in guinea pig right atrium.1,2 It is selective for histamine H2 over H1 and H3 receptors with relative potencies of 71, <0.0001, and <0.008, respectively, compared to histamine. Dimaprit (6 μM) inhibits histamine release from isolated peritoneal mast cells in a rat model of anaphylaxis induced by A. suum extract, which is not affected by pretreatment with mepyramine (Item No. 20978), an H1 receptor inverse agonist, or cimetidine (Item No. 18743), an H2 receptor antagonist.3 It stimulates gastric acid secretion in vivo in anaesthetized rats and cats with relative potencies of 19.5 and approximately 400 to 500, respectively, compared to histamine.4 Dimaprit inhibits 2-(2-pyridyl)ethylamine-induced bronchoconstriction in guinea pigs in a dose-dependent manner.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hill, S.J. Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol. Rev. 42(1), 45-83 (1990).

    2. Rising, T.J., and Steward, A. The determination of receptor constants for histamine H2-agonists in the guinea-pig isolated right atrium using an irreversible H2-antagonist. Br. J. Pharmacol. 87(1), 211-216 (1986).

    3. Kohno, S., Ogawa, K., Nabe, T., et al. Dimaprit, a histamine H2-agonist, inhibits anaphylactic histamine release from mast cells and the decreased release is restored by thioperamide (H3-antagonist), but not by cimetidine (H2-antagonist). Jpn. J. Pharmacol. 62(1), 75-79 (1993).

    4. Parsons, M.E., Owen, D.A.A., Ganellin, C.R., et al. Dimaprit-[S-[3-(N,N-dimethylamino)propyl]isothiourea] — A highly specific histamine H2-receptor agonist. Part 1. Pharmacology. Agents Actions 7(1), 31–37 (1977).

    5. Drazen, J.M., Schneider, M.W., and Venugopalan, C.S. Bronchodilator activity of dimaprit in the guinea pig in vitro and in vivo. Eur. J. Pharmacol. 55(3), 233-239 (1979).