Dimaprit dihydrochloride - CAS 23256-33-9
Category: Inhibitor
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Molecular Formula:
C6H15N3S.2HCl
Molecular Weight:
234.19
COA:
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Targets:
Histamine Receptor
Description:
The hydrochloride salt form of Dimaprit, which has been found to be a histamine H2 receptor agonist.
Purity:
≥99% by HPLC
Appearance:
White Solid
Synonyms:
S-(3-Dimethylaminopropyl)isothiourea dihydrochloride
MSDS:
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InChIKey:
DFWCPLGXFMSUCW-UHFFFAOYSA-N
InChI:
InChI=1S/C6H15N3S.2ClH/c1-9(2)4-3-5-10-6(7)8;;/h3-5H2,1-2H3,(H3,7,8);2*1H
Canonical SMILES:
CN(C)CCCSC(=N)N.Cl.Cl
1.In vitro relaxation of dog cerebral veins in response to histamine is mediated by histamine H2 receptors.
Monge L;García-Villalón AL;Fernández N;García JL;Gómez B;Diéguez G Eur J Pharmacol. 1997 Nov 5;338(2):135-41.
There is little information on the histamine receptor mechanisms involved in cerebral venodilation, thus the role of histamine present in human cerebrospinal fluid is difficult to assess. In isolated canine pial veins, concentration-response curves to histamine (10[-7]-10[-3] M), the histamine H1 receptor agonist, 2-pyridylethylamine (10[-6]-10[-2] M), the histamine H2 receptor agonist, dimaprit (S-(3-dimethylaminopropyl) isothiourea dihydrochloride, 10[-6]-10[-2] M), and the histamine H3 receptor agonist, imetit (S-[2-(1 midazol-4-yl)ethyl]isothiourea dihydrobromide, 10[-7]-10[-3] M) were isometrically determined. In resting veins, histamine, 2-pyridylethylamine and dimaprit had no significant effect, whereas in endothelin-1-precontracted veins, these drugs produced concentration-dependent relaxation (Emax in % of active tone and pD2 were: for histamine, 72 +/- 6 and 5.36 +/- 0.09; for 2-pyridylethylamine, 59 +/- 5 and 3.28 +/- 0.05; for dimaprit, 65 +/- 7 and 4.81 +/- 0.10, respectively). The relaxations in response to histamine and dimaprit were competitively antagonized by the histamine H2 receptor antagonist, cimetidine (3 x 10[-6]-10[-4] M) (pA2 = 6.07 +/- 0.03 for histamine, and 6.
2.H2-receptors in the human ocular surface.
Abelson MB;Udell IJ Arch Ophthalmol. 1981 Feb;99(2):302-4.
Ten normal human volunteers participated in a two-part study of H2-receptor activity in the ocular surface. Dimethylaminopropylisothiourea (trivial name, dimaprit dihydrochloride), a highly selective H2-receptor agonist, produced vasodilation without itch. Pretreatment with the H2-receptor antagonist, cimetidine, significantly blocked the vasodilatory effect of dimethylaminopropylisothiourea, whereas pretreatment with the H1-receptor antagonist, antazoline phosphate, did not. We conclude that H2-receptors are present in the human ocular surface.
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CAS 23256-33-9 Dimaprit dihydrochloride

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