Dimaprit dihydrochloride

Names

[ Name ]:
Dimaprit dihydrochloride

[Synonym ]:
S-(3-Dimethylaminopropyl)isothiourea dihydrobromide
Carbamimidothioic acid (3-(dimethylamino)propyl ester
3-(dimethylamino)propyl carbamimidothioate,dihydrochloride

Biological Activity

[Description]:

Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Endocrinology

Signaling Pathways >> Immunology/Inflammation >> NO Synthase

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H2 Receptor

nNOS:49 μM (IC50)

[In Vitro]

Dimaprit has less than 0.0001% the activity of histamine on H1-receptors[1]. Dimaprit (0.1 nM-100 μM) inhibits nNOS concentration dependently with an IC50 of 49±14 μM[2].

[In Vivo]

Dimaprit stimulates gastric acid secretion in rats (1.25 μM/kg/min; rapid i.v. injection), cats (2-64 μM/h; i.v.) and dogs (1-100 nM/kg/min; i.v.)[1]. Dimaprit (0.01-1 μM/kg; i.v. at intervals of 5 min) causes dose-dependent falls in blood pressure in cats. Dimaprit (1-100 nM; intra-arterial injection) causes vasodilatation in the femoral vascular bed, and it (1 μM/kg; bolus or intravenous injection) has no effect on heart rate[1].

[References]

[1]. Parsons ME, et, al. Dimaprit -(S-[3-(N,N-dimethylamino)prophyl]isothiourea) - a highly specific histamine H2 -receptor agonist. Part 1. Pharmacology. Agents Actions. 1977 Mar; 7(1): 31-7.

[2]. Paquay JB, et, al. Nitric oxide synthase inhibition by dimaprit and dimaprit analogues. Br J Pharmacol. 1999 May; 127(2): 331-4.

Chemical & Physical Properties

[ Molecular Formula ]:
C₆H₁₇Cl₂N₃S

[ Molecular Weight ]:
234.19000

[ Exact Mass ]:
233.05200

[ PSA ]:
78.41000

[ LogP ]:
2.96880

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UM3850000

CHEMICAL NAME :: Pseudourea, 2-(3-(dimethylamino)propyl)-2-thio-, dihydrochloride

CAS REGISTRY NUMBER :: 23256-33-9

LAST UPDATED :: 199012

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C6-H15-N3-S.2Cl-H

MOLECULAR WEIGHT :: 234.22

WISWESSER LINE NOTATION :: MUYZS3N1&1 &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: AD277-689

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2930909090

Preparation

Customs

[ HS Code ]: 2930909090

[ Summary ]:
2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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Related Compounds

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