CLOBENPROPIT DIHYDROBROMIDE CAS#: 145231-45-4

CLOBENPROPIT DIHYDROBROMIDE Basic information

Product Name:

CLOBENPROPIT DIHYDROBROMIDE

Synonyms:

N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazoyl)propyl]isothiourea dihydrobromide
3-(1H-Imidazol-4-yl)propyl ((4-chlorophenyl)methyl)carbamimidothioate
Carbamimidothioic acid, ((4-chlorophenyl)methyl)-, 3-(1H-imidazol-4-yl)propyl ester
S-(3-(4(5)-Imidazolyl))propyl-N-(4-chlorobenzyl)isothiourea
CarbaMiMidothioic acid, N-[(4-chlorophenyl)Methyl]-, 3-(1H-iMidazol-5-yl)propyl ester
[(4-Chlorophenyl)methyl]carbamimidothioic acid 3-(1H-imidazol-4-yl)propyl ester
([4-CHLOROPHENYL]METHYL)-3-(1H-IMIDAZOL-4-YL)PROPYL ESTER CARBAMIMIDOTHIOIC ACID DIHYDROBROMIDE
CLOBENPROPIT DIHYDROBROMIDE

CAS:

145231-45-4

MF:

C14H17ClN4S

MW:

308.83

EINECS:

604-604-1

Product Categories:

Histamine receptor

Mol File:

145231-45-4.mol

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CLOBENPROPIT DIHYDROBROMIDE Chemical Properties

Boiling point:: 525.3±60.0 °C(Predicted)
Density: 1.31±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: H₂O: >20 mg/mL
pka: 14.55±0.10(Predicted)
form: solid
color: white
Water Solubility: H2O: >20mg/mL
ethanol: 3.30mg/mL
DMSO: >30mg/mL
InChI: 1S/C14H17ClN4S.2BrH/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);2*1H
InChIKey: JIJQPEZAVLJZBO-UHFFFAOYSA-N
SMILES: Br[H].Br[H].Clc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1

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Safety Information

WGK Germany: 3
Storage Class: 11 - Combustible Solids

MSDS

Language:English Provider:SigmaAldrich

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CLOBENPROPIT DIHYDROBROMIDE Usage And Synthesis

Uses

Clobenpropit Dihydrobromide and it’s analogues functions as potent histamine H3 antagonist.

Definition

ChEBI: An imidothiocarbamic ester that consists of isothiourea bearing S-3-(imidazol-4-yl)propyl and N-4-chlorobenzyl substituents. An extremely potent histamine H3 antagonist/inverse agonist (pA

Biological Activity

An extremely potent histamine H 3 antagonist/inverse agonist (pA 2 =9.93). Also displays partial agonist activity at H 4 receptors; induces eosinophil shape change with an EC 50 of 3 nM. Also available as part of the Histamine H 3 Receptor Tocriset™ .

Biochem/physiol Actions

Selective H3 histamine receptor antagonist that crosses the blood-brain barrier.

in vivo

Clobenpropit (15 mg/kg; i.p.; once daily for 7 days) counteracts the modulatory effects of MK-801 (HY-15084B) on dopamine and histamine levels and prevents MK-801-induced hyper locomotor behaviors^[1].
Clobenpropit (1, 2, 5 μmoL/kg; i.v.) causes a resuscitating effect in rats subjected to the hemorrhagic shock^[2].

Animal Model:	150-200g, 12-week-old male wistar albino rats^[1]
Dosage:	15 mg/kg
Administration:	I.p.; once daily for 7 days
Result:	Exhibited a significant reduction of hyperlocomotor activities induced by a single-dose administration of MK-801 (0.2 mg/kg, i.p.), and reduced the MK-801-induced dopamine release, exhibited further increase in histamine levels in the hypothalamus.

Animal Model:	205-470g, adult male Wistar rats^[2]
Dosage:	1, 2, 5 μmoL/kg (after 6-hydroxydopamine (50 mg/kg (SC) for 3 consecutive days)
Administration:	I.v.
Result:	Triggered a statistically significant increase of mean arterial pressure (MAP) (dose 2 μmol/kg) and heart rate (HR) (doses of 1, 2, 5 μmol/kg).

IC 50

H₃ receptor

CLOBENPROPIT DIHYDROBROMIDESupplier

J & K SCIENTIFIC LTD.

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3B Pharmachem (Wuhan) International Co.,Ltd.

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Shanghai Sphchem Co., Ltd.

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BOC Sciences

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Hangzhou Sage Chemical Co., Ltd.

Tel: +86057186818502 13588463833
Email: info@sagechem.com

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