| Identification | Back Directory | [Name]
CLOBENPROPIT DIHYDROBROMIDE | [CAS]
145231-45-4 | [Synonyms]
CS-683
VUF 9153
Clobenpropit 2HBr
Clobenpropit dihydro
VUF 9153 DIHYDROBROMIDE
CLOBENPROPIT DIHYDROBROMIDE
Clobenpropit dihydrobromide solid
N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA
S-(3-(4(5)-Imidazolyl))propyl-N-(4-chlorobenzyl)isothiourea
3-(1H-Imidazol-4-yl)propyl ((4-chlorophenyl)methyl)carbamimidothioate
N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazoyl)propyl]isothiourea dihydrobromide
N-(4-CHLOROBENZYL)-S-[3-(4(5)-IMIDAZOLYL)PROPYL]ISOTHIOUREA DIHYDROBROMIDE
[(4-Chlorophenyl)methyl]carbamimidothioic acid 3-(1H-imidazol-4-yl)propyl ester
Carbamimidothioic acid, ((4-chlorophenyl)methyl)-, 3-(1H-imidazol-4-yl)propyl ester
CarbaMiMidothioic acid, N-[(4-chlorophenyl)Methyl]-, 3-(1H-iMidazol-5-yl)propyl ester
([4-CHLOROPHENYL]METHYL)-3-(1H-IMIDAZOL-4-YL)PROPYL ESTER CARBAMIMIDOTHIOIC ACID DIHYDROBROMIDE
VUF 9153, [(4-Chlorophenyl)methyl]-3-(1H-imidazol-4-yl)propyl ester carbamimidothioic acid dihydrobromide | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C14H17ClN4S | [MDL Number]
MFCD00467655 | [MOL File]
145231-45-4.mol | [Molecular Weight]
308.83 |
| Chemical Properties | Back Directory | [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 | [form ]
solid | [pka]
14.55±0.10(Predicted) | [color ]
white | [Water Solubility ]
H2O: >20mg/mL
ethanol: 3.30mg/mL
DMSO: >30mg/mL |
| Hazard Information | Back Directory | [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 |
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