CAS 145231-45-4|Clobenpropit
| Common Name | Clobenpropit | ||
|---|---|---|---|
| CAS Number | 145231-45-4 | Molecular Weight | 470.65300 |
| Density | 1.31g/cm3 | Boiling Point | 551.3ºC at 760mmHg |
| Molecular Formula | C14H19Br2ClN4S | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 287.2ºC |
Names
| Name | clobenpropit |
|---|---|
| Synonym | More Synonyms |
Clobenpropit BiologicalActivity
| Description | Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock[1][2]. |
|---|---|
| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
| Target | H3 receptor |
| In Vivo | Clobenpropit (15 mg/kg；腹腔注射；每天一次，持续 7 天) 可抵消 MK-801 (HY-15084B) 对多巴胺和组胺水平的调节作用，并防止 MK-801 诱导的过度运动行为[1]。< br/>Clobenpropit (1、2、5 μmoL/kg；静脉注射) 对遭受失血性休克的大鼠产生复苏作用[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). |
| References | [1]. Mahmood D, et al. The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats. J Exp Neurosci. 2015 Aug 31;9:73-80. [2]. Wanot B, et al. Cardiovascular effects of H3 histamine receptor inverse agonist/ H4 histamine receptor agonist, clobenpropit, in hemorrhage-shocked rats. PLoS One. 2018 Aug 2;13(8):e0201519. |
Chemical & Physical Properties
| Density | 1.31g/cm3 |
|---|---|
| Boiling Point | 551.3ºC at 760mmHg |
| Molecular Formula | C14H19Br2ClN4S |
| Molecular Weight | 470.65300 |
| Flash Point | 287.2ºC |
| Exact Mass | 467.93900 |
| PSA | 89.86000 |
| LogP | 5.86030 |
| Vapour Pressure | 3.35E-12mmHg at 25°C |
| Index of Refraction | 1.645 |
| InChIKey | UCAIEVHKDLMIFL-UHFFFAOYSA-N |
| SMILES | NC(=NCc1ccc(Cl)cc1)SCCCc1cnc[nH]1 |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
Articles30
More Articles| Histamine H3 receptor activation counteracts adenosine A2A receptor-mediated enhancement of depolarization-evoked [3H]-GABA release from rat globus pallidus synaptosomes. ACS Chem. Neurosci. 5(8) , 637-45, (2014) High levels of histamine H3 receptors (H3Rs) are found in the globus pallidus (GP), a neuronal nucleus in the basal ganglia involved in the control of motor behavior. By using rat GP isolated nerve te... | |
| Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies. J. Med. Chem. 54 , 8136-47, (2011) The histamine H(4) receptor (H(4)R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine H(3) receptor (H(3)R), two acidic residues ... | |
| Adipogenic and lipolytic effects of chronic glucocorticoid exposure. Am. J. Physiol. Cell Physiol. 300 , C198-209, (2011) Glucocorticoids have been proposed to be both adipogenic and lipolytic in action within adipose tissue, although it is unknown whether these actions can occur simultaneously. Here we investigate both ... |
Synonyms
| Clobenpropit dihydrobromide,N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothioureadihydrobromide |
