Clobenpropit

Names

[ Name ]:
Clobenpropit

[Synonym ]:
Clobenpropit dihydrobromide,N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothioureadihydrobromide

Biological Activity

[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 Receptor

Research Areas >> Neurological Disease

Signaling 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

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

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 ...