145231-45-4

145231-45-4 structure

Name: Clobenpropit
Chemical Name: clobenpropit
CAS Number: 145231-45-4
Molecular Formula: C₁₄H₁₉Br₂ClN₄S
Molecular Weight: 470.65300
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-12-17 18:25:02
Modify Date: 2024-01-08 14:53:22
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].

Name	clobenpropit
Synonyms	Clobenpropit dihydrobromide,N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothioureadihydrobromide

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.

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

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