化合物Ciproxifan maleate T2004

Product Introduction
Bioactivity


英文名: Ciproxifan maleate

描述: Ciproxifan maleate (FUB 359) 是一种选择性的，可口服和竞争性的组胺H3受体拮抗剂，IC50值为 9.2 nM。它对其他受体亚型的表观亲和力低，可用于研究衰老性疾病和阿尔兹海默症。

体外活性: Ciproxifan inhibits [3H]HA release from synaptosomes with Ki of 0.5 nM. Ciproxifan inhibits the binding of [125I]iodoproxyfan at the brain H3 receptor with Ki of 0.7 nM. Ciproxifan displays high affinity at H3 receptor but shows low apparent affinity at other receptor subtypes as evaluated in functional tests on isolated organs (histamine H1 and H2, muscarinic M3, adrenergic α1D and β1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4). [1]

体内活性: Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. [1] Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. [3] Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. [4] Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats. [5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 54 mg/mL (139.75 mM)
DMSO : 10 mM


关键字: Inhibitor | FUB-359 Maleate | aging | FUB359 Maleate | inhibit | Ciproxifan | disorders | Ciproxifan maleate | FUB359 | Histamine Receptor | histamine | FUB-359 | Ciproxifan Maleate | FUB 359 Maleate | Alzheimer's

相关产品: Wy 49051 | Thioperamide maleate | Triprolidine hydrochloride monohydrate | Alginic acid | Mirtazapine | Chlorcyclizine | Pitolisant hydrochloride | Meclizine | Bavisant | Meclizine dihydrochloride

相关库: Anti-Neurodegenerative Disease Compound Library | Anti-COVID-19 Compound Library | Histamine & Melatonin Receptor-Targeted Compound Library | Anti-Parkinson's Disease Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | GPCR Compound Library | Inhibitor Library | Orally Active Compound Library | Bioactive Compound Library

化合物Ciproxifan maleate T2004信息由TargetMol中国为您提供，如您想了解更多关于化合物Ciproxifan maleate T2004报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途