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化驗
≥98% (HPLC)
形狀
solid
儲存條件
desiccated
under inert gas
顏色
off-white
溶解度
DMSO: 30 mg/mL
water, high purity: 30 mg/mL
儲存溫度
2-8°C
SMILES 字串
Cl.O=C(C1CC1)c2ccc(OCCCc3c[nH]cn3)cc2
InChI
1S/C16H18N2O2.ClH/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-14;/h5-8,10-12H,1-4,9H2,(H,17,18);1H
InChI 密鑰
PWAPSKMHZQQTRJ-UHFFFAOYSA-N
生化／生理作用
Ciproxifan belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
特點和優勢
This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
Yan Chen et al.
Frontiers in pharmacology, 12, 599393-599393 (2021-06-18)
NLRP3 inflammasome has been implicated in impaired post-injury muscle healing and in muscle atrophy. Histamine receptors play an important role in inflammation, but the role of histamine H3 receptor (H3R) in myocyte regeneration and in the regulation of NLRP3 inflammasome
Tao Luo et al.
CNS neuroscience & therapeutics, 23(4), 301-309 (2017-02-09)
Exposure to pharmacological concentration of inhaled anesthetics such as isoflurane can cause short- or long-term cognitive impairments in preclinical studies. The selective antagonists of the histamine H3 receptors are considered as a promising group of novel therapeutic agents for the
Cecilia Flores-Clemente et al.
Neuroscience letters, 641, 77-80 (2017-01-28)
There is evidence for genetic polymorphism within the human histamine H
Emil Trofimiuk et al.
Behavioural brain research, 283, 145-153 (2015-02-03)
Despite the development of neuroscience and spectacular discoveries, the clear functions and the role of histamine are still not fully understood, especially in the context of the negative impact of prolonged stress exposure on the cognition. The purpose of this
Nayeli Rivera-Ramírez et al.
Neurochemistry international, 101, 38-47 (2016-11-05)
The histamine H3 receptor (H3R) is abundantly expressed in the Central Nervous System where it regulates several functions pre and postsynaptically. H3Rs couple to Gαi/o proteins and trigger or modulate several intracellular signaling pathways, including the cAMP/PKA pathway and the
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