Home Neuronal Signaling Histamine Receptor antagonist Ciproxifan Maleate For research use only.

Ciproxifan Maleate

Synonyms: FUB 359

Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.

Ciproxifan Maleate Chemical Structure

Ciproxifan Maleate Chemical Structure

CAS No. 184025-19-2

Purity & Quality Control

Batch: S281301 DMSO]54 mg/mL]false]Ethanol]54 mg/mL]false]Water]1 mg/mL]false Purity: 100%
100

Ciproxifan Maleate Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.
Targets
Histamine H3 receptor [1]
9.2 nM
In vitro
In vitro 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]
In Vivo
In vivo 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]
Animal Research Animal Models Male Swiss mice
Dosages 1 mg/kg
Administration Intravenous or oral adminstration

Chemical Information & Solubility

Molecular Weight 386.4 Formula

C16H18N2O2.C4H4O4
CAS No. 184025-19-2 SDF Download Ciproxifan Maleate SDF
Smiles C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (139.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : 1 mg/mL


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In vivo
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