Ciproxifan maleate

SKU: orb1225859

Description

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

Key Properties

• CAS Number: 184025-19-2
• MW: 386.4
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂N₂O₆
• SMILES: C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=C\C(=O)O)\C(=O)O
• Target: Histamine Receptor
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED50 of 0.14 mg/kg. Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration is 0.25 sec instead of 0.50 sec. 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. Ciproxifan (1 mg/kg; a single i. v.) decreases the H3-receptor ligand concentration in serum in mice, with the half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively. Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F = 62%) and maximal concentration (Cmax = 420 nM) in mice.
• In Vitro:
  Ciproxifan inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM. Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [125I]iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Histamine Receptor