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Fig. 1 · Structure
Cat. No.
A11117
CAS No.
184025-19-2
Formula
C20H22N2O6
Mol. Weight
386.4

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Ciproxifan maleate

Cat. No. A11117 CAS 184025-19-2

H3-receptor antagonist

Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist.

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Biological Activity

Target & Activity

Target Activity Value
Histamine H3 receptor 9.2 nM

In Vitro Studies

Ciproxifan had a reported IC50 of 11.4 ± 1.2 μM in human recombinant membrane-bound MAO A. In crude pooled brain homogenates from male Wistar rats, Ciproxifan had a reported MAO A IC50 of 37.5 ± 0.2 μM. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Evaluation in Human Recombinant Membrane-Bound MAO A

Biochemical assay · human recombinant membrane-bound MAO A [1]

Ciproxifan was evaluated using human recombinant membrane-bound MAO A. The reported IC50 was 11.4 ± 1.2 μM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
IC50 valuesIC50 11.4 ± 1.2 μM[1]

Literature-Reported Treatment Conditions

Treatment concentration
between 10−9 M and 10−3 M
Exposure duration
over a period of at least 30 minutes (interval of 20–30 seconds)
Reported limits
Not stated in the sentences used: route, vehicle, control.
Methods and source locations

Compound reported in the paper: Ciproxifan

The paper names Ciproxifan without stating the salt or form; not verified as the maleate form supplied as A11117. No dose conversion or lot validation.

Methods > Spectrophotometric IC50 determination using human MAO (S15, S17, S19, S22); Table 2 (T2.h1, T2.h2, T2.h3, T2.r1, T2.r2)

IC50 values: IC50 values — Methods > Spectrophotometric IC50 determination using human MAO (S22); Table 2 (T2.h1, T2.h2, T2.h3, T2.r1, T2.r2)

Evaluation in Rat Brain Homogenate MAO A

Cell-based study · Wistar male rats; crude homogenates prepared from pooled brain from three rats; MAO A [1]

Ciproxifan was evaluated against MAO A in crude pooled brain homogenates from male Wistar rats. The reported IC50 was 37.5 ± 0.2 μM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
IC50 valuesIC50 37.5 ± 0.2 μM[1]

Literature-Reported Treatment Conditions

Treatment concentration
six different concentrations of ciproxifan between 10−9 M and 5 × 10−4 M
Reported limits
Not stated in the sentences used: route, schedule, vehicle, control.
Methods and source locations

Compound reported in the paper: Ciproxifan

The paper names Ciproxifan without stating the salt or form; not verified as the maleate form supplied as A11117. No dose conversion or lot validation.

Methods > Radiometric IC50 determination using rat brain MAO (S24, S25, S26, S27, S28); Table 2 (T2.h1, T2.h2, T2.h3, T2.r1, T2.r2)

IC50 values: IC50 values — Methods > Radiometric IC50 determination using rat brain MAO (S27, S28); Table 2 (T2.h1, T2.h2, T2.h3, T2.r1, T2.r2)

In Vivo Studies

In female wild-type mice, intraperitoneal Ciproxifan at 12 mg/kg significantly reduced LGN mean firing rates during white-noise stimulation in a before-and-after treatment comparison, with a reported median change of −3.0 Hz. In male wild-type mice under the no light condition, total sleep amount did not differ significantly between Ciproxifan and saline treatments (p = 0.71). [2,3]

Ciproxifan and LGN firing during white-noise stimulation

Animal study · female mice; wild-type (C57BL6/J; RRID:IMSR_JAX:000664); n = 126 cells from 4 animals [2]

In vivo single-unit extracellular recordings from the LGN in awake head-fixed mice; ciproxifan (12 mg/kg). During white-noise stimulation, significantly reduced mean firing rates (median, −3.0 Hz; IQR, 5.5 Hz; p < 0.001; n = 126 cells from 4 animals).

Measured endpoints — not treatment concentrations
EndpointReported resultReference
mean firing ratesmean firing rate median, −3.0 Hz[2]

Conditions shared by the study groups

Route
intraperitoneally injected
Treatment course
About 20 min after the injection and removal of the anesthesia
Vehicle
0.9% saline solution
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ciproxifan 12 mg/kgbeforeLGN; ciproxifan (12 mg/kg); during white-noise stimulation: significantly reduced mean firing rates (median, −3.0 Hz; IQR, 5.5 Hz; p < 0.001; n = 126 cells from 4 animals).[2]
Ciproxifan 12 mg/kg
Model: female mice; wild-type (C57BL6/J; RRID:IMSR_JAX:000664); n = 126 cells from 4 animals
Methods and source locations

Compound reported in the paper: Ciproxifan

The paper names Ciproxifan without stating the salt or form; not verified as the maleate form supplied as A11117. No dose conversion or lot validation.

Results > Histamine leads to weaker and slower visual responses in the mouse lateral geniculate nucleus (S1, S9, S19); Materials and methods > Animals (S102, S103); Materials and methods > Surgical procedures (S106, S108, S112, S116); Materials and methods > In vivo electrophysiology (S123, S124, S126, S127); Fig 2 legend (S200)

mean firing rates: mean firing rates; comparator: before — Results > Histamine leads to weaker and slower visual responses in the mouse lateral geniculate nucleus (S1, S9, S19)

Ciproxifan 12 mg/kg · Results > Histamine leads to weaker and slower visual responses in the mouse lateral geniculate nucleus (S1, S9, S19); Materials and methods > In vivo electrophysiology (S126, S127)

Total Sleep Amount in Male Wild-Type Mice

Animal study · C57BL/6J male wildtype (WT); mice (n = 7) [3]

Male wild-type mice received Ciproxifan or saline by intraperitoneal injection. No significant difference in total sleep amount was observed between treatments in the no light condition (p = 0.71).

Measured endpoints — not treatment concentrations
EndpointReported resultReference
total sleep amountReported result No significant difference in total sleep amount was observed between saline and ciproxifan treatments in the no light condition (Fig 3B) (p = 0.71; post hoc t test).[3]

Conditions shared by the study groups

Route
i.p
Treatment course
Twenty minutes before exposure no light or continuous light at ZT13
Vehicle
sterile saline
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ciproxifan 12mg/kginjection of saline with no light exposureNo significant difference in total sleep amount was observed between saline and ciproxifan treatments in the no light condition (Fig 3B) (p = 0.71; post hoc t test).[3]
Ciproxifan 12mg/kg
Model: C57BL/6J male wildtype (WT); mice (n = 7)
Methods and source locations

Compound reported in the paper: Ciproxifan

The paper names Ciproxifan without stating the salt or form; not verified as the maleate form supplied as A11117. No dose conversion or lot validation.

Materials and Methods > Animals (S1); Materials and Methods > Protocols > Experiment 3 (S29, S30); Results > Effects of ciproxifan on the acute induction of sleep early in the dark period (S60, S63); Fig 3 legend (S91)

total sleep amount: total sleep amount; comparator: injection of saline with no light exposure — Results > Effects of ciproxifan on the acute induction of sleep early in the dark period (S63)

Ciproxifan 12mg/kg · Results > Effects of ciproxifan on the acute induction of sleep early in the dark period (S63); Fig 3 legend (S91)

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 184025-19-2
Applications H3-receptor antagonist
Formula C20H22N2O6
Molecular Weight 386.4
SMILES
C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=C\C(=O)O)\C(=O)O

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 53 mg/mL (137.16 mM)
Water 1 mg/mL (2.58 mM)
Ethanol 53 mg/mL (137.16 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Hagenow S, Stasiak A, Ramsay RR, et al. Ciproxifan, a histamine H3 receptor antagonist, reversibly inhibits monoamine oxidase A and B. Sci Rep (2017). PMID: 28084411 DOI: 10.1038/srep40541 Source material
  2. [2] Tripodi M, Asari H. The central histaminergic system slows visual processing in the retina and lateral geniculate nucleus of awake mice. PLoS Biol (2025). PMID: 41187108 DOI: 10.1371/journal.pbio.3003406 Source material
  3. [3] Muindi F, Colas D, Ikeme J, et al. Loss of Melanopsin Photoreception and Antagonism of the Histamine H3 Receptor by Ciproxifan Inhibit Light-Induced Sleep in Mice. PLoS One (2015). PMID: 26083020 DOI: 10.1371/journal.pone.0128175 Source material

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