Ciproxifan hydrochloride
Ciproxifan (FUB 359) hydrochloride is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan hydrochloride displays low apparent affinity at other receptor subtypes. Ciproxifan hydrochloride can be used for the research of aging disorders and Alzheimer's disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1049741-81-2
- Fòrmula: C16H19ClN2O2
- Peso molecular:306.79
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas Histamine Receptor
More
Actividad biológica
Descripciòn
In Vitro
Ciproxifan hydrochloride inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM[1].
Ciproxifan hydrochloride (0.01 nM-1 μM; 60 min) inhibits the binding of [125I]iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Ciproxifan hydrochloride (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration was 0.25 sec instead of 0.50 sec[1].
Ciproxifan hydrochloride (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 hydrochloride (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[1].
Ciproxifan hydrochloride (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 1049741-81-2
-
Peso molecular 306.79
-
Fòrmula C16H19ClN2O2
-
SMILES
O=C(C1CC1)C(C=C2)=CC=C2OCCCC3=CN=CN3.[H]Cl
-
Synonyms
FUB-359 hydrochloride
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
-
Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureza y Documentación
Referencias
[1]. Ligneau X, et, al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther. 1998 Nov;287(2):658-66. [Content Brief]
[2]. Motawaj M, Arrang JM. Ciproxifan, a histamine H₃-receptor antagonist / inverse agonist, modulates methamphetamine-induced sensitization in mice. Eur J Neurosci. 2011 Apr;33(7):1197-204. [Content Brief]
[3]. Mark E Bardgett, et al. Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Neurobiol Learn Mem. 2011 Jan;95(1):64-72. [Content Brief]
[4]. Mark E Bardgett, et al. The H3 antagonist, ciproxifan, alleviates the memory impairment but enhances the motor effects of MK-801 (dizocilpine) in rats. Neuropharmacology. 2010 Nov;59(6):492-502. [Content Brief]
[5]. Mark Day, et al. Differential effects of ciproxifan and nicotine on impulsivity and attention measures in the 5-choice serial reaction time test. Biochem Pharmacol. 2007 Apr 15;73(8):1123-34. [Content Brief]
[6]. Catherine Pillot, et al. Ciproxifan, a histamine H3-receptor antagonist/inverse agonist, modulates the effects of methamphetamine on neuropeptide mRNA expression in rat striatum. Eur J Neurosci. 2003 Jan;17(2):307-14. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ciproxifan hydrochloride Related Classifications
HY-14567A Related Classifications
Powered by Bioz