Ciproxifan

Bezeichnung:Ciproxifan

CAS-Nr184025-18-1

Englisch Name:Ciproxifan

CBNumberCB2503297

SummenformelC16H18N2O2

Molgewicht270.33

MOL-Datei184025-18-1.mol

Ciproxifan physikalisch-chemischer Eigenschaften

Siedepunkt	526.9±35.0 °C(Predicted)
Dichte	1.231
storage temp.	2-8°C
Löslichkeit	H₂O: insoluble
pka	14.54±0.10(Predicted)
Aggregatzustand	solid
Farbe	white

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36/37/38-43
S-Sätze:	26-36/37/39
WGK Germany	3

Gefahreninformationscode (GHS)

Ciproxifan Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R43:Sensibilisierung durch Hautkontakt möglich.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Definition
ChEBI: Cyclopropyl-[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone is an aromatic ketone.
Biologische Aktivität
ciproxifan is a novel and potent antagonist of histamine h3-receptor with a ic50 value of 9.2±1.8nm [1].ciproxifan has shown the in-vitro antagonistic action to h3-receptor with a ic50 value of 9.2±1.8nm. in addition, ciproxifan has been reported to competitively antagonize the (r) α-meha induced relaxation of electrically stimulated guinea pig ileum longitudinal muscle. besides, ciproxifan has been revealed to have the effect on [125i]iodoproxyfan binding with a ki value of 0.7±0.2 nm. apart from these, ciproxifan has been found to be a selective antagonist with pki values of 9.3, 4.9, 4.6, 5.5, 5.4, 4.9, <5.0, 4.8, <5.5 and <5.7 for h3, h2, h1, muscarinic m3, adrenergic α1d, β1, serotonin 5-ht1b, 5-ht2a, 5-ht3 and 5-ht4, respectively [1].
in vitro
Ciproxifan inhibits [³H]HA release from synaptosomes with K_i of 0.5 nM. It inhibits the binding of [¹²⁵I]iodoproxyfan at the brain H3 receptor with K_i of 0.7 nM. It 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 α_1D and β_{1, serotonin 5-HT_1B, 5-HT_2A, 5-HT₃ and 5-HT₄ >).}
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 13 min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, po) 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. It 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. It (3 mg/kg, ip) significantly increased choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, po) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. Ciproxifan (10 mg/kg ip) enhances prepulse inhibition in the DBA/2 strain mice. It (3 mg/kg ip) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Ciproxifan (3 mg/kg ip) improves accuracy and decreased impulsivity in adult male hooded Lister rats.
Einzelnachweise
[1] ligneau x1, lin j, vanni-mercier g, jouvet m, muir jl, ganellin cr, stark h, elz s, schunack w, schwartz j. neurochemical and behavioral effects of ciproxifan, a potent histamine h3-receptor antagonist. j pharmacol exp ther. 1998 nov; 287(2):658-66.

Ciproxifan Upstream-Materialien And Downstream Produkte

Ciproxifan Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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