AMG 9810 Struktur

AMG 9810

Bezeichnung:AMG 9810

CAS-Nr545395-94-6

Englisch Name:AMG 9810

CBNumberCB0306302

SummenformelC21H23NO3

Molgewicht337.41

MOL-Datei545395-94-6.mol

AMG 9810 physikalisch-chemischer Eigenschaften

Siedepunkt	512.5±50.0 °C(Predicted)
Dichte	1.175±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: >5mg/mL
pka	12.22±0.20(Predicted)
Aggregatzustand	powder
Farbe	white to beige

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3

Gefahreninformationscode (GHS)

AMG 9810 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
Beschreibung
AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC₅₀s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC₅₀s = 92.7 and 294 nM for human and rat, respectively), heat (IC₅₀s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC₅₀s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.
Verwenden
AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.[Cayman Chemical]
Definition
ChEBI: 3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-propenamide is a member of cinnamamides and a secondary carboxamide.
Biologische Aktivität
AMG 9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC 50 = 17 nM). Inhibits capsaicin-, proton-, heat- and endogenous ligand-induced activation of human and rat recombinant TRPV1 receptors. Displays antihyperalgesic properties in a rat model of inflammatory pain.
Biochem/physiol Actions
AMG 9810?is the cinnamide TRPV1 (vanilloid receptor 1) antagonist, that can prevent eye wiping behavior, stimulated by capsaicin and can inverse hyperalgesia in an animal model of inflammatory pain. It possesses antihyperalgesic properties.
Lager
+4°C (desiccate)
Einzelnachweise
[1]. gavva nr, tamir r, qu y, et al. amg 9810 [(e)-3-(4-t-butylphenyl)-n-(2, 3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (trpv1) antagonist with antihyperalgesic properties. j pharmacol exp ther, 2005, 313(1):474-84.

AMG 9810 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

545395-94-6, AMG 9810 Verwandte Suche:

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