EFAROXAN HYDROCHLORIDE Struktur

EFAROXAN HYDROCHLORIDE

Bezeichnung:EFAROXAN HYDROCHLORIDE

CAS-Nr89197-00-2

Englisch Name:EFAROXAN HYDROCHLORIDE

CBNumberCB9376896

SummenformelC13H17ClN2O

Molgewicht252.74

MOL-Datei89197-00-2.mol

EFAROXAN HYDROCHLORIDE physikalisch-chemischer Eigenschaften

storage temp.	Store at RT
Löslichkeit	H₂O: 300 mg/mL
Aggregatzustand	solid
Farbe	White
Wasserlöslichkeit	Soluble to 100 mM in water
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20° for up to 1 month.

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	7-35-45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3

Gefahreninformationscode (GHS)

EFAROXAN HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
S-Sätze Betriebsanweisung:
S7:Behälter dicht geschlossen halten.
S35:Abfälle und Behälter müssen in gesicherter Weise beseitigt werden.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
Efaroxan HCl (89197-00-2) is a selective α2-adrenergic receptor antagonist1 (selectivity ratio of α2/α1 = 724)4 and imidazoline receptor antagonist2. Induces release of insulin in the rat insulinoma cell line RIN-5AH by interaction with ATP-sensitive potassium channels independently from imidazoline I1 or I2 receptors.3 Efaroxan HCl increases resting plasma insulin levels and markedly potentiates the rise in insulin levels produced by adrenaline in the rat.4
Verwenden
Efaroxan Hydrochloride is a potent α2-AR adrenoceptor antagonist.
Biologische Aktivität
Potent, highly selective α 2 adrenoceptor antagonist and imidazoline I 1 receptor ligand (pK i values are 7.87, 7.42, 5.74, 7.28 and < 5 for α 2A , α 2B , α 2C , I 1 , and I 2 receptors respectively). Promotes insulin secretion, at a site distinct from I 1 or I 2 (the putative I 3 receptor) in vitro and in vivo .
Einzelnachweise
1) Chapleo et al. (1984), alpha-Adrenoceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoceptor activity; J.Med.Chem., 27 570 2) Eglen et al. (1998), ‘Seeing through a glass darkly’: casting light on imidazoline ‘I’ sites; Trends Pharmacol. Sci., 19 381 3) Olmos et al. (1994), Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors; Eur. .J. Pharmacol., 262 41 4) Berridge et al. (1992), Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats; Eur. J. Pharmacol., 213 205

EFAROXAN HYDROCHLORIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

89197-00-2, EFAROXAN HYDROCHLORIDE Verwandte Suche:

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