Nepicastat hydrochloride

Bezeichnung:Nepicastat hydrochloride

CAS-Nr170151-24-3

Englisch Name:Nepicastat hydrochloride

CBNumberCB22611129

SummenformelC14H16ClF2N3S

Molgewicht331.81

MOL-Datei170151-24-3.mol

Nepicastat hydrochloride physikalisch-chemischer Eigenschaften

storage temp.	Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	DMSO: soluble10mg/mL, clear
Aggregatzustand	powder
Farbe	white to beige
InChIKey	DIPDUAJWNBEVOY-PPHPATTJSA-N

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3

Gefahreninformationscode (GHS)

Nepicastat hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Nepicastat is an inhibitor of dopamine β-hydroxylase (DBH; IC₅₀ = 9 nM for the purified human enzyme). It is selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC₅₀s or K_is = >10 μM). Nepicastat dose-dependently reduces norepinephrine content and increases dopamine content in the mesenteric artery, left ventricle, and cerebral cortex in spontaneously hypertensive rats, as well as in the renal artery, left ventricle, and cerebral cortex in beagle dogs. It attenuates increases in diastolic blood pressure and heart rate induced by preganglionic sympathetic nerve stimulation in pithed spontaneously hypertensive rats when administered orally at doses of 10 and 30 mg/kg. Nepicatstat (50 mg/kg) reduces the progressive ratio response for cocaine, but not food or sucrose pellets, in rats. It also reduces reinstatement of cocaine-seeking behavior induced by cues, yohimbine , or foot-shock in rats.
Verwenden
Nepicastat Hydrochloride is a potent and selective dopamine β-hydrolase inhibitor. Used in cardiovascular treatment where deficiencies in ventricles results in heart failure.
Lager
Store at -20°C
Einzelnachweise
[1]. stanley wc, li b, bonhaus dw, et al. catecholamine modulatory effects of nepicastat (rs-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. br j pharmacol, 1997, 121(8): 1803-1809.
[2]. stanley wc, lee k, johnson lg, et al. cardiovascular effects of nepicastat (rs-25560-197), a novel dopamine beta-hydroxylase inhibitor. j cardiovasc pharmacol, 1998, 31(6): 963-970.
[3]. devoto p, flore g, saba p, et al. the dopamine beta-hydroxylase inhibitor nepicastat increases dopamine release and potentiates psychostimulant-induced dopamine release in the prefrontal cortex. addict biol, 2014, 19(4): 612-622.

Nepicastat hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

170151-24-3, Nepicastat hydrochloride Verwandte Suche:

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