Naloxonazine dihydrochloride

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CAS NO:	880759-65-9
包装:	5mg
市场价:	1900元

Naloxonazine dihydrochloride 是一种特异性的μ-opioid receptor拮抗剂，IC₅₀为 5.4 nM。Naloxonazine dihydrochloride 也具有抗利什曼原虫活性。

生物活性

Naloxonazine dihydrochloride is a specificμ-opioid receptorantagonist with anIC₅₀of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity^[1]^[2]^[3].

IC₅₀& Target

μ Opioid Receptor/MOR

5.4 nM (IC₅₀)

体外研究
(In Vitro)

Naloxonazine is relatively stable in solution^[2].
Naloxonazine (72 h) is active against the intracellular amastigote stage ofLeishmania donovaniwith a half maximal inhibitory concentration (GI₅₀) of 3.45 μM^[3].
Naloxonazine (10 μM; 0-72 h) is active at early stages ofLeishmania donovaniinfection^[3].
Naloxonazine affects acidic compartments of the host cell which in turn limitL. donovaniintracellular growth^[3].

体内研究
(In Vivo)

Naloxonazine (20 mg/kg; i.p.; once) attenuates the increment of locomotor activity induced by acute methamphetamine in mice^[1]

Animal Model:	Male ICR mice, methamphetamine (METH)-induced locomotor activity model^[1]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection, once, 60 min before injecting saline (i.p.) or METH (1 mg/kg, i.p.)
Result:	Significantly attenuated the acute METH-induced increase in locomotor activity and phosphor-Thr75 DARPP-32 levels.

分子量

723.69

性状

Solid

Formula

C₃₈H₄₄Cl₂N₄O₆

CAS 号

880759-65-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)