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Naloxonazine dihydrochloride

Names

[ CAS No. ]:
82824-01-9

[ Name ]:
Naloxonazine dihydrochloride

[Synonym ]:
NALOXONAZINE DIHYDROCHLORIDE OPIOID ANTA GONIST
NALOXONAZINE DIHYDROCHLORIDE
NALOXONAZINE 2HCL
naloxonazine

Biological Activity

[Description]:

Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function[1].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[In Vitro]

Naloxonazine(0-50 μM, 24-72 h) 对细胞内 Leishmania donovani 的无鞭毛体阶段具有抑制活性，其最大抑制浓度 GI50为3.45 μM。而对 THP-1 宿主细胞的 GI50为 34 μM[1]。 Naloxonazine(10 μM, 4-72 h)可以抑制寄生虫细胞内生长，处理 24 h 可以抑制 70%，处理 72 h可以抑制 95%[1]。 Naloxonazine(10 μM, 4 or 24-72 h)导致 vATPase亚基 (ATP6V0C和TCIRG1) 和肌动蛋白 (ACTB) 基因及蛋白表达水平上调，并且影响了宿主细胞的细胞内酸性区室[1]。

[In Vivo]

Naloxonazine (0-15 mg/kg, i.p., 20 h)在雄性 Wistar大鼠中，当剂量为 15 mg/kg 时，(olfactory discriminative stimulus)S+/CS+ 相关反应显著降低约 55%，由 14.63 降至 6.82。而在(olfactory stimulus)S-/CS-刺激条件下观察到更大的行为抑制，反应率降低 66%，从 9.00 降至 3.00[2]。

[References]

[1]. Géraldine De Muylder, et al. Naloxonazine, an Amastigote-Specific Compound, Affects Leishmania Parasites through Modulation of Host-Encoded Functions. PLoS Negl Trop Dis. 2016 Dec 30;10(12):e0005234.   

[2]. Roberto Ciccocioppo, et al.  Effect of selective blockade of mu(1) or delta opioid receptors on reinstatement of alcohol-seeking behavior by drug-associated stimuli in rats. Neuropsychopharmacology. 2002 Sep;27(3):391-9.   

Chemical & Physical Properties

[ Density]:
1.12g/cm3

[ Boiling Point ]:
433.7ºC at 760 mmHg

[ Molecular Formula ]:
C38H42N4O6

[ Molecular Weight ]:
650.76300

[ Flash Point ]:
216.1ºC

[ Exact Mass ]:
650.31000

[ PSA ]:
130.58000

[ LogP ]:
3.15100

[ Index of Refraction ]:
1.612

Safety Information

[ WGK Germany ]:
3

Related Compounds