CAS 82824-01-9|Naloxonazine dihydrochloride

Introduction:Basic information about CAS 82824-01-9|Naloxonazine dihydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameNaloxonazine dihydrochloride
CAS Number82824-01-9Molecular Weight650.76300
Density1.12g/cm3Boiling Point433.7ºC at 760 mmHg
Molecular FormulaC38H42N4O6Melting Point/
MSDS/Flash Point216.1ºC

Names

NameNaloxonazine dihydrochloride,Bis-[5-α-4,5-Epoxy-3,14-dihydroxy-17-(2-propenyl)-morphinan-6-ylidene]hydrazinedihydrochloride
SynonymMore Synonyms

Naloxonazine dihydrochloride BiologicalActivity

DescriptionNaloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function[1].
Related CatalogResearch Areas >>InfectionSignaling Pathways >>GPCR/G Protein >>Opioid ReceptorSignaling Pathways >>Neuronal Signaling >>Opioid ReceptorResearch Areas >>Neurological Disease
In VitroNaloxonazine(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 VivoNaloxonazine (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

Density1.12g/cm3
Boiling Point433.7ºC at 760 mmHg
Molecular FormulaC38H42N4O6
Molecular Weight650.76300
Flash Point216.1ºC
Exact Mass650.31000
PSA130.58000
LogP3.15100
Index of Refraction1.612
InChIKeyAJPSBXJNFJCCBI-ACDAVLQGSA-N
SMILESC=CCN1CCC23c4c5ccc(O)c4OC2C(=NN=C2CCC4(O)C6Cc7ccc(O)c8c7C4(CCN6CC=C)C2O8)CCC3(O)C1C5

Safety Information

WGK Germany3

Synonyms

NALOXONAZINE DIHYDROCHLORIDE OPIOID ANTA GONIST
NALOXONAZINE DIHYDROCHLORIDE
NALOXONAZINE 2HCL
naloxonazine
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