880759-65-9

880759-65-9 structure

Name: Naloxonazine dihydrochloride
Chemical Name: Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, [(5α)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-ylidene]hydrazone, dihydrochloride, (5α)
CAS Number: 880759-65-9
Molecular Formula: C₃₈H₄₃ClN₄O₆
Molecular Weight: 687.22400
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2016-02-19 06:38:03
Modify Date: 2024-04-01 18:49:59
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3].

Name	Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, [(5α)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-ylidene]hydrazone, dihydrochloride, (5α)
Synonyms	NALOXONAZINE DIHYDROCHLORIDE HYDRATE NALOXONAZINE DIHYDROCHLORIDE OPIOID ANTA GONIST Naloxonazine dihydrochloride Demethylasterriquinone B1

Description	Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3].
Related Catalog	Research Areas >> Infection Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
Target	μ-opioid receptor:5.4 nM (IC50)
In Vitro	Naloxonazine is relatively stable in solution[2]. Naloxonazine (72 h) is active against the intracellular amastigote stage of Leishmania donovani with a half maximal inhibitory concentration (GI50) of 3.45 μM[3]. Naloxonazine (10 μM; 0-72 h) is active at early stages of Leishmania donovani infection[3]. Naloxonazine affects acidic compartments of the host cell which in turn limit L. donovani intracellular growth[3].
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.
References	[1]. Chien CC, et al. Naloxonazine, a specific mu-opioid receptor antagonist, attenuates the increment of locomotor activity induced by acute methamphetamine in mice. Toxicol Lett. 2012 Jul 7;212(1):61-5. [2]. Hahn EF, et al. Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites. Life Sci. 1982 Sep 20-27;31(12-13):1385-8. [3]. De Muylder G, 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.

Molecular Formula	C₃₈H₄₃ClN₄O₆
Molecular Weight	687.22400
Exact Mass	686.28700
PSA	130.58000
LogP	3.95300

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