<Suppliers Price>

Naloxonazine dihydrochloride

Names

[ CAS No. ]:
880759-65-9

[ Name ]:
Naloxonazine dihydrochloride

[Synonym ]:
NALOXONAZINE DIHYDROCHLORIDE HYDRATE
NALOXONAZINE DIHYDROCHLORIDE OPIOID ANTA GONIST
Naloxonazine dihydrochloride
Demethylasterriquinone B1

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C38H43ClN4O6

[ Molecular Weight ]:
687.22400

[ Exact Mass ]:
686.28700

[ PSA ]:
130.58000

[ LogP ]:
3.95300

Related Compounds