Naloxone hydrochloride dihydrate Chemical Properties

Melting point:

182 °C (dec.)(lit.)

storage temp. 

2-8°C

solubility 

ethanol: 3.3 mg/mL stable for several months refrigerated if protected from light.

form 

powder

color 

white to off-white

optical activity

[α]25/D 178.6°, c = 2.5 in H2O(lit.)

Merck 

13,6388

BRN 

6260807

CAS DataBase Reference

51481-60-8(CAS DataBase Reference)

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

22-24/25-26-36/37/39-36

WGK Germany 

3

Naloxone hydrochloride dihydrate Usage And Synthesis

Chemical Properties

White or almost white, hygroscopic, crystalline powder.

Uses

Naloxone Hydrochloride Dihydrate is a specific opioid antagonist. Narcotic antagonist.

Uses

Antagonist (to narcotics).

brand name

Narcan (Bristol-Myers Squibb); Narcan (Endo).

Biochem/physiol Actions

Competitive antagonist for μ, κ, δ, and σ opioid receptors; blocks the action of σ-agonists at opioid sites. Naloxone′s antagonistic effect last for about 45 min and thus, requires repeated dosage. It results in critical side effects such as pulmonary edema.

Purification Methods

This opiate antagonist has been recrystallised from EtOH/Et2O or H2O. It is soluble in H2O (5%) and EtOH but insoluble in Et2O. The free base has m 184o (177-178o also reported) after recrystallisation from EtOAc, and [] D -194.5o (c 0.93, CHCl3). [Olofson et al. Tetrahedron Lett 1567 1977, Gold et al. Med Res Rev 2 211 1982.]

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