product name Naloxone HCl
Description: Naloxone HCl is an inverse opioid agonist drug used to counteract the effects of opiate overdose. Naloxone is useful both in acute opioid overdose and in reducing respiratory or mental depression due to opioids. It is included as a part of emergency overdose response kits distributed to heroin and other opioid drug users, and this has been shown to reduce rates of deaths due to overdose. Naloxone cannot be absorbed via the GI tract, so it is commonly combined with a number of oral opioid preparations, including buprenorphine and pentazocine.
References: J Pharmacol Exp Ther. 2000 May;293(2):607-17; Psychopharmacology (Berl). 1999 Mar;142(3):302-8.
363.84
Formula
C19H21NO4.HCl
CAS No.
357-08-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (200.6 mM)
Water: 73 mg/mL (200.6 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Naloxone significantly reduces the LPS-induced degeneration of the midbrain neurons. Naloxone inactives stereoisomer (+)-naloxone protected the dopaminergic neurons with equal potency. Naloxone inhibits LPS-induced activation of microglia and release of proinflammatory factors, and inhibition of microglia generation of superoxide free radical best correlated with the neuroprotective effect of naloxone isomers. Naloxone is found to partially inhibit the binding of [(3)H]LPS to cell membranes, whereas it failes to prevent damage to dopaminergic neurons by peroxynitrite, a product of nitric oxide and superoxide. Naloxone (18.0 mg/kg) suppresses water intake when water is presented as the sole source of fluid. Naloxone produces a dose-dependent decrease in ethanol consumption, without altering water intake, when rats are given a free-choice between the ethanol solution and water. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Naloxone (10 mg/kg) causes a dose-dependent reduction of break-points and locomotor activity in both the beer and near-beer rats. Naloxone inhibits the LPS-induced activation of microglia and significantly reduces the LPS-induced loss of dopaminergic neurons in the rat substantia nigral. Naloxone abolishes this antinociceptive activity both in the hot-plate test and in the first phase of the formalin test without affecting the serum concentration of paracetamol. Naloxone prevents the increase in 5-HT concentration in the central nervous system and the reduction in 5-HT2 receptors in cortical membranes. |
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| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2000 May;293(2):607-17; Psychopharmacology (Berl). 1999 Mar;142(3):302-8. |
