Naloxone HCl 357-08-4

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Molecular Weight: 363.84 Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose.


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.


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.



Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	363.84
Formula	C19H21NO4.HCl
CAS No.	357-08-4

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	73 mg/mL (200.63 mM)
		Water	73 mg/mL (200.63 mM)
		Ethanol	<1 mg/mL (

Chemical Name	Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)-, hydrochloride (1:1), (5α)-

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Product Categories : Neuronal Signaling > Opioid Receptor Inhibitor