Naloxone

Names

[ CAS No. ]:
465-65-6

[ Name ]:
Naloxone

[Synonym ]:
[14C]-Naloxone
[3H]-Naloxone
Narcanti
Nalone
Naloxonum
EN 1530 base
(4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one
Narcon
l-Naloxone
Narcan
n-Allylnoroxymorphone
Naloxona

Biological Activity

[Description]:

Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

Research Areas >> Neurological Disease

[References]

[1]. van Dorp E, et al. Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32.

Chemical & Physical Properties

[ Density]:
1.43 g/cm3

[ Boiling Point ]:
532.8ºC at 760 mmHg

[ Melting Point ]:
184ºC

[ Molecular Formula ]:
C₁₉H₂₁NO₄

[ Molecular Weight ]:
327.37

[ Flash Point ]:
276.1ºC

[ Exact Mass ]:
327.14700

[ PSA ]:
70.00000

[ LogP ]:
1.23930

[ Storage condition ]:
2-8°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QD2260000

CHEMICAL NAME :: Morphinan-6-one, 4,5-alpha-epoxy-3,14-dihydroxy-17-(2-propenyl)-

CAS REGISTRY NUMBER :: 465-65-6

LAST UPDATED :: 199806

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C19-H21-N-O4

MOLECULAR WEIGHT :: 327.41

WISWESSER LINE NOTATION :: T B6566 B6/CO 4ABBC R BX FV HO PN GHT&&TTJ CQ JQ P2U1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 260 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 30 mg/kg

SEX/DURATION :: female 16-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - gastrointestinal system Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 500 ug/kg

SEX/DURATION :: female 17-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Human Cells - not otherwise specified

DOSE/DURATION :: 120 umol/L/24H

REFERENCE :: JJCREP Japanese Journal of Cancer Research. (Elsevier Science Pub. BV, POB 211, 1000 AE Amsterdam, Netherlands) V.76- 1985- Volume(issue)/page/year: 78,519,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4324 No. of Facilities: 14 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 306 (estimated) No. of Female Employees: 121 (estimated)

Safety Information

[ Symbol ]:

GHS02, GHS06, GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H225-H301 + H311 + H331-H370

[ Precautionary Statements ]:
P210-P260-P280-P301 + P310-P311

[ Hazard Codes ]:
F,T

[ Risk Phrases ]:
11-23/24/25-39/23/24/25

[ Safety Phrases ]:
7-16-36/37-45

[ RIDADR ]:
UN1230 - class 3 - PG 2 - Methanol, solution

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Morphine-induced internalization of the L83I mutant of the rat μ-opioid receptor.

Br. J. Pharmacol. 172(2) , 593-605, (2014)

Naturally occurring single-nucleotide polymorphisms (SNPs) within GPCRs can result in alterations in various pharmacological parameters. Understanding the regulation and function of endocytic traffick...

Sympathetic activity induced by naloxone-precipitated morphine withdrawal is blocked in genetically engineered mice lacking functional CRF1 receptor.

Toxicol. Appl. Pharmacol. 283(1) , 42-9, (2015)

There is large body evidence indicating that stress can lead to cardiovascular disease. However, the exact brain areas and the mechanisms involved remain to be revealed. Here, we performed a series of...

Involvement of neurotransmitters in the action of the nociceptin/orphanin FQ peptide-receptor system on passive avoidance learning in rats.

Neurochem. Res. 39(8) , 1477-83, (2014)

The nociceptin/orphanin FQ peptide (NOP) receptor and its endogenous ligand plays role in several physiologic functions of the central nervous system, including pain, locomotion, anxiety and depressio...