General
Preferred name
NALOXONE
Synonyms
NALOXONE HYDROCHLORIDE ()
Naloxone (hydrochloride) ()
Naloxone HCl ()
NALOXONE HYDROCHLORIDE DIHYDRATE ()
Naloxone (hydrochloride) ()
Naloxone-d5 (CRM) ()
Naloxoni hydrochloridum anhydrous ()
Evzio (autoinjector) ()
Anhydrous naloxone hydrochloride ()
Narcanti ()
Rivive ()
Prenoxad ()
Naloxone hydrochloride component of cassipa ()
NIH 7890 ()
Naloxone hydrochloride component of zubsolv ()
NSC-757109 ()
Narcan Neonatal ()
Naloxone hydrochloride component of targiniq ()
Naloxone hydrochloride anhydrous ()
EN-15304 ()
Naloxone hydrochloride component of suboxone ()
Evzio ()
Rezenopy ()
Naloxone hydrochloride (autoinjector) ()
Naloxone hydrochloride component of talwin nx ()
Zimhi ()
Rextovy ()
Narcan ()
Kloxxado ()
Naloxone hydrochloride component of bunavail ()
Narconil ()
Naloxoni hydrochloridum dihydrate ()
Nyxoid ()
Naloxone chlorhydrate ()
Naloxone hydrochloride dihydrate component of bunavail ()
Naloxone hydrochloride dihydrate component of cassipa ()
[3H]naloxone ()
Dbl naloxone ()
Naloxona ()
NSC-70413 ()
Naloxone ()
Naloxone-d5 ()
P&D ID
PD009757
CAS
357-08-4
465-65-6
1261079-38-2
Tags
available
drug
Approved by
EMA
FDA
First approval
2017
1971
Drug indication
Pruritus
Opioid dependence
Epilepsy
Respiratory depression
Narcotic depression
Drug Status
vet_approved
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias[1].
ABSORPTION Tmax:; 0.4mg IM injection = 0.38 hr; Nasal spray (one 2mg spray) = 0.33 hr; Nasal spray (one 4mg spray) = 0.50 hr ; ; Cmax:; 0.4mg IM injection = 0.88 ng/mL; Nasal spray (one 2mg spray) = 2.91 ng/mL; Nasal spray (one 4mg spray) = 4.83 ng/mL
TOXICITY LD50, IV administration, mouse = 150 ± 5 mg/kg;; LD50, IV administration, rat = 109 ± 4 mg/kg; ;
HALF-LIFE 0.4mg IM injection = 1.24 hr; Nasal spray (one 2mg spray) = 1.85 hr; Nasal spray (one 4mg spray) = 2.08 hr;
DESCRIPTION Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias[1].
DESCRIPTION 5-HT release inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Broad spectrum opioid antagonist (Tocriscreen Total)
Cell lines
0
Organisms
2
Compound Sets
26
Axon Medchem Screening Library
Cayman Chemical Bioactives
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Total
External IDs
85
Properties
(calculated by RDKit )
Molecular Weight
327.15
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
5
Aromatic Ring Count
1
cLogP
1.3
TPSA
70.0
Fraction CSP3
0.53
Chiral centers
4.0
Largest ring
6.0
QED
0.8
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Primary Target
Miscellaneous Opioids
MOA
Antagonist
Opioid Receptor antagonist
Target
CREB1, ESR1, OPRD1, OPRK1, OPRM1, TLR4
Opioid antagonist
Opioid Receptor
Indication
respiratory depression
Therapeutic Class
Antinarcotic Agents
Pathway
GPCR/G protein
Neuronal Signaling
Source data