Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H21NO3.ClH |
Molecular Weight | 347.836 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.[H][C@@]12OC3=C4C(C[C@H]5N(CC=C)CC[C@@]14[C@@]5([H])C=C[C@@H]2O)=CC=C3O
InChI
InChIKey=NAHATSPWSULUAA-ZQGPYOJVSA-N
InChI=1S/C19H21NO3.ClH/c1-2-8-20-9-7-19-12-4-6-15(22)18(19)23-17-14(21)5-3-11(16(17)19)10-13(12)20;/h2-6,12-13,15,18,21-22H,1,7-10H2;1H/t12-,13+,15-,18-,19-;/m0./s1
DescriptionSources: http://en.medicine-cure.com/ovr4_nalorfin.htmCurator's Comment: description was created based on several sources, including:
http://en.pharmacodia.com/web/drug/1_12280.html | https://www.ncbi.nlm.nih.gov/pubmed/16433932 | https://www.ncbi.nlm.nih.gov/pubmed/6301606 | doi:10.3181/00379727-77-18904
Sources: http://en.medicine-cure.com/ovr4_nalorfin.htm
Curator's Comment: description was created based on several sources, including:
http://en.pharmacodia.com/web/drug/1_12280.html | https://www.ncbi.nlm.nih.gov/pubmed/16433932 | https://www.ncbi.nlm.nih.gov/pubmed/6301606 | doi:10.3181/00379727-77-18904
Nalorphine has a mixed opioid agonist-antagonist properties. Nalorphine inhibits the cholinesterases of mouse brain, bovine erythrocytes and horse serum. It acts on mu-, k- and sigma-opioid receptors. Nalorfin by virtue of the agonistic effect has an analgesic effect but to a much lesser extent than morphine. Initially, before the appearance of a "pure" morphine-naloxone antagonist, nalorphine was used as an antidote for severe respiratory depression and other body function disorders caused by acute poisoning in case of an overdose of morphine, promedol, fentanyl or other narcotic analgesics, or with increased sensitivity to them. At present, nalorphine is practically not used for this purpose. It was replaced by naloxone. Large doses of nalorphine can cause nausea, cramps, drowsiness, headache, mental stimulation.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3198 Sources: doi: 10.3181/00379727-77-18904 |
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Target ID: CHEMBL4329 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16433932 |
1.6 nM [Ki] | ||
Target ID: CHEMBL270 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8819494 |
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Target ID: CHEMBL3602 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6301606 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | Norfin Approved UseIt is used as an antidote for opiates. |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.12 μg/g |
2 mg/kg single, subcutaneous dose: 2 mg/kg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
NALORPHINE unknown | Canis lupus population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.17 μg × h/g |
2 mg/kg single, subcutaneous dose: 2 mg/kg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
NALORPHINE unknown | Canis lupus population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
23 min |
2 mg/kg single, subcutaneous dose: 2 mg/kg route of administration: Subcutaneous experiment type: SINGLE co-administered: |
NALORPHINE unknown | Canis lupus population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Sample Use Guides
In Vivo Use Guide
Sources: http://en.medicine-cure.com/ovr4_nalorfin.htm
Adults appoint 0,005 - 0,01 g (1 - 2 ml of a 0.5% solution). If the effect is insufficient, the injections are repeated at intervals of 10 to 15 minutes. The total dose should not exceed 0.04 g (8 ml of 0.5% solution).
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8819494
Maximum stimulation of [35S]GTPyS binding by Nalorphine using a single saturating concentration of ligand (10 uM) was compared with stimulation by DAAMGO (10 uM). Intrinsic activity determined for Nalorphine in C6 glioma cells was 9%.
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NCI_THESAURUS |
C67413
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CFR |
21 CFR 522.1452
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SUB03381MIG
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CHEMBL415284
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C76849
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5484366
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ACTIVE MOIETY
SUBSTANCE RECORD