Compounds > nalorphine hydrochloride
Page last updated: 2024-08-01 19:52:39

nalorphine hydrochloride

Description

Cross-References

ID SourceID
PubMed CID5484366
CHEMBL ID1908349
SCHEMBL ID149571
MeSH IDM0330061

Synonyms (39)

Synonym
miromorfalil
17-allyl-7,8-didehydro-4,5alpha-epoxymorphinan-3,6alpha-diol hydrochloride
morphinan-3,6-alpha-diol, 17-allyl-7,8-didehydro-4,5-alpha-epoxy-, hydrochloride
einecs 200-321-8
normorphine, n-allyl-, hydrochloride
n-allylnormorphine hydrochloride
morphinan-3,6-diol, 7,8-didehydro-4,5-epoxy-17-(2-propenyl)-(5alpha,6alpha)-, hydrochloride
nalorphine hydrochloride
allylmorphine hydrochloride
n-allyl-2,12-dihydroxy-1,11-epoxymorphinene-13 hydrochloride
cloridrato de nalorfina (tn)
nalline [veterinary] (tn)
57-29-4
D08248
nalorphine hydrochloride (usp)
dtxcid3027825
cas-57-29-4
dtxsid3047847 ,
tox21_112614
unii-9fpe56z2tw
9fpe56z2tw ,
nalorphine hcl
nalorphine hydrochloride [usp]
nalorphine hydrochloride ciii
CHEMBL1908349
nalorphine hydrochloride [who-dd]
nalorphine hydrochloride [usp monograph]
nalorphine hydrochloride [green book]
nalorphine hydrochloride [mart.]
morphinan-3,6-diol, 7,8-didehydro-4,5-epoxy-17-(2-propenyl)-(5.alpha.,6.alpha.)-, hydrochloride
nalorphine hydrochloride [mi]
nalorphine hydrochloride ciii [usp-rs]
SCHEMBL149571
nalorphine hydrochloride 1.0 mg/ml in methanol (as free base)
(4r,4ar,7s,7ar,12bs)-3-prop-2-enyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-7,9-diol;hydrochloride
nalorphinehydrochlorideciii(250mg)
Q27272499
nalorphine.hcl, 1mg/ml in methanol
nalorphine.hcl

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency11.8856AID686978

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.0020AID151753

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Delta-type opioid receptorRattus norvegicus (Norway rat)EC500.0015AID149030
Mu-type opioid receptorRattus norvegicus (Norway rat)EC500.0015AID149030
Kappa-type opioid receptorRattus norvegicus (Norway rat)EC500.0015AID149030

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1132896Toxicity in sc dosed mouse1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1123214Binding affinity to opioid receptor in rat brain homogenates1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
ISSN: 0022-2623		Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions.
AID1147932Analgesic activity in sc dosed rat by tail flick test1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
ISSN: 0022-2623		Adrenergic sulfonanilides. 4. Centrally active beta-adrenergic agonists.
AID149030Displacement of [3H]dalamid ([D-Ala2,Met5] enkephalinamide) from opioid receptors of rat brain membrane1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
ISSN: 0022-2623		Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry
AID1147931Analgesic activity in sc dosed mouse assessed as reduction in phenylalanine-induced writhing1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
ISSN: 0022-2623		Adrenergic sulfonanilides. 4. Centrally active beta-adrenergic agonists.
AID124938Compound administered subcutaneously was evaluated for Opioid antagonist activity versus morphine by tail flick antagonism test in mice 95% confidence limits are in brackets1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
ISSN: 0022-2623		Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
AID151753Compound administered subcutaneously was evaluated for inhibition constant measured as the displacement of [3H]DAGO from rat brain1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
ISSN: 0022-2623		Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
AID177917Analgesic agonist activity by mouse acetylcholine writhing test through subcutaneous administration1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
ISSN: 0022-2623		Synthesis and antinociceptive activity of 4-(cyclopropylmethyl)-3,4,5,6-tetrahydro-2H-1,5-methano-1, 4-benzodiazocin-9-amine and congeners.
AID1149072Analgesic activity in sc dosed mouse by Nilsen assay1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
ISSN: 0022-2623		Optical resolution of (+/-)-2,5-dimethyl-2'-hydroxy-9alpha- and -9beta-propyl-6,7-benzomorphans and their pharmacological properties.
AID108529Analgesic antagonistic activity in mice using morphine(56.07 umol/kg) induced Straub-tail test after sc administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
ISSN: 0022-2623		N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID122577Compound administered subcutaneously was evaluated for antinociceptive activity determined by hot plate test in mice1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
ISSN: 0022-2623		Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
AID112670In vivo antagonist/agonist nature after subcutaneous administration using hot plate assay1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
ISSN: 0022-2623		Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry
AID1132897Agonist activity at opioid receptor in myenteric plexus of guinea pig ileum relative to morphine1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1123213Antinociceptive activity in sc dosed mouse by Nilsen assay1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
ISSN: 0022-2623		Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions.
AID1132894Inhibition of morphine-induced analgesia in mouse by tail clip method1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1123212Antinociceptive activity in sc dosed mouse by hot-plate assay1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
ISSN: 0022-2623		Deoxymorphines: role of the phenolic hydroxyl in antinociception and opiate receptor interactions.
AID1132902Analgesic activity in sc dosed mouse at maximum tolerated dose by hot plate method1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1136988Narcotic antagonist activity in morphine-dependent rhesus monkey assessed as mild to severe abstinence1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
ISSN: 0022-2623		Azabicycloalkanes as analgetics. 3. Structure-activity relationships of 1-phenyl-6-azabicyclo[3.2.1]octanes and absolute stereochemistry of (+)-1-(3-hydroxyphenyl)-6-methyl-6-azabicyclo[3.2.1]octane and its 7-endo-methyl derivative.
AID169763In vivo narcotic antagonist activity in rat after subcutaneous administration of the compound1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
ISSN: 0022-2623		Synthesis and antinociceptive activity of 4-(cyclopropylmethyl)-3,4,5,6-tetrahydro-2H-1,5-methano-1, 4-benzodiazocin-9-amine and congeners.
AID1132901Analgesic activity in sc dosed mouse at maximum tolerated dose by tail clip method1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID122576Antinociceptive activity was determined by tail flick test in mice after subcutaneous administration; IA means inactive at 1,10 or 30.0 mg/kg1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
ISSN: 0022-2623		Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
AID1132895Toxicity in mouse assessed as Straub tail activity1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID112666In vivo antagonist/agonist nature after subcutaneous administration to mice using tail flick (TF) antagonist assay vs. morphine1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
ISSN: 0022-2623		Probes for narcotic receptor mediated phenomena. 13. Potential irreversible narcotic antagonist-based ligands derived from 6,14-endo-ethenotetrahydronororipavine with 7-(methoxyfumaroyl)amino, (bromoacetyl)amino, or isothiocyanate electrophiles: chemistry
AID1149071Analgesic activity in sc dosed mouse by Eddy hot-plate assay1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
ISSN: 0022-2623		Optical resolution of (+/-)-2,5-dimethyl-2'-hydroxy-9alpha- and -9beta-propyl-6,7-benzomorphans and their pharmacological properties.
AID1149073Physical dependence capacity in monkey assessed as single dose suppression of morphine withdrawal syndrome at 1.5 to 6 mg/kg1976Journal of medicinal chemistry, Mar, Volume: 19, Issue:3
ISSN: 0022-2623		Optical resolution of (+/-)-2,5-dimethyl-2'-hydroxy-9alpha- and -9beta-propyl-6,7-benzomorphans and their pharmacological properties.
AID128033Compound was tested for analgesic activity in mouse using mouse writhing test following subcutaneous administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
ISSN: 0022-2623		N-substituent modulation of opiate agonist/antagonist activity in resolved 3-methyl-3-(m-hydroxyphenyl)piperidines.
AID1136977Narcotic antagonist activity in iv dosed rabbit assessed as inhibition of morphine-induced respiratory depression1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
ISSN: 0022-2623		Azabicycloalkanes as analgetics. 3. Structure-activity relationships of 1-phenyl-6-azabicyclo[3.2.1]octanes and absolute stereochemistry of (+)-1-(3-hydroxyphenyl)-6-methyl-6-azabicyclo[3.2.1]octane and its 7-endo-methyl derivative.
AID1132893Analgesic activity in sc dosed mouse assessed as inhibition of phenylquinone-induced writhing1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID122578Compound administered subcutaneously was evaluated for antinociceptive activity determined by p-phenylquinone-writhing test in mice1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
ISSN: 0022-2623		Hexahydro-1H-1-pyrindines from acid rearrangement of 9-alkylidene-5-(m-methoxyphenyl)-2-methylmorphans. A new structural type of narcotic antagonists.
AID177919Analgesic agonist activity by rat intracarotid bradykinin writhing test through subcutaneous administration1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
ISSN: 0022-2623		Synthesis and antinociceptive activity of 4-(cyclopropylmethyl)-3,4,5,6-tetrahydro-2H-1,5-methano-1, 4-benzodiazocin-9-amine and congeners.
AID1132900Suppression of abstinence in withdrawn, morphine-dependent rhesus monkey1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1147948Antagonism of morphine-induced analgesia in sc dosed rat1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
ISSN: 0022-2623		Adrenergic sulfonanilides. 4. Centrally active beta-adrenergic agonists.
AID1132898Antagonist activity at opioid receptor in myenteric plexus of guinea pig ileum relative to nalorphine1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
ISSN: 0022-2623		Diastereoisomeric N-tetrahydrofurfurylnoroxymorphones with opioid agonist--antagonist properties.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560		Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (81.82)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's1 (9.09)24.3611
2020's1 (9.09)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
isoproterenol
1
catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent		1976197648.0low010000
meperidine
1
ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic		1986198638.0low010000
meperidine hydrochloride
2
hydrochlorideantispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic		1977198642.5high020000
imipramine hydrochloride
1
hydrochlorideantidepressant1976197648.0low010000
soterenol
1
1976197648.0medium010000
heart
1
1976197648.0high010000
etorphine
1
alcohol;
morphinane alkaloid		opioid analgesic;
opioid receptor agonist;
sedative		1986198638.0medium010000
codeine
1
morphinane alkaloid;
organic heteropentacyclic compound		antitussive;
drug allergen;
environmental contaminant;
opioid analgesic;
opioid receptor agonist;
prodrug;
xenobiotic		1976197648.0low010000
nalorphine
1
morphinane alkaloid1986198638.0low010000
naloxone
1
morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist		1986198638.0low010000
oxycodone
1
organic heteropentacyclic compound;
semisynthetic derivative		antitussive;
mu-opioid receptor agonist;
opioid analgesic		1976197648.0low010000
codeine phosphate
1
1977197747.0low010000
dihydromorphine
1
morphinane alkaloid1986198638.0low010000
naloxone hydrochloride
2
hydrochlorideantidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist		1977197747.0medium020000
morphine chloride
3
hydrochloride1976197747.3high030000
enkephalin, leucine-2-alanine
1
1986198638.0low010000
morphine sulfate
5
alkaloid sulfate salt1976198641.6high050000
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Chemical Dependence0
2
1976197747.5high020000
Drug Withdrawal Symptoms0
1
1977197747.0medium010000
Morphine Abuse0
1
1976197648.0medium010000
Morphine Dependence0
1
1976197648.0medium010000
Muscle Contraction0
1
1976197648.0medium010000
Substance Withdrawal Syndrome0
1
1977197747.0medium010000
Substance-Related Disorders0
2
1976197747.5high020000

Bioavailability (1)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019