Compounds > nalorphine hydrochloride
Page last updated: 2024-12-11

nalorphine hydrochloride

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

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

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency11.88560.000811.382244.6684AID686978
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00200.00000.38458.6000AID151753
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00050.36496.9000AID149030
Mu-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00000.06470.9320AID149030
Kappa-type opioid receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00150.00040.00390.0180AID149030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1132896Toxicity in sc dosed mouse1977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

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
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.02

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.02 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.02)

All Compounds (24.57)

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%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		1.9510catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
meperidine
Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.		1.9610ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
meperidine hydrochloride
pethidine hydrochloride : The hydrochloride salt of pethidine. An analgesic used for the treatment of postoperative and labour pain.		2.3620hydrochlorideantispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
imipramine hydrochloride
[no description available]		1.9510hydrochlorideantidepressant
soterenol
soterenol: adrenergic beta-2 agonist used as bronchodilator; it has a number of gastrointestinal side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search ETHANOLAMINES (75-86); RN given refers to parent cpd without isomeric designation		1.9510
heart
[no description available]		1.9510
etorphine
[no description available]		1.9610alcohol;
morphinane alkaloid		opioid analgesic;
opioid receptor agonist;
sedative
codeine
[no description available]		1.9510morphinane alkaloid;
organic heteropentacyclic compound		antitussive;
drug allergen;
environmental contaminant;
opioid analgesic;
opioid receptor agonist;
prodrug;
xenobiotic
nalorphine
Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.		1.9610morphinane alkaloid
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		1.9610morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
oxycodone
Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain.		1.9510organic heteropentacyclic compound;
semisynthetic derivative		antitussive;
mu-opioid receptor agonist;
opioid analgesic
codeine phosphate
[no description available]		1.9510
dihydromorphine
Dihydromorphine: A semisynthetic analgesic used in the study of narcotic receptors.		1.9610morphinane alkaloid
naloxone hydrochloride
naloxone hydrochloride : A hydrochloride resulting from the formal reaction of equimolar amounts of naloxone and hydrogen chloride. A specific opioid antagonist, it is used to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		2.3620hydrochlorideantidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
morphine chloride
morphine hydrochloride : The hydrochloride salt of morphine.		2.6430hydrochloride
enkephalin, leucine-2-alanine
Enkephalin, Leucine-2-Alanine: A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate.		1.9610
morphine sulfate
[no description available]		3.0650alkaloid sulfate salt
ConditionIndicatedRelationship StrengthStudiesTrials
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		01.9510
Chemical Dependence
[description not available]		02.3520
Drug Withdrawal Symptoms
[description not available]		01.9510
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		01.9510
Substance-Related Disorders
Disorders related to substance use or abuse.		02.3520
Morphine Abuse
[description not available]		01.9510
Morphine Dependence
Strong dependence, both physiological and emotional, upon morphine.		01.9510