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Identification
- Summary
Nalbuphine is an opioid agonist-antagonist used to treat pain, for pre and postoperative analgesia, and for analgesia in labor and delivery.
- Generic Name
- Nalbuphine
- DrugBank Accession Number
- DB00844
- Background
A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors. Nalbuphine is the only opioid analgesic that is not a controlled substance in the United States.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Nalbuphine (DB00844)
- Weight
- Average: 357.4434
Monoisotopic: 357.194008357 - Chemical Formula
- C21H27NO4
- Synonyms
- N-cyclobutylmethyl-4,5α-epoxy-3,6α,14-morphinantriol
- Nalbufina
- Nalbuphin
- Nalbuphine
- Nalbuphinum
- External IDs
- EN-2234 A
Pharmacology
- Indication
For the relief of moderate to severe pain.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Severe pain •••••••••••• Management of Moderate pain •••••••••••• Treatment of Obstetrical analgesia during labor and delivery therapy •••••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Nalbuphine is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Nalbuphine's analgesic potency is essentially equivalent to that of morphine on a milligram basis. The opoioid antagonist activity of nalbuphine is about one-fourth to that of nalorphine and 10 times to that of pentazocine. Nalbuphine by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e.g., morphine, oxymorphone, fentanyl), nalbuphine may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. Nalbuphine may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphine should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.
- Mechanism of action
The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Nalbuphine is thought primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with some binding to the delta receptor and minimal agonist activity at the sigma receptor.
Target Actions Organism AKappa-type opioid receptor agonistHumans AMu-type opioid receptor antagonistHumans ADelta-type opioid receptor antagonistHumans - Absorption
The mean absolute bioavailability was 81% and 83% for the 10 and 20 mg intramuscular doses, respectively, and 79% and 76% following 10 and 20 mg of subcutaneous nalbuphine. Clinical studies show that the duration of analgesic activity of the drug can range from 3 to 6 hours.
- Volume of distribution
Not Available
- Protein binding
Not appreciably bound.
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
The plasma half-life of nalbuphine is about 5 hours.
- Clearance
Not Available
- Adverse Effects
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Oral, acute LD50 is 1100 mg/kg in dog. Symptoms of overdose include primarily sleepiness and mild dysphoria.
- Pathways
Pathway Category Nalbuphine Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of adverse effects can be increased when Nalbuphine is combined with 1,2-Benzodiazepine. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Nalbuphine. Acetophenazine The risk or severity of hypotension and CNS depression can be increased when Acetophenazine is combined with Nalbuphine. Aclidinium The risk or severity of adverse effects can be increased when Aclidinium is combined with Nalbuphine. Agomelatine The risk or severity of CNS depression can be increased when Nalbuphine is combined with Agomelatine. - Food Interactions
- Avoid alcohol. Ingesting alcohol may increase the sedative and CNS depressant effects of nalbuphine.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Nalbuphine hydrochloride ZU4275277R 23277-43-2 YZLZPSJXMWGIFH-BCXQGASESA-N - International/Other Brands
- Mexifen (Medicus) / Nalbuphine (Mylan) / Nalpain (Orpha-Devel)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nubain Injection, solution 20 mg/1mL Intramuscular; Intravenous; Subcutaneous Endo Pharmaceuticals 1979-05-15 2006-11-30 US 
Nubain Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous Endo Pharmaceuticals 1979-05-15 2007-01-31 US Nubain Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous Physicians Total Care, Inc. 1979-05-15 2011-05-31 US Nubain Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous Endo Pharmaceuticals 1979-05-15 2006-03-31 US Nubain Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous Physicians Total Care, Inc. 1979-05-15 2011-05-31 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nalbuphine Hci Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous HF Acquisition Co LLC, DBA HealthFirst 2019-10-29 Not applicable US Nalbuphine Hci Injection, solution 20 mg/1mL Intramuscular; Intravenous; Subcutaneous HF Acquisition Co LLC, DBA HealthFirst 2019-10-29 Not applicable US Nalbuphine Hydrochloride Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous Hospira, Inc. 2005-07-19 Not applicable US Nalbuphine Hydrochloride Injection, solution 20 mg/1mL Intramuscular; Intravenous; Subcutaneous McKesson Corporation dba SKY Packaging 2004-12-31 Not applicable US Nalbuphine Hydrochloride Injection, solution 10 mg/1mL Intramuscular; Intravenous; Subcutaneous General Injectables & Vaccines, Inc 2010-03-01 2023-09-01 US
Categories
- ATC Codes
- N02AF02 — Nalbuphine
- Drug Categories
- Alkaloids
- Analgesics
- Central Nervous System Agents
- Central Nervous System Depressants
- Heterocyclic Compounds, Fused-Ring
- Mixed Agonist / Antagonist Opioids
- Morphinan Derivatives
- Morphinans
- Narcotics
- Nervous System
- Opiate Alkaloids
- Opiate Partial Agonists
- Opioid Agonist/Antagonist
- Opioid Antagonists
- Opioids
- Peripheral Nervous System Agents
- Phenanthrenes
- Semi-synthetic Opioids
- Sensory System Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenanthrenes and derivatives
- Sub Class
- Not Available
- Direct Parent
- Phenanthrenes and derivatives
- Alternative Parents
- Tetralins / Coumarans / 1-hydroxy-2-unsubstituted benzenoids / Alkyl aryl ethers / Aralkylamines / Piperidines / Tertiary alcohols / Trialkylamines / Secondary alcohols / 1,2-aminoalcohols show 6 more
- Substituents
- 1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / Alcohol / Alkyl aryl ether / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Coumaran / Cyclic alcohol show 17 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- organic heteropentacyclic compound (CHEBI:7454)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- L2T84IQI2K
- CAS number
- 20594-83-6
- InChI Key
- NETZHAKZCGBWSS-CEDHKZHLSA-N
- InChI
- InChI=1S/C21H27NO4/c23-14-5-4-13-10-16-21(25)7-6-15(24)19-20(21,17(13)18(14)26-19)8-9-22(16)11-12-2-1-3-12/h4-5,12,15-16,19,23-25H,1-3,6-11H2/t15-,16+,19-,20-,21+/m0/s1
- IUPAC Name
- (1S,5R,13R,14S,17S)-4-(cyclobutylmethyl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7,9,11(18)-triene-10,14,17-triol
- SMILES
- O[C@H]1CC[C@@]2(O)[C@H]3CC4=CC=C(O)C5=C4[C@@]2(CCN3CC2CCC2)[C@H]1O5
References
- Synthesis Reference
Michael R. Magruder, "Nalbuphine-narcotic analgesic composition and method of producing analgesia." U.S. Patent US4366159, issued August, 1981.
US4366159- General References
- Gear RW, Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD: The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain. Pain. 1999 Nov;83(2):339-45. [Article]
- FDA Approved Drug Products: NUBAIN (nalbuphine) injection, for intramuscular, subcutaneous, or intravenous use (December 2023) [Link]
- External Links
- Human Metabolome Database
- HMDB0014982
- KEGG Drug
- D08246
- KEGG Compound
- C07251
- PubChem Compound
- 5311304
- PubChem Substance
- 46507383
- ChemSpider
- 4470813
- BindingDB
- 50105085
- 7238
- ChEBI
- 7454
- ChEMBL
- CHEMBL895
- ZINC
- ZINC000003812989
- Therapeutic Targets Database
- DAP000380
- PharmGKB
- PA164745372
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Nalbuphine
- FDA label
- Download (51.4 KB)
- MSDS
- Download (74.4 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Diagnostic Conscious Sedation Failure During Procedure 1 somestatus stop reason just information to hide Not Available Completed Other Lower Abdominal Oncologic Surgery 1 somestatus stop reason just information to hide Not Available Completed Prevention Analgesia 1 somestatus stop reason just information to hide Not Available Completed Prevention Bariatric Surgery Candidates / Obesity, Morbid / Visceral Pain 1 somestatus stop reason just information to hide Not Available Completed Prevention Postoperative pain 3 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Barr Pharmaceuticals
- Bristol-Myers Squibb Co.
- Cardinal Health
- Dispensing Solutions
- Endo Pharmaceuticals Inc.
- Hospira Inc.
- Mckesson Corp.
- Neuman Distributors Inc.
- Physicians Total Care Inc.
- Quality Care
- Dosage Forms
Form Route Strength Solution Parenteral 10.00 mg Injection Intramuscular; Intravenous; Subcutaneous 10 mg/ml Solution Intravenous 10.000 mg Solution Intravenous 10 mg Injection, solution Parenteral 10 mg/ml Injection Intramuscular; Intravenous; Subcutaneous 10 mg/1mL Injection Intramuscular; Intravenous; Subcutaneous 20 mg/1mL Solution Parenteral 10.000 mg Injection, solution Intramuscular; Intravenous; Subcutaneous 10 mg/1mL Injection, solution Intramuscular; Intravenous; Subcutaneous 20 mg/1mL Solution Intramuscular; Intravenous; Subcutaneous 10 mg / mL Solution Intramuscular; Intravenous; Subcutaneous 20 mg / mL Injection, solution 10 mg/1ml - Prices
Unit description Cost Unit Nubain 20 mg/ml ampule 4.9USD ml Nubain 10 mg/ml vial 3.53USD ml Nalbuphine 20 mg/ml ampul 3.2USD ml Nalbuphine 200 mg/10 ml vial 2.66USD ml Nalbuphine 10 mg/ml ampul 1.46USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 230 °C as HCl salt Not Available water solubility 35.5 mg/mL at 25 °C as HCl salt Not Available logP 1.4 Not Available pKa 8.71 and 9.96 (hcl form) FDA Label - Predicted Properties
Property Value Source Water Solubility 2.09 mg/mL ALOGPS logP 2 ALOGPS logP 1.19 Chemaxon logS -2.2 ALOGPS pKa (Strongest Acidic) 10.39 Chemaxon pKa (Strongest Basic) 9.62 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 73.16 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 97 m3·mol-1 Chemaxon Polarizability 38.56 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.968 Blood Brain Barrier + 0.9642 Caco-2 permeable + 0.7337 P-glycoprotein substrate Substrate 0.8532 P-glycoprotein inhibitor I Non-inhibitor 0.8781 P-glycoprotein inhibitor II Non-inhibitor 0.8923 Renal organic cation transporter Inhibitor 0.5431 CYP450 2C9 substrate Non-substrate 0.8645 CYP450 2D6 substrate Substrate 0.5896 CYP450 3A4 substrate Substrate 0.5919 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9421 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9029 CYP450 3A4 inhibitor Non-inhibitor 0.93 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9562 Ames test Non AMES toxic 0.6897 Carcinogenicity Non-carcinogens 0.9598 Biodegradation Not ready biodegradable 0.9796 Rat acute toxicity 2.6502 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.747 hERG inhibition (predictor II) Non-inhibitor 0.8054
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-056u-9024000000-f340950b62bc62155aad Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0a4i-0009000000-82575d89aef2007c4242 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0009000000-55edbba9c6cdab4cf0dc Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-052f-0019000000-7bb213b7bf385e80b405 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0009000000-eedccc27d3bce60dc1eb Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4r-0009000000-d2c478c11987a85252a5 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0pbc-0019000000-9948aca7da89d8d5d1d0 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 191.0692712 predictedDarkChem Lite v0.1.0 [M-H]- 191.4669712 predictedDarkChem Lite v0.1.0 [M-H]- 180.80849 predictedDeepCCS 1.0 (2019) [M+H]+ 192.0832712 predictedDarkChem Lite v0.1.0 [M+H]+ 192.0452712 predictedDarkChem Lite v0.1.0 [M+H]+ 183.20406 predictedDeepCCS 1.0 (2019) [M+Na]+ 190.8232712 predictedDarkChem Lite v0.1.0 [M+Na]+ 189.40193 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled opioid receptor that functions as a receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as a receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions
- Specific Function
- dynorphin receptor activity
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Hoehe M, Duka T: Opiates increase plasma catecholamines in humans. Psychoneuroendocrinology. 1993;18(2):141-8. [Article]
- Chen SL, Huang EY, Chow LH, Tao PL: Dextromethorphan differentially affects opioid antinociception in rats. Br J Pharmacol. 2005 Feb;144(3):400-4. [Article]
- Tao PL, Liang KW, Sung WY, Wu YT, Huang EY: Nalbuphine is effective in decreasing the rewarding effect induced by morphine in rats. Drug Alcohol Depend. 2006 Sep 15;84(2):175-81. Epub 2006 Mar 6. [Article]
- Smith MA, Greene-Naples JL, Lyle MA, Iordanou JC, Felder JN: The effects of repeated opioid administration on locomotor activity: I. Opposing actions of mu and kappa receptors. J Pharmacol Exp Ther. 2009 Aug;330(2):468-75. doi: 10.1124/jpet.108.150011. Epub 2009 Apr 29. [Article]
- Mello NK, Mendelson JH, Sholar MB, Jaszyna-Gasior M, Goletiani N, Siegel AJ: Effects of the mixed mu/kappa opioid nalbuphine on cocaine-induced changes in subjective and cardiovascular responses in men. Neuropsychopharmacology. 2005 Mar;30(3):618-32. [Article]
- Gear RW, Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD: The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain. Pain. 1999 Nov;83(2):339-45. [Article]
- Peng X, Knapp BI, Bidlack JM, Neumeyer JL: Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. J Med Chem. 2007 May 3;50(9):2254-8. Epub 2007 Apr 4. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin (PubMed:10529478, PubMed:12589820, PubMed:7891175, PubMed:7905839, PubMed:7957926, PubMed:9689128). Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone (PubMed:10529478, PubMed:10836142, PubMed:12589820, PubMed:19300905, PubMed:7891175, PubMed:7905839, PubMed:7957926, PubMed:9689128). Also activated by enkephalin peptides, such as Met-enkephalin or Met-enkephalin-Arg-Phe, with higher affinity for Met-enkephalin-Arg-Phe (By similarity). Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors (PubMed:7905839). The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15 (PubMed:12068084). They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B (By similarity). Also couples to adenylate cyclase stimulatory G alpha proteins (By similarity). The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4 (By similarity). Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization (By similarity). Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction (By similarity). The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins (By similarity). The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation (By similarity). Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling (By similarity). Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling (By similarity). Endogenous ligands induce rapid desensitization, endocytosis and recycling (By similarity). Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties (By similarity)
- Specific Function
- beta-endorphin receptor activity
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- Kishioka S, Ko MC, Woods JH: Diltiazem enhances the analgesic but not the respiratory depressant effects of morphine in rhesus monkeys. Eur J Pharmacol. 2000 May 26;397(1):85-92. [Article]
- Hoehe M, Duka T: Opiates increase plasma catecholamines in humans. Psychoneuroendocrinology. 1993;18(2):141-8. [Article]
- Zernig G, Lewis JW, Woods JH: Clocinnamox inhibits the intravenous self-administration of opioid agonists in rhesus monkeys: comparison with effects on opioid agonist-mediated antinociception. Psychopharmacology (Berl). 1997 Feb;129(3):233-42. [Article]
- Picker MJ: Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists. J Pharmacol Exp Ther. 1997 Dec;283(3):1009-17. [Article]
- McNicol ED, Boyce D, Schumann R, Carr DB: Mu-opioid antagonists for opioid-induced bowel dysfunction. Cochrane Database Syst Rev. 2008 Apr 16;(2):CD006332. doi: 10.1002/14651858.CD006332.pub2. [Article]
- Tao PL, Liang KW, Sung WY, Wu YT, Huang EY: Nalbuphine is effective in decreasing the rewarding effect induced by morphine in rats. Drug Alcohol Depend. 2006 Sep 15;84(2):175-81. Epub 2006 Mar 6. [Article]
- Smith MA, Greene-Naples JL, Lyle MA, Iordanou JC, Felder JN: The effects of repeated opioid administration on locomotor activity: I. Opposing actions of mu and kappa receptors. J Pharmacol Exp Ther. 2009 Aug;330(2):468-75. doi: 10.1124/jpet.108.150011. Epub 2009 Apr 29. [Article]
- Mello NK, Mendelson JH, Sholar MB, Jaszyna-Gasior M, Goletiani N, Siegel AJ: Effects of the mixed mu/kappa opioid nalbuphine on cocaine-induced changes in subjective and cardiovascular responses in men. Neuropsychopharmacology. 2005 Mar;30(3):618-32. [Article]
- Meerpohl JJ, Timmer A: [News from the cochrane library: mu opioid antagonists for opioid-induced bowel dysfunction]. Z Gastroenterol. 2008 Sep;46(9):917-21. doi: 10.1055/s-2008-1027720. Epub 2008 Sep 22. [Article]
- Peng X, Knapp BI, Bidlack JM, Neumeyer JL: Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors. J Med Chem. 2007 May 3;50(9):2254-8. Epub 2007 Apr 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein coupled receptor that functions as a receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine
- Specific Function
- G protein-coupled enkephalin receptor activity
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- Chen JC, Smith ER, Cahill M, Cohen R, Fishman JB: The opioid receptor binding of dezocine, morphine, fentanyl, butorphanol and nalbuphine. Life Sci. 1993;52(4):389-96. [Article]
- De Souza EB, Schmidt WK, Kuhar MJ: Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J Pharmacol Exp Ther. 1988 Jan;244(1):391-402. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 05, 2024 03:14