AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
Try a sample question
Select a question to fill the search bar, then submit it or edit it first.
AI can make mistakes. Verify answers against the original sources before relying on them.
nalorphine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists, morphinan derivates | 1877 | 62-67-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.598 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.127 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 23.988 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 31.333 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 50.860 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 71.100 | % | High | 1 |
| herg | hERG pIC50 | 4.810 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 10.715 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 10.617 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 49.140 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK2,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IGF1R,ITK,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 56 | |||
| kinase-selectivity-class | EIF2AK3,MAP2K6,MAP3K14,TEK | 4 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.499 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 121.339 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 48.390 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 9.268 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 68.480 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 171.396 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 84.510 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 44.780 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 933.254 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V03AB02 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes |
| MeSH PA | D009292 | Narcotic Antagonists |
| MeSH PA | D018689 | Sensory System Agents |
Related Drugs by ATC class:
V03AB Antidotes 28 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Dogs | Respiratory and circulatory depression resulting from overdosage of, or unusual sensitivity to, morphine and other narcotics | Indication |
| Dogs | Depression | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Nalline Hydrochloride | Boehringer lngelheim Animal Health USA Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.71 | acidic |
| pKa2 | 7.88 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | Ki | 9.72 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 7.32 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 9.42 | CHEMBL | |||||
| Delta-type opioid receptor | GPCR | Ki | 6.92 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | Ki | 8.70 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 7.82 | CHEMBL | |||||
| Opioid receptor | GPCR | EC50 | 8.82 | CHEMBL | |||||
| Opioid receptor | GPCR | IC50 | 7.23 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D08247 | KEGG_DRUG |
| C0027355 | UMLSCUI |
| CHEBI:7458 | CHEBI |
| CHEMBL415284 | ChEMBL_ID |
| DB11490 | DRUGBANK_ID |
| D009269 | MESH_DESCRIPTOR_UI |
| 5284595 | PUBCHEM_CID |
| 1629 | IUPHAR_LIGAND_ID |
| 30 | INN_ID |
| U59WB2WRY2 | UNII |
| 001612 | NDDF |
| 004659 | NDDF |
| 373774009 | SNOMEDCT_US |
| 6526001 | SNOMEDCT_US |
| 96192005 | SNOMEDCT_US |
| CHEMBL1908349 | ChEMBL_ID |
| 57-29-4 | SECONDARY_CAS_RN |
Pharmaceutical products:
None