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phencyclidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| muscarinic receptors agonists/antagonists | 2121 | 77-10-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 72 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 6.90 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.35 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 16 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 11.20 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PRKDC,TGFBR1 | 19 | |||
| kinase-selectivity-class | AXL,GRK2,PDK4 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug abuse | 195.49 | 81.53 | 63 | 399 | 104708 | 42516165 |
| Toxicity to various agents | 130.72 | 81.53 | 58 | 404 | 229078 | 42391795 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug abuse | 296.21 | 104.74 | 85 | 562 | 177326 | 110411326 |
| Toxicity to various agents | 227.34 | 104.74 | 89 | 558 | 480466 | 110108186 |
| Completed suicide | 149.90 | 104.74 | 55 | 592 | 242326 | 110346326 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D006213 | Hallucinogens |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018691 | Excitatory Amino Acid Antagonists |
| CHEBI has role | CHEBI:35471 | psychotropic drug |
| CHEBI has role | CHEBI:38867 | anaesthetic |
| CHEBI has role | CHEBI:50910 | neurotoxin |
| CHEBI has role | CHEBI:60643 | NMDA receptor antagonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.1 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 5.96 | CHEMBL | |||||
| Lysosomal Pro-X carboxypeptidase | Enzyme | IC50 | 7.04 | CHEMBL | |||||
| Glutamate [NMDA] receptor | Ion channel | Ki | 7.82 | CHEMBL | |||||
| Glutamate NMDA receptor; GRIN1/GRIN2B | Ion channel | IC50 | 5.90 | CHEMBL | |||||
| Glutamate NMDA receptor; GRIN1/GRIN2A | Ion channel | IC50 | 6.40 | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 1 | Ion channel | Ki | 7.28 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 6.28 | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 2C | Ion channel | Ki | 7.22 | CHEMBL | |||||
| Cholinesterase | Enzyme | Ki | 6.28 | CHEMBL | |||||
| Acetylcholine receptor subunit alpha | Ion channel | IC50 | 6.66 | CHEMBL | |||||
| Glutamate NMDA receptor | Ion channel | Ki | 7.42 | CHEMBL | |||||
| Muscarinic acetylcholine receptor | GPCR | Kd | 5.04 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D05453 | KEGG_DRUG |
| 956-90-1 | SECONDARY_CAS_RN |
| 4027426 | VANDF |
| C0031381 | UMLSCUI |
| CHEBI:8058 | CHEBI |
| 1PC | PDB_CHEM_ID |
| CHEMBL275528 | ChEMBL_ID |
| DB03575 | DRUGBANK_ID |
| CHEMBL542581 | ChEMBL_ID |
| D010622 | MESH_DESCRIPTOR_UI |
| 6468 | PUBCHEM_CID |
| 4282 | IUPHAR_LIGAND_ID |
| 1058 | INN_ID |
| J1DOI7UV76 | UNII |
| d03880 | MMSL |
| 9721008 | SNOMEDCT_US |
Pharmaceutical products:
None