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tandospirone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anxiolytics, buspirone derivatives | 2563 | 87760-53-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.513 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.851 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 25.119 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 33.343 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 22.830 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 35.830 | % | High | 1 |
| herg | hERG pIC50 | 5.352 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 15.101 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 166.725 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 16.570 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.500 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 165.577 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 18.020 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.129 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 31.920 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 144.544 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 61.590 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 13.460 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 521.195 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Rapid eye movement sleep behaviour disorder | 59.55 | 55.31 | 7 | 119 | 378 | 90627943 |
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 |
|---|---|---|
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bruxism (teeth grinding) | indication | 191983006 | DOID:2846 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.82 | Basic |
| pKa2 | 2.23 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | GPCR | Ki | 7.55 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.49 | CHEMBL | |||||
| D(4) dopamine receptor | GPCR | Ki | 8.14 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01992 | KEGG_DRUG |
| C0074676 | UMLSCUI |
| CHEBI:145673 | CHEBI |
| CHEMBL274047 | ChEMBL_ID |
| DB12833 | DRUGBANK_ID |
| CHEMBL2103888 | ChEMBL_ID |
| C055267 | MESH_SUPPLEMENTAL_RECORD_UI |
| 91273 | PUBCHEM_CID |
| 55 | IUPHAR_LIGAND_ID |
| 6332 | INN_ID |
| 112457-95-1 | SECONDARY_CAS_RN |
| 190230I669 | UNII |
| 190230I669 | INXIGHT DRUGS |
Pharmaceutical products:
None