guanabenz 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihypertensives, guanidine derivatives | 3952 | 5051-62-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An alpha-2 selective adrenergic agonist used as an antihypertensive agent.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 11 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.19 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 75 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| fu (Fraction unbound in plasma) | 0.10 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 7, 1982 | 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 |
|---|---|---|
| FDA MoA | N0000009918 | Adrenergic alpha2-Agonists |
| FDA EPC | N0000175554 | Central alpha-2 Adrenergic Agonist |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D000322 | Adrenergic Agonists |
| MeSH PA | D058647 | Adrenergic alpha-2 Receptor Agonists |
| MeSH PA | D000316 | Adrenergic alpha-Agonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:176497 | geroprotectors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Cerebrovascular disease | contraindication | 62914000 | DOID:6713 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Myocardial infarction in recovery phase | contraindication | 418044006 | |
| Central nervous system depression | contraindication | 418072004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.84 | Basic |
| pKa2 | 0.0 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2B adrenergic receptor | GPCR | AGONIST | Ki | 7.17 | DRUG MATRIX | CHEMBL | |||
| Alpha-2C adrenergic receptor | GPCR | AGONIST | Ki | 6.79 | DRUG MATRIX | CHEMBL | |||
| Alpha-2A adrenergic receptor | GPCR | AGONIST | Ki | 7.82 | DRUG MATRIX | CHEMBL | |||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7.21 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.97 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 6.80 | DRUG MATRIX | |||||
| Amine oxidase [flavin-containing] A | Enzyme | IC50 | 5.75 | DRUG MATRIX | |||||
| Trace amine-associated receptor 1 | GPCR | EC50 | 7.05 | CHEMBL | |||||
| Nischarin | Membrane receptor | Ki | 7.46 | CHEMBL | |||||
| Solute carrier family 22 member 1 | Transporter | IC50 | 5.31 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.93 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.95 | DRUG MATRIX | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.12 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 6.41 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 5.68 | CHEMBL | |||||
| Adrenergic receptor alpha-2 | GPCR | IC50 | 8.77 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019768 | VUID |
| N0000147859 | NUI |
| D00605 | KEGG_DRUG |
| 23256-50-0 | SECONDARY_CAS_RN |
| 4018026 | VANDF |
| 4019768 | VANDF |
| C0018312 | UMLSCUI |
| CHEBI:5553 | CHEBI |
| CHEMBL420 | ChEMBL_ID |
| DB00629 | DRUGBANK_ID |
| CHEMBL1200560 | ChEMBL_ID |
| D006143 | MESH_DESCRIPTOR_UI |
| 5702063 | PUBCHEM_CID |
| 5443 | IUPHAR_LIGAND_ID |
| 3108 | INN_ID |
| GGD30112WC | UNII |
| 227225 | RXNORM |
| 4806 | MMSL |
| 485 | MMSL |
| d00130 | MMSL |
| 000645 | NDDF |
| 004496 | NDDF |
| 372867002 | SNOMEDCT_US |
| 77764008 | SNOMEDCT_US |
| 82951001 | SNOMEDCT_US |
Pharmaceutical products:
None