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2022 Update-Veterinary Drugs & Uses
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DrugCentral 2023 ๐
2022 Update-Veterinary Drugs & Uses
Search
Structure ๐
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L1000
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FDA-approved
EMA-approved
PMDA-approved
Target Card Uniprot Example:
P23975
reboxetine ๐ถ
Veterinary Use |
Indications/Contra
| FAERs-F
| FAERs-M
| Orange Bk
| BioActivity |
Stem definition
Drug id
CAS RN
serotonin and/or norepinephrine reuptake inhibitors, fluoxetine derivatives
2361
71620-89-8
Description:
Molecule
Description
Molfile
Inchi
Smiles
Synonyms:
reboxetine mesilate
reboxetine mesylate
edronax
reboxetine
norebox
reboxitine
A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER.
Molecular weight: 313.40
Formula: C19H23NO3
CLOGP: 3.06
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 39.72
ALOGS: -4.15
ROTB: 6
Drug dosage:
Dose
Unit
Route
8
mg
O
ADMET properties:
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Property
Value
Reference
BA (Bioavailability)
94 %
Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)
8 mg/mL
Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)
10 hours
Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)
10 %
Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)
1
Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)
0.82 mL/min/kg
Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)
0.65 L/kg
Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)
0.55 ยตM/kg/day
Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)
0.02 %
Lombardo F, Berellini G, Obach RS
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Approvals:
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Date
Agency
Company
Orphan
Jan. 1, 1997
YEAR INTRODUCED
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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:
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Source
Code
Description
ATC
N06AX18
NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTIDEPRESSANTS
Other antidepressants
MeSH PA
D018663
Adrenergic Agents
MeSH PA
D018759
Adrenergic Uptake Inhibitors
MeSH PA
D000928
Antidepressive Agents
MeSH PA
D002491
Central Nervous System Agents
MeSH PA
D049990
Membrane Transport Modulators
MeSH PA
D018377
Neurotransmitter Agents
MeSH PA
D014179
Neurotransmitter Uptake Inhibitors
MeSH PA
D011619
Psychotropic Drugs
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Drug Use
| Suggest Off label Use Form|
|View source of the data|
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Disease
Relation
SNOMED_ID
DOID
Major depressive disorder
indication
370143000
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๐ถ Veterinary Drug Use
None
๐ถ Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
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Dissociation level
Dissociation constant
Type (acidic/basic)
pKa1
8.44
Basic
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Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
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Target
Class
Pharos
UniProt
Action
Type
Activity value
(-log[M])
Mechanism
action
Bioact source
MoA source
Sodium-dependent serotonin transporter
Transporter
P31645
SC6A4_HUMAN
Ki
8.05
CHEMBL
Sodium-dependent noradrenaline transporter
Transporter
P23975
SC6A2_HUMAN
Ki
8.96
CHEMBL
5-hydroxytryptamine receptor 2C
GPCR
P28335
5HT2C_HUMAN
Ki
6.34
PDSP
5-hydroxytryptamine receptor 6
GPCR
P50406
5HT6R_HUMAN
Ki
6.34
WOMBAT-PK
Sodium-dependent dopamine transporter
Transporter
Q01959
SC6A3_HUMAN
Ki
7.22
CHEMBL
G protein-activated inward rectifier potassium channel 2
Ion channel
P48051
KCNJ6_HUMAN
IC50
4.19
WOMBAT-PK
Kir3.1/Kir3.2
Ion channel
P48051
P48549
KCNJ6_HUMAN
KCNJ3_HUMAN
IC50
4.32
WOMBAT-PK
Kir3.1/Kir3.4
Ion channel
P48544
P48549
KCNJ5_HUMAN
KCNJ3_HUMAN
IC50
4.39
WOMBAT-PK
Sodium-dependent serotonin transporter
Transporter
SC6A4_RAT
Ki
6.30
CHEMBL
Transporter
Transporter
Q9WTR4_RAT
Ki
7.86
CHEMBL
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External reference:
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ID
Source
41X
PDB_CHEM_ID
006792
NDDF
127151
PUBCHEM_CID
153494
RXNORM
321995004
SNOMEDCT_US
395859006
SNOMEDCT_US
4025263
VANDF
4025264
VUID
4025264
VANDF
4808
IUPHAR_LIGAND_ID
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Pharmaceutical products:
None
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reboxetine