pridinol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
2263 511-45-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pridinol
  • pridinol methanesulfonate salt
  • pridinol methanesulfonate
antispasmodic & muscle relaxant; RN given refers to parent cpd; structure in Merck Index, 9th ed, #7539
  • Molecular weight: 295.43
  • Formula: C20H25NO
  • CLOGP: 4.07
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -4.19
  • ROTB: 5

Drug dosage:

DoseUnitRoute
6 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.03 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 77 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.813 Moderate 0.68
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.180 Moderate 0.68
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 30.409 10^-6 cm/s Moderate 0.68
dh-clint Dog hepatocyte intrinsic clearance 22.387 uL/min/10^6 cells Moderate 0.68
dppb Dog plasma protein binding (% unbound) 26.190 % Moderate 0.68
fcs-ppb Fetal calf serum protein binding (% unbound) 43.930 % Moderate 0.68
herg hERG pIC50 5.427 pIC50 Moderate 0.68
hh-clint Human hepatocyte intrinsic clearance 9.795 uL/min/10^6 cells Moderate 0.68
hlm-clint Human liver microsomal intrinsic clearance 21.429 uL/min/mg protein Moderate 0.68
hppb Human plasma protein binding (% unbound) 30.530 % Moderate 0.68
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK 42
kinase-selectivity-class AKT3,AXL,BRAF,EPHB4,ERBB2,FLT3,GRK2,PDK4,SIK2,SIK3,STK33,TEK,TGFBR1 13
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.527 Moderate 0.68
mh-clint Mouse hepatocyte intrinsic clearance 156.675 Moderate 0.68
mppb Mouse plasma protein binding (% unbound) 44.780 Moderate 0.68
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.054 Moderate 0.68
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 54.990 % Moderate 0.68
rh-clint Rat hepatocyte intrinsic clearance 276.058 uL/min/10^6 cells Moderate 0.68
rh-fuinc Rat hepatocyte fraction unbound in incubation 67.780 % Moderate 0.68
rppb Rat plasma protein binding (% unbound) 38.960 % Moderate 0.68
solubility-dd Solubility at pH 7.4 in DMSO 841.395 uM Moderate 0.68

Approvals:

None

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:

SourceCodeDescription
ATC M03BX03 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Other centrally acting agents
ATC M03BX53 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Other centrally acting agents
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:51371 muscle relaxant

Related Drugs by ATC class:

M03BX Other centrally acting agents 9 drugs

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 levelDissociation constantType (acidic/basic)
pKa1 8.8 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M1 GPCR Ki 8.80 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 8.15 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 8.19 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 8.59 PDSP
Muscarinic acetylcholine receptor M5 GPCR Ki 7.80 PDSP

External reference:

IDSource
D08418 KEGG_DRUG
C0071968 UMLSCUI
CHEBI:75247 CHEBI
CHEMBL404215 ChEMBL_ID
DB13642 DRUGBANK_ID
C009185 MESH_SUPPLEMENTAL_RECORD_UI
4904 PUBCHEM_CID
1320 INN_ID
9E75Q6SUUB UNII
34479 RXNORM
006583 NDDF
39003011000001103 SNOMEDCT_US
CHEMBL1528011 ChEMBL_ID

Pharmaceutical products:

None