CP-409092 - CAS 194098-25-4
Catalog number: 194098-25-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
GABA Receptor
CP-409092 is a GABA(A) partial agonist developed for the treatment of General Anxiety Disorder (GAD) and presents an interesting phenomenon of human pharmacokinetic predictions. In vitro, CP-409092 was abroadly metabolized in rat and human systems predominantly to acid metabolite formed by oxidative deamination of the N-methyl group of CP-409092 mediated by MAO-A (as deduced from inhibition experiments).
Solid powder
N-[4-(methylaminomethyl)phenyl]-4-oxo-1,5,6,7-tetrahydroindole-3-carboxamide; 4-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylic acid (4-methylaminomethylphenyl)amide; CP 409,092; CP 409092; CP-409,092; CP-409092; CP409,092; CP409092
Canonical SMILES:
1.Dog colonoscopy model for predicting human colon absorption.
Sutton SC;Evans LA;Fortner JH;McCarthy JM;Sweeney K Pharm Res. 2006 Jul;23(7):1554-63. Epub 2006 Jun 21.
PURPOSE: ;This study was conducted to develop and validate a dog colon model that predicts colon permeability in humans.;METHODS: ;The following compounds were studied: Class 1 highly soluble (HS)/highly permeable (HP): aminophylline, propranolol, CP-409092; Class 2 LS/HP: nifedipine; trovafloxacin, sertraline; Class 3 HS/LP: azithromycin, atenolol, CP-331684, CP-424391; Class 4 LS/LP: CJ-13610. Administration to dogs was made 30 cm cranial to the anal sphincter with a lubricated Schott Model VFS-5 flexible endoscope. The bioavailability of the compound following the colon administration in dogs, relative to the same formulation administered orally (relative bioavailability), was determined.;RESULTS: ;Except for atenolol, a small hydrophillic molecule, the relative bioavailability from administration to the colon of the dog correlated well with the following compound properties: high solubility and high, passive permeability > high solubility, low permeability > low solubility, high, passive permeability approximately low solubility, low permeability.;CONCLUSION: ;The dog colon model is proposed as a surrogate for human intubation studies when the controlled release candidate falls in BCS Classes 2 (LS/HP), 3 (HS/LP), and 4 (LS/LP).
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CAS 194098-25-4 CP-409092

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