A novel intravenous vehicle for preclinical cardiovascular screening of small molecule drug candidates in rat

Screening novel, poorly soluble small-molecule candidates for cardiovascular liabilities represents a key challenge in early drug discovery. This report describes a novel vehicle composed of 20% N,N-Dimethylacetamide (DMA)/40% Propylene glycol (PG)/40% Polyethylene Glycol (PEG-400) (DPP) for adminis...

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Veröffentlicht in:	Journal of pharmacological and toxicological methods 2016-11, Vol.82, p.62-67
Hauptverfasser:	Banfor, Patricia N., Gintant, Gary A., Lipari, John M., Zocharski, Philip D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetamides - administration & dosage Acetamides - chemistry Acetamides - toxicity Animals Blood pressure Cardiac contractility Cardiovascular screening Drug Carriers - administration & dosage Drug Carriers - chemistry Drug Carriers - toxicity Drug Discovery - methods Drug Evaluation, Preclinical Excipients - administration & dosage Excipients - chemistry Excipients - toxicity Formulation Heart rate Hemodynamics - drug effects Infusions, Intravenous Lethal Dose 50 Male Methods Models, Cardiovascular Pharmaceutical Preparations - administration & dosage Pharmaceutical Preparations - blood Pharmaceutical Preparations - chemistry Pharmacokinetic Polyethylene Glycols - administration & dosage Polyethylene Glycols - chemistry Polyethylene Glycols - toxicity Propylene Glycol - administration & dosage Propylene Glycol - chemistry Propylene Glycol - toxicity Rats, Sprague-Dawley Safety pharmacology Small Molecule Libraries - administration & dosage Small Molecule Libraries - adverse effects Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacokinetics Solubility Vehicle
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