Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.

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Liu G, Zhao H, Liu B, Xin Z, Liu M, Serby MD, Lubbers NL, Widomski DL, Polakowski JS, Beno DW, Trevillyan JM, Sham HL

Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):495-500. Epub 2006 Oct 10.

PubMed ID

17055723 [ View in PubMed

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Abstract

The hemodynamic effects of a series of potent and selective 4-aminopyridine carboxamide-based pan-JNK inhibitors were assessed in an anesthetized rat model. The effects of these agents on mean arterial pressure, heart rate, cardiac contractility, and peripheral vascular resistance are described, and the implication for targeting protein kinases in metabolic diseases is discussed.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cyclohexyl-{4-[5-(3,4-Dichlorophenyl)-2-Piperidin-4-Yl-3-Propyl-3h-Imidazol-4-Yl]-Pyrimidin-2-Yl}Amine	Mitogen-activated protein kinase 10	IC 50 (nM)	2	N/A	N/A	Details