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IS20 is a nonpeptide agonist of prokineticin receptor 1 (PKR1) and a positive allosteric modulator (PAM) of PKR2.1 It increases intracellular calcium release and Akt phosphorylation in PKR1-expressing CHO cells (EC50 = 44 nM). It also enhances prokineticin-induced ERK phosphorylation in PKR2-expressing CHO cells when used at a concentration of 1 nM. IS20 (0.5 mg/kg, i.p.) increases survival, reduces cardiac lesion formation, improves cardiac function, and increases neovasculogenesis in a mouse model of myocardial infarction.
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1. Discovery and cardioprotective effects of the first non-