Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists
The 2-(phenylamino)imidazoline 25d was found to be a high affinity, selective prostacyclin receptor antagonist which demonstrated analgesic activity in the rat.
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2015, Microvascular ResearchCitation Excerpt :In order to achieve optimal responsiveness to prostanoid receptor agonists and antagonists, complete EGM-2 medium was diluted with serum-free EGM-2 to 10% and 30% in experiments that investigated angiogenic activation and inhibition, respectively. In these experiments the specific IP receptor antagonist CAY10441 (Clark et al., 2004) (also known as RO1138452 (Bley et al., 2006)) was used to test the involvement of the receptor in HUVEC migration and tube formation (Fig. 3A–D). Marked inhibition of HUVEC tube formation was readily apparent using phase-contrast microscopy (Fig. 3C and D).
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2015, European Journal of PharmacologyCitation Excerpt :However, it remains to be determined if either the prostaglandin I2/prostanoid IP system or the prostaglandin E2/prostanoid EP2 receptor system plays an important role in the vasodilator effects of NO on retinal blood vessels. To determine the role of the prostaglandin I2/prostanoid IP receptor system in the NO-mediated retinal vasodilatory mechanism, we examined the effects of 4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-1H-imadazol-2-amine (CAY10441), an antagonist of the prostanoid IP receptor (Clark et al., 2004), and 9α,11α-azoprosta-5Z,13E-dien-1-oic acid (U-51605), an inhibitor of prostaglandin I2 synthase (Gorman et al., 1979), on vasodilation of rat retinal arterioles induced by the NO donor (±)-(E)-4-ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide (NOR3) in vivo. We also determined whether the NO/cyclooxygenase-1/prostaglandin I2 axis is present in human retinal vascular endothelial cells.
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