Dihydroquinazoline and Triazinedione Derivatives as Prok1 and Prok2 receptor antagonists in HEK-293 transfected cells

BALBONI, GIANFRANCO;CONGIU, CENZO;DEPLANO, ALESSANDRO;DEMURTAS, MONICA;Buyn, Joon Seok;Sohn, Joo Mi;Lee, Jae Yeol;Sbai, Oualid;Rondard, Philippe;ONNIS, VALENTINA

2015-01-01

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Abstract

Prokineticin were originally identified as potent agents mediating gut motility, but were later shown to promote angiogenesis in steroidogenic glands, heart and reproductive system. They also modulate neurogenesis, circadian rhythms, nociception, haematopoiesis as well as immune response.[1] Prokineticin are thought to be associated with pathologies of the reproductive systems,[2] myocardial infarction,[3] and tumorigenesis.[4,5] Consequently, antagonism of the prokineticins functions may have utility in the treatment of disorders or diseases including gastrointestinal motility, angiogenesis, haematopoiesis, diabetes and pain. Here we report the identification and pharmacological characterization of a new prototype (KYS-05090) in comparison with our reference prokineticin receptor antagonist (PC-7), [6, 7] (Figure 1). Figure 1. Prokineticin receptor antagonists