LPA (lysophosphatidic acid), which has been shown to be involved in certain diseases such as atherosclerosis and cancer, can act through its receptor like LPA receptor 1, LPA receptor 2, or LPA receptor 3 and elicit different biological actions, like Ca2+ mobilization, changing in cAMP accumulation, changing cell shape and motility, and cell proliferation. ONO-7300243 is a potent and selective LPA1 receptors antagonist with IC50 value of 0.16μM (measured by intracellular Ca2+ concentration), much more potent to LPA2 receptor (IC50=8.6μM) and LPA3 receptor (IC50>10μM). ONO-7300243 could inhibit LPA-induced [Ca22+] increase. ONO-7300243 showed strong effects on benign prostatic hyperplasia (BPH). Oral administration of ONO-7300243 at dose of 30mg/kg led to reduced intraurethral pressure in rats.
作用机制
The basic residues in the active site of of LPA1 can form interactions with acidic functional groups of ONO-7300243[1].
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