L-O-Phosphoserine是 III 类代谢型谷氨酸受体（mGluR4、mGluR7 和 mGluR8）的激动剂，也是竞争性 NMDA 受体拮抗剂。
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O-Phospho-L-serine serves as the direct forerunner of L-serine in the pathway of serine synthesis and functions as an activator for the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8). Additionally, it acts as a mild inhibitor for mGluR1 and a strong inhibitor for mGluR2[1].
体外研究
O-phosphate L-serine (I-SOP) weakly binds to mGluR1 and antagonizes the effect of L-glutamic acid. L-SOP can activate class III receptors (mGluR4, mGluR6, mGluR7, and mGluR8), but mGluR7 has a much lower affinity for L-SOP than other class III receptors and a lower effect on both ligands [1].
O-Phospho-L-serine (l-SOP) leads to increased intracellular calcium levels in cells expressing mGluR4 and obstructs the l-glutamate induced mGluR1 activation with a Ki of 1 mM. It presents a much stronger inhibition of mGluR2 activation with a Ki of 1 μM, showcasing a thousand-fold greater potency against mGluR2 than mGluR1. l-SOP also causes alterations in membrane potential in HEK/TRPC4 cells expressing mGluR4 or mGluR6 and initiates TRPC4β activity through Gαi/o proteins[2].
O-Phospho-L-serine (l-SOP) prevents the proliferation of Müller glial cells without impacting the death of photoreceptor cells caused by light exposure. It interferes with the proliferation of Müller glia, coinciding with or following the activation of ascl1a and stat3 in the light-damaged retina, and inhibits the regeneration of cone cells in the retina following light damage[3].
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