L-半胱氨酸亚磺酸是几种大鼠代谢型谷氨酸受体 (mGluR) 的有效激动剂，对 mGluR1、mGluR5、mGluR2、mGluR4、mGluR6 和 mGluR8 的 pEC50 分别为 3.92、4.6、3.9、2.7、4.0 和 3.94 .
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.
L-Cysteinesulfinic acid is an endogenous agonist of a metabotropic receptor coupled to stimulation of phospholipase D (PLD) activity. L-CSA is an endogenous agonist of the PLD-coupled metabotropic excitatory amino acids (EAA) receptor. L-CSA selectively activates the PLD-coupled receptor. 1 mM L-CSA induces a significant increase in PLD activity in hippocampal slices, whereas 1 mM concentrations of L-glutamate, L-aspartate, and L-HCA are without effect. L-CSA elicits a dose-dependent increase in PLD activity in rat hippocampal slices in the presence of iGluR antagonists, with an approximate EC50 of 500 uM. The PLD response induced by 1 mM L-CSA is not significantly decreased in the presence of 1 uM tetrodotoxin, suggesting that this response is not dependent upon L-CSA-induced increasesin cell firing[1].
参考文献:
[1]. Shi Q, et al. L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists. J Pharmacol Exp Ther. 2003 Apr;305(1):131-42.
[2]. Boss V, et al. L-cysteine sulfinic acid as an endogenous agonist of a novel metabotropic receptor coupled to stimulation of phospholipase D activity.
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