Frey P, Berney D, Herrling P L, Mueller W, Urwyler S
Sandoz Research Institute, Berne, Switzerland.
Neurosci Lett. 1988 Aug 31;91(2):194-8. doi: 10.1016/0304-3940(88)90767-7.
The 6,7-dichloro derivative of 3-hydroxy-2-quinoxalinecarboxylic acid (diCl-HQC) is a relatively potent antagonist at the two excitatory amino acid receptor subtypes activated by N-methyl-D-aspartate (NMDA) and kainic acid. It antagonizes NMDA-induced excitation in the frog spinal cord (pA2 5.8), i.e. with a potency similar to D-2-amino-7-phosphonoheptanoate (D-AP-7). It also antagonizes NMDA-induced sodium efflux from rat brain slices (pA2 5.6). The compound inhibits kainic acid-induced sodium efflux from rat brain slices with a pA2 of 5.4 and it inhibits [3H]kainic acid binding to rat brain membranes with a pKi of 5.4. DiCl-HQC is only weakly active at the quisqualate receptor. This spectrum of activities may make this compound a useful tool to investigate the pharmacology of excitatory amino acid receptors.
3-羟基-2-喹喔啉羧酸的6,7-二氯衍生物（二氯-HQC）是N-甲基-D-天冬氨酸（NMDA）和红藻氨酸激活的两种兴奋性氨基酸受体亚型的相对强效拮抗剂。它拮抗蛙脊髓中NMDA诱导的兴奋（pA2 5.8），即效力与D-2-氨基-7-磷酸庚酸（D-AP-7）相似。它还拮抗NMDA诱导的大鼠脑片钠外流（pA2 5.6）。该化合物抑制红藻氨酸诱导的大鼠脑片钠外流，pA2为5.4，并且它抑制[3H]红藻氨酸与大鼠脑膜的结合，pKi为5.4。二氯-HQC在quisqualate受体上仅有微弱活性。这种活性谱可能使该化合物成为研究兴奋性氨基酸受体药理学的有用工具。
