四种假定的谷氨酸拮抗剂与谷氨酸的相互作用及其对蟾蜍脊髓的影响。

The interaction of four putative glutamate antagonists with glutamate and their effects on the toad spinal cord.

Bailey P A, Phillis J W

Gen Pharmacol. 1976 Sep;7(4):283-7. doi: 10.1016/0306-3623(76)90090-2.

Abstract

Four putative glutamate antagonists (L-glutamate diethyl ester, L-glutamate dimethyl ester, L-proline and 1-hydroxy-3-amino-pyrrolidone-2) were tested on the isolated hemisected toad spinal cord. 2. 1-hydroxy-3-amino-pyrrolidone-2 (10(-3)-10(-2) M) selectively antagonized the depolarizations evoked in both dorsal and ventral roots by applications of L-glutamate (5 X 10(-4) M). 3 1-hydroxy-3-amino-pyrrolidone-2 also antagonized the depolarizations evoked in both dorsal and ventral roots by stimulation of the adjacent dorsal root. 4. The dimethyl and diethyl esters of L-glutamate and L-proline had their own depolarizing actions on the dorsal and ventral roots, and neither potentiated nor antagonized the effects of L-glutamate. 5. The results with 1-hydroxy-3-amino-pyrrolidone-2 offer further evidence for the involvement of L-glutamate and L-aspartate in synaptic transmission in the amphibian spinal cord.

摘要

对四种假定的谷氨酸拮抗剂（L - 谷氨酸二乙酯、L - 谷氨酸二甲酯、L - 脯氨酸和1 - 羟基 - 3 - 氨基 - 吡咯烷 - 2）在离体半切蟾蜍脊髓上进行了测试。2. 1 - 羟基 - 3 - 氨基 - 吡咯烷 - 2（10⁻³ - 10⁻² M）选择性地拮抗了通过施加L - 谷氨酸（5×10⁻⁴ M）在背根和腹根中诱发的去极化。3. 1 - 羟基 - 3 - 氨基 - 吡咯烷 - 2还拮抗了通过刺激相邻背根在背根和腹根中诱发的去极化。4. L - 谷氨酸和L - 脯氨酸的二甲酯和二乙酯对背根和腹根有它们自身的去极化作用，并且既不增强也不拮抗L - 谷氨酸的作用。5. 1 - 羟基 - 3 - 氨基 - 吡咯烷 - 2的结果为L - 谷氨酸和L - 天冬氨酸参与两栖类脊髓的突触传递提供了进一步的证据。