Antonelli T, Carlà V, Lambertini L, Moroni F, Bianchi C
Pharmacol Res Commun. 1984 Feb;16(2):189-97. doi: 10.1016/s0031-6989(84)80094-6.
Pyroglutamic acid (1-PCA), a cyclic derivative of glutamic acid, was administered i.p. (7.7 mmol/kg) or intracerebroventricularly (25 - 50 mumol) to freely moving guinea-pigs, provided with semi-permanently implanted epidural cups. The effect of this compound on cortical Acetylcholine (ACh) and GABA outflow, as well as on gross behaviour and electrocorticogram (E.Co.G.) was investigated. 1-PCA increased the release of ACh and GABA from the cortical surface, did not change their cortical content, decreased the spontaneous motor activity and synchronized the E.Co.G.. These results suggest that 1-PCA increases GABA release, possibly by changing amino acid transport through the biological barrier or by acting as antagonist on the receptors for glutamic acid. In turn, the activation of the GABA system increases, as previously demonstrated, the cortical ACh release and causes mild sedation and E.Co.G. synchronization.
焦谷氨酸（1-PCA）是谷氨酸的环状衍生物，以腹腔注射（7.7毫摩尔/千克）或脑室内注射（25 - 50微摩尔）的方式给予自由活动的豚鼠，这些豚鼠已半永久性植入硬膜外杯。研究了该化合物对皮质乙酰胆碱（ACh）和GABA流出的影响，以及对总体行为和脑电图（E.Co.G.）的影响。1-PCA增加了皮质表面ACh和GABA的释放，不改变它们在皮质中的含量，减少了自发运动活动并使E.Co.G.同步化。这些结果表明，1-PCA可能通过改变氨基酸通过生物屏障的转运或作为谷氨酸受体的拮抗剂来增加GABA的释放。反过来，如先前所示，GABA系统的激活会增加皮质ACh的释放，并导致轻度镇静和E.Co.G.同步化。
