Sheehan M J, de Belleroche J
Neuropeptides. 1983 Oct;3(6):429-34. doi: 10.1016/0143-4179(83)90033-1.
Cholecystokinin octapeptide and its analogue, caerulein, facilitated the K+-evoked release of 14C-GABA from tissue slices of rat parietal cortex. The effect of caerulein was maximal at 1 nM where an enhancement of 36% was produced. Cholecystokinin octapeptide gave rise to a similar maximal enhancement (29%), but was two orders of magnitude less potent. The enhancement of 14C-GABA release by caerulein was reversed by proglumide, a putative competitive antagonist at the cholecystokinin receptor. The possibility that the cholecystokinin-induced facilitation of GABA release in the cortex is involved in the anticonvulsant properties of cholecystokinin-like peptides is discussed.
胆囊收缩素八肽及其类似物蛙皮素可促进大鼠顶叶皮质组织切片中钾离子诱发的14C-γ-氨基丁酸(GABA)释放。蛙皮素在1 nM时作用最强,可使释放增强36%。胆囊收缩素八肽也产生类似的最大增强作用(29%),但效力低两个数量级。蛙皮素引起的14C-GABA释放增强被丙谷胺逆转,丙谷胺是胆囊收缩素受体的一种假定竞争性拮抗剂。文中讨论了胆囊收缩素诱导皮质中GABA释放促进作用可能与胆囊收缩素样肽的抗惊厥特性有关。