De Bundel Dimitri, Aourz Najat, Kiagiadaki Foteini, Clinckers Ralph, Hoyer Daniel, Kastellakis Andreas, Michotte Yvette, Thermos Kyriaki, Smolders Ilse
Department of Pharmaceutical Chemistry, Research Group Experimental Neuropharmacology, Drug Analysis and Drug Information, Vrije Universiteit Brussel, Brussels, Belgium.
Neuroreport. 2010 Mar 10;21(4):254-8. doi: 10.1097/WNR.0b013e3283353a64.
Somatostatin-14 (SRIF-14) exerts anticonvulsive effects in several rat seizure models, generally attributed to sst(2) receptor activation. Whereas sst(1) immunoreactivity has been localized to both polymorphic interneurons and principal cells in the rat hippocampus, its potential role as an inhibitory autoreceptor or as a receptor involved in mediating anticonvulsive actions remains unknown. We showed that intrahippocampal administration of the sst(1) antagonist SRA880 (1 microM) induced a robust increase in hippocampal SST-14 levels without affecting gamma-aminobutyric acid levels in conscious rats, indicating that the sst(1) receptor acts as an inhibitory autoreceptor. SRA880 did not affect seizure severity and did not reverse the anticonvulsive action of SRIF-14 (1 microM) against pilocarpine-induced seizures, suggesting that hippocampal sst(1) receptors are not involved in the anticonvulsive effects of SRIF-14.
生长抑素-14（SRIF-14）在多种大鼠癫痫模型中发挥抗惊厥作用，这通常归因于sst(2)受体的激活。虽然sst(1)免疫反应性已定位到大鼠海马体中的多形性中间神经元和主细胞，但它作为抑制性自身受体或参与介导抗惊厥作用的受体的潜在作用仍不清楚。我们发现，在清醒大鼠海马内注射sst(1)拮抗剂SRA880（1微摩尔）可使海马体SST-14水平显著升高，而不影响γ-氨基丁酸水平，这表明sst(1)受体作为一种抑制性自身受体发挥作用。SRA880不影响癫痫发作的严重程度，也不能逆转SRIF-14（1微摩尔）对毛果芸香碱诱导的癫痫发作的抗惊厥作用，这表明海马体sst(1)受体不参与SRIF-14的抗惊厥作用。
