Vasar E E, Riago L K, Soosaar A Kh, Nurk A M, Maĭmets M O
Biull Eksp Biol Med. 1985 Dec;100(12):711-3.
Subcutaneous administration of caerulein (100-500 micrograms/kg) significantly reduced the development of picrotoxin (8 mg/kg) seizures in male mice. The same doses of caerulein inhibited 3H-flunitrazepam binding in in vivo experiments. Proglumide, an antagonist of cholecystokinin receptors, in low dose (5 mg/kg) potentiated the effects of caerulein (100 micrograms/kg), whereas the administration of proglumide in high dose (25 mg/kg) reduced the action of caerulein on 3H-flunitrazepam binding and picrotoxin seizures. Caerulein (5-1000 nM) decreased 3H-flunitrazepam binding in in vitro experiments only after supplementation of the binding medium with 120 mM NaCl and 5mM KCl. The results suggest the possible interaction of caerulein with chloride ionophor. It seems probable that the direct interaction of caerulein with chloride ionophor in involved in the inhibitory effect of caerulein on picrotoxin seizures and 3H-flunitrazepam binding.
皮下注射蛙皮素（100 - 500微克/千克）可显著降低雄性小鼠对印防己毒素（8毫克/千克）诱发癫痫的易感性。相同剂量的蛙皮素在体内实验中可抑制3H-氟硝西泮结合。胆囊收缩素受体拮抗剂丙谷胺，低剂量（5毫克/千克）时可增强蛙皮素（100微克/千克）的作用，而高剂量（25毫克/千克）给药时则可减弱蛙皮素对3H-氟硝西泮结合及印防己毒素诱发癫痫的作用。仅在结合介质中添加120 mM氯化钠和5 mM氯化钾后，蛙皮素（5 - 1000 nM）在体外实验中才会降低3H-氟硝西泮结合。结果提示蛙皮素可能与氯离子载体相互作用。蛙皮素与氯离子载体的直接相互作用似乎参与了蛙皮素对印防己毒素诱发癫痫及3H-氟硝西泮结合的抑制作用。
