Ibii N, Ikeda M, Takahara Y, Eigyo M, Akiyoshi T, Matsushita A
Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.
Peptides. 1989 Jul-Aug;10(4):779-83. doi: 10.1016/0196-9781(89)90113-7.
Ceruletide (CLT: 160 micrograms/kg, SC) produced a relatively long-lasting inhibition of haloperidol (HPD: 2 mg/kg, PO) catalepsy in rats. Neither bilateral vagotomies nor hypophysectomy abolished the anticataleptic effect of CLT. However, (-)-L-364,718 and proglumide blocked the effect of CLT. CLT (160 micrograms/kg) significantly inhibited HPD (2 mg/kg)-induced increase in dopamine (DA) release from the rat striatum. This effect of CLT was also antagonized by proglumide. These results suggest that CLT (160 micrograms/kg) primarily acts on cholecystokinin-A receptor in the brain, exerts some modulatory influence on HPD binding to striatal DA receptors via unknown neural pathways and, consequently, inhibits HPD catalepsy.
蛙皮素（CLT：160微克/千克，皮下注射）对大鼠氟哌啶醇（HPD：2毫克/千克，口服）引起的僵住症产生了相对持久的抑制作用。双侧迷走神经切断术和垂体切除术均未消除CLT的抗僵住症作用。然而，（-）-L-364,718和丙谷胺阻断了CLT的作用。CLT（160微克/千克）显著抑制了HPD（2毫克/千克）诱导的大鼠纹状体多巴胺（DA）释放增加。CLT的这一作用也被丙谷胺拮抗。这些结果表明，CLT（160微克/千克）主要作用于脑中的胆囊收缩素-A受体，通过未知的神经通路对HPD与纹状体DA受体的结合产生某种调节作用，从而抑制HPD引起的僵住症。
