Institute of Psychiatric Research, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
J Psychopharmacol. 2013 Feb;27(2):152-61. doi: 10.1177/0269881112454230. Epub 2012 Aug 21.
Rats with chronic inhibition of GABA synthesis by infusion of l-allyglycine, a glutamic acid decarboxylase inhibitor, into their dorsomedial/perifornical hypothalamus are anxious and exhibit panic-like cardio-respiratory responses to treatment with intravenous (i.v.) sodium lactate (NaLac) infusions, in a manner similar to what occurs in patients with panic disorder. We previously showed that either NMDA receptor antagonists or metabotropic glutamate receptor type 2/3 receptor agonists can block such a NaLac response, suggesting that a glutamate mechanism is contributing to this panic-like state. Using this animal model of panic, we tested the efficacy of CBiPES and THIIC, which are selective group II metabotropic glutamate type 2 receptor allosteric potentiators (at 10-30 mg/kg i.p.), in preventing NaLac-induced panic-like behavioral and cardiovascular responses. The positive control was alprazolam (3mg/kg i.p.), a clinically effective anti-panic benzodiazepine. As predicted, panic-prone rats given a NaLac challenge displayed NaLac-induced panic-like cardiovascular (i.e. tachycardia and hypertensive) responses and "anxiety" (i.e. decreased social interaction time) and "flight" (i.e. increased locomotion) -associated behaviors; however, systemic injection of the panic-prone rats with CBiPES, THIIC or alprazolam prior to the NaLac dose blocked all NaLac-induced panic-like behaviors and cardiovascular responses. These data suggested that in a rat animal model, selective group II metabotropic glutamate type 2 receptor allosteric potentiators show an anti-panic efficacy similar to alprazolam.
通过向大鼠的背内侧/室旁下丘脑内输注 l-allylglycine(谷氨酸脱羧酶抑制剂)来慢性抑制 GABA 合成的大鼠,在用静脉内(i.v.)乳酸钠(NaLac)输注治疗时会出现焦虑和类似惊恐障碍患者的惊恐样心肺反应。我们之前曾表明,NMDA 受体拮抗剂或代谢型谷氨酸受体 2/3 受体激动剂都可以阻断这种 NaLac 反应,表明谷氨酸机制参与了这种惊恐样状态。使用这种惊恐动物模型,我们测试了 CBiPES 和 THIIC 的疗效,它们是选择性的 II 组代谢型谷氨酸受体 2 型变构调节剂(10-30mg/kg i.p.),以预防 NaLac 诱导的惊恐样行为和心血管反应。阳性对照是阿普唑仑(3mg/kg i.p.),一种临床有效的抗惊恐苯二氮䓬类药物。正如预测的那样,给予 NaLac 挑战的易惊恐大鼠表现出 NaLac 诱导的惊恐样心血管(即心动过速和高血压)反应和“焦虑”(即社交互动时间减少)和“逃避”(即运动增加)相关行为;然而,在 NaLac 剂量之前,向易惊恐大鼠系统注射 CBiPES、THIIC 或阿普唑仑可阻断所有 NaLac 诱导的惊恐样行为和心血管反应。这些数据表明,在大鼠动物模型中,选择性的 II 组代谢型谷氨酸受体 2 型变构调节剂显示出与阿普唑仑相似的抗惊恐功效。