Department of Psychiatry, Ramón y Cajal University Hospital, Madrid, Spain.
Pharmacol Biochem Behav. 2012 Feb;100(4):752-74. doi: 10.1016/j.pbb.2011.04.010. Epub 2011 Apr 30.
Anxiety and stress-related disorders, namely posttraumatic stress disorder (PTSD), generalized anxiety disorder (GAD), obsessive-compulsive disorder (ODC), social and specific phobias, and panic disorder, are a major public health issue. A growing body of evidence suggests that glutamatergic neurotransmission may be involved in the biological mechanisms underlying stress response and anxiety-related disorders. The glutamatergic system mediates the acquisition and extinction of fear-conditioning. Thus, new drugs targeting glutamatergic neurotransmission may be promising candidates for new pharmacological treatments. In particular, N-methyl-d-aspartate receptors (NMDAR) antagonists (AP5, AP7, CGP37849, CGP39551, LY235959, NPC17742, and MK-801), NMDAR partial agonists (DCS, ACPC), α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors (AMPARs) antagonists (topiramate), and several allosteric modulators targeting metabotropic glutamate receptors (mGluRs) mGluR1, mGluR2/3, and mGluR5, have shown anxiolytic-like effects in several animal and human studies. Several studies have suggested that polyamines (agmatine, putrescine, spermidine, and spermine) may be involved in the neurobiological mechanisms underlying stress-response and anxiety-related disorders. This could mainly be attributed to their ability to modulate ionotropic glutamate receptors, especially NR2B subunits. The aim of this review is to establish that glutamate neurotransmission and polyaminergic system play a fundamental role in the onset of anxiety-related disorders. This may open the way for new drugs that may help to treat these conditions.
焦虑和应激相关障碍,即创伤后应激障碍(PTSD)、广泛性焦虑障碍(GAD)、强迫症(ODC)、社交和特定恐惧症以及惊恐障碍,是一个主要的公共卫生问题。越来越多的证据表明,谷氨酸能神经传递可能参与了应激反应和焦虑相关障碍的生物学机制。谷氨酸能系统介导了恐惧条件反射的获得和消退。因此,靶向谷氨酸能神经传递的新药可能是新的药物治疗的有前途的候选药物。特别是,N-甲基-D-天冬氨酸受体(NMDAR)拮抗剂(AP5、AP7、CGP37849、CGP39551、LY235959、NPC17742 和 MK-801)、NMDAR 部分激动剂(DCS、ACPC)、α-氨基-3-羟基-5-甲基-4-异恶唑丙酸受体(AMPAR)拮抗剂(托吡酯)和几种靶向代谢型谷氨酸受体(mGluRs)mGluR1、mGluR2/3 和 mGluR5 的变构调节剂,在几项动物和人类研究中显示出抗焦虑样作用。几项研究表明,多胺(胍丁胺、腐胺、亚精胺和精胺)可能参与了应激反应和焦虑相关障碍的神经生物学机制。这主要归因于它们调节离子型谷氨酸受体,特别是 NR2B 亚基的能力。本综述的目的是确定谷氨酸能神经传递和多胺能系统在焦虑相关障碍的发生中起着重要作用。这可能为治疗这些疾病的新药开辟道路。