摘要
y-氨基丁酸A型-苯二氮革(GABArBZ)受体广泛分布于中枢神经系统,是嵌于神经细胞膜上的异质性多肽五聚体,不同的亚单位组合发挥不同的神经抑制性药理作用,如镇静催眠、抗惊厥、抗焦虑等。PET可用于活体内受体结合的研究。GABAA-BZ受体PET显像剂分为拈抗剂、激动剂、反向激动剂3类,其中以拮抗剂显像剂11C-氟马西尼最为成熟,在癫痫、焦虑症、抑郁症、植物状态、成瘾等神经精神疾病中广泛应用。
Gamma-aminobutyric acid type A-benzodiazepine receptors are heterogeneous polypeptide pentamers widely spread in the central nervous system on the neuron membrane. Different subunit combinations educe various neuro-inhibitory pharmacological effects such as sedative, hypnosis, anticonvulsion and anxiolysis. PET can be utilized to study the binding of the receptors in vivo. PET radioligands of gammaaminobutyric acid type A-benzodiazepine receptors can be classified into 3 types: antagonists, agonists and reverse agonists, of which antagonist radiotracer 11C-flumazenil is the most commonly applied in epilepsy, anxiety disorders, depression, vegetative state, addiction and other neuro-psychiatric disorders.
出处
《国际放射医学核医学杂志》
2012年第1期1-8,共8页
International Journal of Radiation Medicine and Nuclear Medicine