LY 225910 is a potent and selective cholecystokinin receptor antagonist that specifically blocks the CCK2 receptor and influences neurotransmitter release[1-2]. LY 225910 is utilized to investigate the role of the CCK2 receptor in brain processes such as emotion, anxiety, and pain, as well as its modulation of GABAergic neurotransmission[3-4].
In vivo, LY 225910 (25ng; single injection) administered intrathecally in a rat model of lipopolysaccharide-induced central nervous system inflammation enhances the analgesic effects of morphine[5]. LY 225910 (0.1mg/kg) was administered as a single intraperitoneal injection to male Sprague-Dawley rats. LY 225910 exhibited anxiolytic-like effects within 24 hours, but at 24 hours post-administration, LY 225910 impaired the rats' novel object recognition and spatial recognition abilities[6].
References:
[1] Crosby KM, Baimoukhametova DV, Bains JS, et al. Postsynaptic Depolarization Enhances GABA Drive to Dorsomedial Hypothalamic Neurons through Somatodendritic Cholecystokinin Release. J Neurosci. 2015 Sep 23;35(38):13160-70.
[2] Rust VA, Crosby KM. Cholecystokinin acts in the dorsomedial hypothalamus of young male rats to suppress appetite in a nitric oxide-dependent manner. Neurosci Lett. 2021 Nov 1;764:136295.
[3] Lee JH, Kim SY, Kwon YK, et al. Characteristics of the cholecystokinin-induced depolarization of pacemaking activity in cultured interstitial cells of Cajal from murine small intestine. Cell Physiol Biochem. 2013;31(4-5):542-54.
[4] Soltani N, Roohbakhsh A, Allahtavakoli M, et al. Heterogeneous effects of cholecystokinin on neuronal response properties in deep layers of rat barrel cortex. Somatosens Mot Res. 2018 Jun;35(2):131-138.
[5] Xanthos DN, Kumar N, Theodorsson E, et al. The roles of nerve growth factor and cholecystokinin in the enhancement of morphine analgesia in a rodent model of central nervous system inflammation. Neuropharmacology. 2009 Mar;56(3):684-91.
[6] Ballaz SJ, Bourin M, Akil H, et al. Blockade of the cholecystokinin CCK-2 receptor prevents the normalization of anxiety levels in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jan 10;96:109761.
LY 225910是一种有效的胆囊收缩素受体拮抗剂，可特异性阻断CCK2受体并影响神经递质释放[1-2]。LY 225910可用于研究CCK2受体在情绪、焦虑和疼痛等大脑过程中的作用机制，以及其对GABA神经传递的调节[3-4]。
在体内，LY 225910 (25ng；单次注射)鞘内注射用于处理经脂多糖诱导中枢神经系统炎症的大鼠模型。LY 225910能够增强吗啡的镇痛效果[5]。LY 225910(0.1mg/kg)单次腹腔注射用于处理雄性Sprague-Dawley大鼠。LY 225910在24小时内表现出抗焦虑样作用，但在24小时后，LY 225910损害了大鼠对新物体识别和位置识别能力[6]。