| Description | Gacyclidine (OTO311) is a small molecule N-methyl-D-aspartate (NMDA) receptor antagonist. Local injection of Gacyclidine in the cochlea inhibits salicylate-induced tinnitus and can be used to treat brain injury, spinal cord injury and tinnitus. |
| In vitro | 在初级皮层培养中，gacyclidine 及其对映体，在浓度范围0.1至5.0μM，可阻止谷氨酸引起的神经元死亡。[1] |
| In vivo | 在大鼠体内，gacyclidine的神经毒性远低于MK-801。在使用gacyclidine治疗后18或96小时牺牲的动物中，未检测到坏死神经元（剂量为1、5、10或20 mg/kg，静脉注射）。在最高剂量（20 mg/kg）而非较低剂量（1-100 mg/kg）时，电子显微镜揭示少数细胞质或线粒体内的液泡。此外，在大鼠中，gacyclidine在三种脊髓损伤模型中表现出剂量和时间依赖性的神经保护作用。gacyclidine的益处包括减少损伤大小和改善伤后功能参数。在创伤性脑损伤模型中，gacyclidine改善行为参数和神经元存活。在伤后0至30分钟内给药时获得最佳保护。[1] |
| Synonyms | GK 11, OTO311, OTO-311, OTO 311, GK-11 |
| molecular weight | 263.44 |
| Molecular formula | C16H25NS |
| CAS | 68134-81-6 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 2.63 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Hirbec H, et al. Gacyclidine: a new neuroprotective agent acting at the N-methyl-D-aspartate receptor. CNS Drug Rev. 2001 Summer;7(2):172-98. 2. Hoizey G, et al. Modified gas chromatographic-mass spectrometric assay for the determination of gacyclidine enantiomers in human plasma. J Chromatogr B Biomed Sci Appl. 1999 Aug 20;731(2):317-22. 3. Chenoweth JA, et al. Altered mental status and end organ damage associated with the use of gacyclidine: a case series. J Med Toxicol. 2015 Mar;11(1):115-20. 4. Lallement G, et al. Review of the value of gacyclidine (GK-11) as adjuvant medication to conventional treatments of organophosphate poisoning: primate experiments mimicking various scenarios of military or terrorist attack by soman. Neurotoxicology. 1999 Aug;20(4):675-84. |