| Description | (E/Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity . |
| In vitro | 我们研究了mGluR5在培养的大鼠皮层细胞中急性NMDA和谷氨酸介导的神经退行性病变中的作用，采用了mGluR5拮抗剂SIB-1893（20或200 μM；大鼠皮层细胞），发现它们能提供显著的保护。[4] |
| In vivo | (E/Z)-SIB-1893 (10、20和30 mg/kg；i.p.；0-180分钟) 显著降低动物在注射30 mg/kg后90、120和180分钟时的体温。相比之下，10和20 mg/kg的剂量对大鼠的体温没有影响。根据我们的临床前研究，(E/Z)-SIB-1893在自由活动的大鼠中以剂量依赖的方式产生低体温。[1] 在这项测试中，SIB 1893（10和20 mg/kg；小鼠；i.p.）并不影响丙戊酸、乙琥胺、苯巴比妥和氯硝西泮的保护作用。SIB 1893与传统抗癫痫化合物的联合治疗并未引起运动障碍。仅在与苯巴比妥联合使用时观察到长期记忆障碍。[2] |
| Synonyms | SIB 1893 |
| molecular weight | 195.26 |
| Molecular formula | C14H13N |
| CAS | 6266-99-5 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90.0 mg/mL (460.9 mM), Sonication is recommended. |
| References | 1. Łuszczki JJ, et al. Non-competitive metabotropic glutamate subtype 5 receptor antagonist (SIB-1893) decreases body temperature in rats. Pharmacol Rep. 2005;57(6):795-801. 2. Borowicz KK, et al. Influence of SIB 1893, a selective mGluR5 receptor antagonist, on the anticonvulsant activity of conventional antiepileptic drugs in two models of experimental epilepsy. Pol J Pharmacol. 2003;55(5):735-740. 3. Storto M, et al. Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice. J Hepatol. 2003;38(2):179-187. 4. O'Leary DM, et al. Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism. Br J Pharmacol. 2000;131(7):1429-1437. |