| Bioactivity | NNC 05-2090 is a potent inhibitor of mGAT2, with a Ki of 1.4 μM. Anticonvulsant properties[1]. |
| Invitro | NNC 05-2090呈剂量依赖性，对DBA/2小鼠的声诱发强直和阵挛惊厥有抑制作用，其ED50值为19 μmol/kg[2]。NNC 05-2090呈剂量依赖性，在最大电休克（MES）实验中拮抗强直后肢扩展反应，其ED50值为73 mmol/kg[2]。NNC 05-2090在最高剂量（72-242 mmol/kg）明显（P<0.05）降低了全身性癫痫的严重程度（癫痫分级为3-5级），并且在这些剂量下NNC 05-2090也显著缩短了后放电持续时间（P<0.05）[2]。 |
| Name | NNC 05-2090 |
| CAS | 184845-43-0 |
| Formula | C27H30N2O2 |
| Molar Mass | 414.54 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. C Thomsen, et al. 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br J Pharmacol. 1997 Mar;120(6):983-5. [2]. N O Dalby, et al. Anticonvulsant properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 1997 Jul;28(1):51-61. |