| Bioactivity | Lupanine (D-Lupanine) is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM[1]. |
| Target | Ki: 500 nM (Nicotinic receptor) and 11000 nM (Muscarinic receptor) |
| Invitro | Lupanine 对烟碱受体具有结合亲和力，Ki 值为 500 nM。而 Lupanine 对毒蕈碱受体的亲和力非常弱，Ki 值为 11000 nM[1]。Lupanine (0-100 μM) 是 SH-SY5Y 细胞的弱激动剂和脱敏剂，EC50 和 DC50 分别为 10.7 μM 和 28.2 μM[2]。 |
| In Vivo | Lupanine (腹腔注射 100-300 毫克/千克；口服 175-700 毫克/千克) 在 EOPS 雄性瑞士小鼠 (20-22 克) 和哈特利豚鼠 (400-500 克) 中单次注射的毒性要小得多[1]。Lupanine (1-7.5 mg/kg；i.v.) 比 Sparteine 更有效地对抗颈动脉闭塞引起的继发性反射性高血压和刺激肺胃神经引起的猫狗低血压[1]。Lupanine 对阿托品治疗的狗注射乙酰胆碱 (500 pg/kg i.v.) 引起的烟碱型高血压有抑制作用[1]。 |
| Name | Lupanine |
| CAS | 550-90-3 |
| Formula | C15H24N2O |
| Molar Mass | 248.36 |
| 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]. K Yovo, et al. Comparative pharmacological study of sparteine and its ketonic derivative lupanine from seeds of Lupinus albus. Planta Med. 1984 Oct;50(5):420-4. [2]. Green BT, et al. Anagyrine desensitization of peripheral nicotinic acetylcholine receptors. A potential biomarker of quinolizidine alkaloid teratogenesis in cattle. Res Vet Sci. 2017 Dec;115:195-200. |