中文名 | aspergillimide |
英文名 | aspergillimide |
别名 | 曲霉酰亚胺 |
英文别名 | aspergillimide (rel)-Asperparaline A Spiro[5H,6H-5a,9a-(iminomethano)-1H-cyclopent[f]indolizine-7(8H),3'-pyrrolidine]-2',5',10-trione, tetrahydro-1,1',8,8,11-pentamethyl-, (1R,3'R,5aR,8aR,9aS)-rel-(-)- |
CAS | 195966-93-9 |
化学式 | C20H29N3O3 |
分子量 | 359.46256 |
密度 | 1.30±0.1 g/cm3(Predicted) |
沸点 | 546.1±50.0 °C(Predicted) |
酸度系数 | 8.68±0.60(Predicted) |
体外研究 | Asperparaline A (1 μM; 1 min) markedly and reversibly blocks the acetylcholine (Ach; 10 µM)-induced current in the silkworm larval neurons. Asperparaline A (1-1000 nM; 1 min) differentially blocks the peak and slowly desensitizing currents, with IC 50 s of 20.2 and 39.6 nM, respectively. Asperparaline A (10 μM; 1 min) reduces the peak current amplitude of the ACh (100 µM)-induced response of α3β4 nAChR by 33.4%, while barely influencing the amplitudes of the responses to ACh of the α4β2 and α7 nAChRs in X. laevis oocytes. |
体内研究 | Asperparaline A (10 μg/g; p.o.) exhibits paralysis against silk worms within 1 h and lasts for 7 to 10 h. Asperparaline A (3 μg/g; injection with a micro-syringe) exhibits paralysis activity against silk worms within 20 min and lasts for 4 to 5 h. |