TZP 101
| 中文名称 | TZP 101 |
|---|---|
| 中文同义词 | 化合物 T17202;化合物 ULIMORELIN |
| 英文名称 | TZP 101 |
| 英文同义词 | TZP 101;(7R,10R,13S,16R)-13-cyclopropyl-7-[(4-fluorophenyl)methyl]-10,11,16-trimethyl-17-oxa-5,8,11,14-tetrazabicyclo[16.4.0]docosa-1(22),18,20-triene-6,9,12-trione;UliMorelin |
| CAS号 | 842131-33-3 |
| 分子式 | C30H39FN4O4 |
| 分子量 | 538.6534632 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 842131-33-3.mol |
| 结构式 |  |
TZP 101 性质
| 形态 | Solid |
|---|
Ulimorelin (TZP-101) 是生长素释放肽受体 (GRLN) 激动剂，EC50 为 29 nM，Ki 为 16 nM。Ulimorelin 是一种促运动剂，通过竞争性拮抗 α1-肾上腺素受体引起血管舒张。Ulimorelin 可以刺激肠蠕动，可用于营养不良。
Ulimorelin (TZP-101; 0.3-5 mg/kg; i.v.) causes a dose dependent increase in the numbers and amplitudes of phasic pressure waves recorded from the colorectum.
Ulimorelin (1, 3, 5 mg/kg; i.v.) causes a substantial and prolonged (~1 h) increase in colorectal propulsive activity and expulsion of colonic contents.
Ulimorelin (p.o.; 8 mg/kg) has a C
max
of 0.39 μM and a AUC of 82 μM•min for rats. Ulimorelin (i.v.; 2 mg/kg) has a T
1/2
of 50 mins, a CL of 24 mL/min/kg, and a V
ss
of 1.7 L/kg for rats.
| Animal Model: | Male Sprague-Dawley rats |
| Dosage: | 0.3, 1, 3, 5 mg/kg |
| Administration: | i.v. |
| Result: | Caused a dose dependent increase in the numbers and amplitudes of phasic pressure waves recorded from the colorectum. |