842131-33-3
842131-33-3 結(jié)構(gòu)式
基本信息
中文別名
化合物 T17202 英文別名
TZP 101UliMorelin
(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
常見問題列表
生物活性
Ulimorelin (TZP-101) 是生長素釋放肽受體 (GRLN) 激動(dòng)劑，EC50 為 29 nM，Ki 為 16 nM。Ulimorelin 是一種促運(yùn)動(dòng)劑，通過競爭性拮抗 α1-腎上腺素受體引起血管舒張。Ulimorelin 可以刺激腸蠕動(dòng)，可用于營養(yǎng)不良。體內(nèi)研究
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. |