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编 号:F611086
分子式:C30H39FN4O4
分子量:538.65
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生物活性:
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.

体内研究:
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 Cmax of 0.39 μM and a AUC of 82 μM?min for rats. Ulimorelin (i.v.; 2 mg/kg) has a T1/2 of 50 mins, a CL of 24 mL/min/kg, and a Vss 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.
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