| Identification | Back Directory | [Name]
TZP 101 | [CAS]
842131-33-3 | [Synonyms]
TZP 101
UliMorelin
(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 | [Molecular Formula]
C30H39FN4O4 | [MDL Number]
MFCD19443750 | [MOL File]
842131-33-3.mol | [Molecular Weight]
538.653 |
| Hazard Information | Back Directory | [Uses]
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[1][2][3]. | [Definition]
ChEBI: Ulimorelin is an oligopeptide. | [in vivo]
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[1].
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[1].
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[3].
| Animal Model: | Male Sprague-Dawley rats[1] | | 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. |
| [IC 50]
α adrenergic receptor | [References]
[1] Pustovit RV, et al. The?mechanism?of?enhanced?defecation?caused?by the?ghrelin?receptor?agonist,?ulimorelin. Neurogastroenterol Motil.?2014 Feb;26(2):264-71. DOI:10.1111/nmo.12259
[2] Broad J, et al. Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. Eur J Pharmacol.?2015?Apr 5;752:34-9. DOI:10.1016/j.ejphar.2015.02.005
[3] Hoveyda HR, et al. Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I): Development of ulimorelin (TZP-101) from hit to clinic. J Med Chem. 2011 Dec 22;54(24):8305-20. DOI:10.1021/jm2007062 |
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