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TZP 101

Product NameTZP 101
CAS842131-33-3
MFC30H39FN4O4
MW538.6534632
EINECS
MOL File842131-33-3.mol

Chemical Properties

form

Solid

Usage And Synthesis

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 C_max of 0.39 μM and a AUC of 82 μMmin 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^[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. Themechanismofenhanceddefecationcausedby theghrelinreceptoragonist,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.2015Apr 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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