| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T59604 | ||||
| Target Name | Growth hormone secretagogue receptor 1 (GHSR) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | TZP-101 | Drug Info | EC50 = 29 nM | [5] | |
| 4-(3-hexylureido)-N-phenylbenzenesulfonamide | Drug Info | IC50 = 4300 nM | [3] | ||
| AwFwLL-NH2 | Drug Info | IC50 = 15 nM | [2] | ||
| DprwFwLL-NH2 | Drug Info | IC50 = 210 nM | [2] | ||
| DwFwLL-NH2 | Drug Info | IC50 = 60 nM | [2] | ||
| HwFwLL-NH2 | Drug Info | IC50 = 58 nM | [2] | ||
| KwFwLL-NH2 | Drug Info | IC50 = 32 nM | [2] | ||
| QwFwLL-NH2 | Drug Info | IC50 = 120 nM | [2] | ||
| RPKPfQwFwLL-NH2 | Drug Info | IC50 = 3.2 nM | [2] | ||
| RQ-00000005 | Drug Info | IC50 = 3000 nM | [1] | ||
| RwFwLL-NH2 | Drug Info | IC50 = 12 nM | [2] | ||
| WFwGG-NH2 | Drug Info | IC50 = 540 nM | [2] | ||
| WFwLL-NH2 | Drug Info | IC50 = 530 nM | [2] | ||
| Action against Disease Model | TZP-101 | Drug Info | Previously we have shown in a rodent model of postoperative ileus that the synthetic ghrelin receptor agonist TZP-101 prevents the delay in gastric emptying and improves small intestinal transit. The goal of the present study was to investigate whether TZP-101 affects colonic transit and food intake in rats with postoperative ileus. TZP-101 (0.03-1 mg/kg) dose-dependently decreased the time to first bowel movement and increased fecal pellet output measured at 12 h and 24 h post-surgery compared to the vehicle. The administration of TZP-101 was not associated with a significant alteration in food intake. | [4] | |
| References | |||||
| REF 1 | Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues. Bioorg Med Chem Lett. 2000 Jan 3;10(1):5-8. | ||||
| REF 2 | Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. J Biol Chem. 2007 May 25;282(21):15799-811. | ||||
| REF 3 | Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6237-40. | ||||
| REF 4 | Effect of the ghrelin receptor agonist TZP-101 on colonic transit in a rat model of postoperative ileus. Eur J Pharmacol. 2009 Feb 14;604(1-3):132-7. | ||||
| REF 5 | Pharmacological demarcation of the growth hormone, gut motility and feeding effects of ghrelin using a novel ghrelin receptor agonist. Endocrinology. 2008 Dec;149(12):6280-8. | ||||
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