Ulimorelin
 | |
| Clinical data | |
|---|---|
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| KEGG | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C30H39FN4O4 |
| Molar mass | 538.664 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Ulimorelin (INN, USAN) (developmental code name TZP-101) is a drug with a modified cyclic peptide structure which acts as a selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR-1a).[1] Unlike many related drugs, ulimorelin has little or no effect on growth hormone (GH) release in rats.[2] However, like ghrelin and other ghrelin agonists, ulimorelin does stimulate GH release with concomitant increases in insulin-like growth factor 1 (IGF-1) in humans.[3] It has been researched for enhancing gastrointestinal motility, especially in gastroparesis[4] and in aiding recovery of bowel function following gastrointestinal surgery, where opioid analgesic drugs used for post-operative pain relief may worsen existing constipation.[5][6][7][8] While ulimorelin has been shown to increase both upper and lower gastrointestinal motility in rats,[8] and showed promising results initially in humans,[4][6] it failed in pivotal clinical trials in post operative ileus.[7]
A common side effect of ghrelin is reduced blood pressure. Ulimorelin has been shown to inhibit vasoconstriction of rat arteries in vitro elicited by the α1-adrenoceptors agonists phenylephrine and methoxamine, and to increase artery tension at high concentrations.[9] Effects on blood pressure, however, were not observed in human clinical trials.[4][7]
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.
