Endocrine effects of the novel ghrelin receptor inverse agonist PF-5190457: Results from a placebo-controlled human laboratory alcohol co-administration study in heavy drinkers.
Clicks: 250
ID: 55169
2019
Both animal and human work suggests that the ghrelin system may be involved in the mechanisms that regulate the development and maintenance of alcohol use disorder. Previously, in a Phase 1b study, we tested pharmacological blockade of the growth hormone secretagogue receptor 1a (GHS-R1a, also known as the ghrelin receptor), in heavy drinking individuals with PF-5190457, an orally bioavailable, potent and selective GHS-R1a inverse agonist. We report here the effects of PF-5190457 on endocrine blood concentrations of amylin, gastric inhibitory polypeptide, glucagon-like peptide 1, insulin, leptin, pancreatic polypeptide, peptide YY, thyroid stimulating hormone, free triiodothyronine (T3), thyroxine (T4), cortisol, prolactin, and glucose during PF-5190457 dosing, as compared to placebo, in absence of alcohol as well as during an alcohol challenge when PF-5190457 was on steady-state. Blood hormone levels were largely unaffected by PF-5190457, both during dosing and in the context of alcohol challenge. The relevance of these findings to the use of PF-5190457 as a probe for endogenous ghrelin signaling in alcohol use disorder is discussed. CLINICALTRIALS.GOV: NCT02039349.
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lee2019endocrineneuropharmacology
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| Authors | Lee, Mary R;Farokhnia, Mehdi;Cobbina, Enoch;Saravanakumar, Anitha;Li, Xiaobai;Battista, Jillian T;Farinelli, Lisa A;Akhlaghi, Fatemeh;Leggio, Lorenzo; |
| Journal | Neuropharmacology |
| Year | 2019 |
| DOI | S0028-3908(19)30346-6 |
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