Advances in the development of nonpeptide small molecules targeting ghrelin receptor

G Giorgioni, F Del Bello, W Quaglia… - Journal of Medicinal …, 2022 - ACS Publications
Ghrelin is an octanoylated peptide acting by the activation of the growth hormone
secretagogue receptor, namely, GHS-R1a. The involvement of ghrelin in several …

Pharmacological GHSR (ghrelin receptor) blockade reduces alcohol binge-like drinking in male and female mice

RS Richardson, A Sulima, KC Rice, JA Kucharczk… - …, 2023 - Elsevier
Ghrelin is a peptide that is produced by endocrine cells that are primarily localized in the
stomach. Ghrelin receptors (GHSR) are expressed in the brain and periphery. Preclinical …

The role of ghrelin/GHS-R1A signaling in nonalcohol drug addictions

M Sustkova-Fiserova, C Charalambous… - International Journal of …, 2022 - mdpi.com
Drug addiction causes constant serious health, social, and economic burden within the
human society. The current drug dependence pharmacotherapies, particularly relapse …

Associations of early life stress with leptin and ghrelin in healthy young adults

TE Daniels, KJ Mathis, AP Gobin… - …, 2023 - Elsevier
Background Childhood adversity is a major risk factor for cardiometabolic health problems.
Stress-related changes in diet suggest a role for endocrine factors that influence dietary …

[HTML][HTML] A randomized, double-blind, placebo-controlled study of a GHSR blocker in people with alcohol use disorder

ML Faulkner, M Farokhnia, MR Lee, L Farinelli… - JCI …, 2024 - pmc.ncbi.nlm.nih.gov
BACKGROUND Studies have demonstrated the role of ghrelin in alcohol-related behaviors
and consumption. Blockade of the growth hormone secretagogue receptor (GHSR), which is …

Drug clearance by aldehyde oxidase: can we avoid clinical failure?

F Toselli, M Golding, J Nicolaï, E Gillent, H Chanteux - Xenobiotica, 2022 - Taylor & Francis
Despite increased awareness of aldehyde oxidase (AO) as a major drug-metabolising
enzyme, predicting the pharmacokinetics of its substrates remains challenging. Several drug …

[HTML][HTML] In vitro pharmacological characterization of growth hormone secretagogue receptor ligands using the dynamic mass redistribution and calcium mobilization …

C Sturaro, C Ruzza, F Ferrari, P Pola… - European Journal of …, 2024 - Elsevier
Ghrelin modulates several biological functions via selective activation of the growth
hormone secretagogue receptor (GHSR). GHSR agonists may be useful for the treatment of …

Differential response in ethanol behaviors of female rats given various weight loss surgeries

ER Orellana, MK Piscura, N Horvath… - Alcohol and …, 2021 - academic.oup.com
Aims Currently, the only effective treatment for morbid obesity and its comorbidities is weight
loss surgery (WLS). Growing evidence suggests that different types of WLS, such as Roux …

Mesolimbic exendin-4 attenuates reward salience evoked by neuropeptide Y and ghrelin

AM Brigande, JG Darwich, PJ Currie - Behavioural Brain Research, 2023 - Elsevier
In the present study, we investigated the effects of the glucagon-like peptide-1 (GLP-1)
agonist exendin-4 (Ex-4) on the stimulatory action of neuropeptide Y (NPY) and ghrelin …

Edinger-Westphal ghrelin receptor signalling regulates binge alcohol consumption in a sex specific manner

A Pearl, P Pinares-Garcia, A Shesham, X Maddern… - bioRxiv, 2024 - biorxiv.org
Background: Rates of risky drinking are continuing to rise, particularly in women, yet sex as
a biological variable has been largely ignored. An emerging yet understudied potential …