scholarly journals GIP Receptor Agonism Attenuates GLP-1 Receptor Agonist Induced Nausea and Emesis in Preclinical Models

Diabetes ◽  
2021 ◽  
pp. db210459
Author(s):  
Tito Borner ◽  
Caroline E. Geisler ◽  
Samantha M. Fortin ◽  
Richard Cosgrove ◽  
Jorge Alsina Alsina-Fernandez ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Preclinical Models ◽  
Nausea And Emesis ◽  
Gip Receptor

scholarly journals The dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide: a novel cardiometabolic therapeutic prospect

2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Enrique Z. Fisman ◽  
Alexander Tenenbaum
Keyword(s):  
Receptor Agonist ◽  
Therapeutic Option ◽  
Insulin Response ◽  
Glucagon Secretion ◽  
Long Term Effects ◽  
Glucose Levels ◽  
Lower Glucose ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1 ◽  
Gip Receptor

AbstractIncretin hormones are peptides released in the intestine in response to the presence of nutrients in its lumen. The main incretins are glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). GLP-1 stimulates insulin secretion, inhibits glucagon secretion at pancreatic α cells and has also extrapancreatic influences as slowing of gastric emptying which increases the feeling of satiety. GIP is the main incretin hormone in healthy people, causative of most the incretin effects, but the insulin response after GIP secretion in type 2 diabetes mellitus (T2DM) is strongly reduced. Therefore, in the past GIP has been considered an unappealing therapeutic target for T2DM. This conception has been changing during recent years, since it has been reported that resistance to GIP can be reversed and its effectiveness restored by improving glycemic control. This fact paved the way for the development of a GIP receptor agonist-based therapy for T2DM, looking also for the possibility of finding a combined GLP-1/GIP receptor agonist. In this framework, the novel dual GIP and GLP-1 receptor agonist tirzepatide seems to be not just a new antidiabetic medication. Administered as a subcutaneous weekly injection, it is a manifold single pharmacological agent that has the ability to significantly lower glucose levels, as well as improve insulin sensitivity, reduce weight and amend dyslipidemia favorably modifying the lipid profile. Tirzepatide and additional dual GLP-1/GIP receptor agonists that could eventually be developed in the future seem to be a promising furthest advance for the management of several cardiometabolic settings. Obviously, it is too early to be overly hopeful since it is still necessary to determine the long-term effects of these compounds and properly verify the potential cardiovascular benefits. Anyway, we are currently facing a novel and very appealing therapeutic option.

The Novel Dual GLP-1/GIP Receptor Agonist DA-CH5 Is Superior to Single GLP-1 Receptor Agonists in the MPTP Model of Parkinson’s Disease

2020 ◽  
Vol 10 (2) ◽  
pp. 523-542 ◽  
Author(s):  
Lingyu Zhang ◽  
Liping Zhang ◽  
Yanwei Li ◽  
Lin Li ◽  
Josefine Ulrikke Melchiorsen ◽  
...  
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Receptor Agonist ◽  
The Novel ◽  
Receptor Agonists ◽  
Mptp Model ◽  
Gip Receptor

scholarly journals The dual GLP‐1/GIP receptor agonist DA4‐JC shows superior protective properties in the APP/PS1 mouse model of Alzheimer’s disease

2020 ◽  
Vol 16 (S9) ◽  
Author(s):  
Mark Maskery ◽  
Simon Gengler ◽  
Elizabeth Mary Goulding ◽  
Josefine Ulrikke Melchiorsen ◽  
Mette M. Rosenkilde ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Mouse Model ◽  
Receptor Agonist ◽  
Protective Properties ◽  
Model Of Alzheimer’S Disease ◽  
Gip Receptor

CB 1 cannabinoid receptor agonist mouse VD-hemopressin(α) produced supraspinal analgesic activity in the preclinical models of pain

2018 ◽  
Vol 1680 ◽  
pp. 155-164 ◽  
Author(s):  
Ting Zheng ◽  
Run Zhang ◽  
Ting Zhang ◽  
Meng-Na Zhang ◽  
Biao Xu ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Preclinical Models

scholarly journals A GIP Receptor Agonist Exhibits β-Cell Anti-Apoptotic Actions in Rat Models of Diabetes Resulting in Improved β-Cell Function and Glycemic Control

PLoS ONE ◽  
2010 ◽  
Vol 5 (3) ◽  
pp. e9590 ◽  
Author(s):  
Scott B. Widenmaier ◽  
Su-Jin Kim ◽  
Gary K. Yang ◽  
Thomas De Los Reyes ◽  
Cuilan Nian ◽  
...  
Keyword(s):  
Glycemic Control ◽  
Receptor Agonist ◽  
Cell Function ◽  
Β Cell ◽  
Rat Models ◽  
Β Cell Function ◽  
Gip Receptor

679-P: The Novel GIP, GLP-1, and Glucagon Triple Receptor Agonist LY3437943 Exhibits Robust Efficacy in Preclinical Models of Obesity and Diabetes

Diabetes ◽  
2021 ◽  
Vol 70 (Supplement 1) ◽  
pp. 679-P
Author(s):  
TAMER COSKUN ◽  
JULIE S. MOYERS ◽  
WILLIAM C. ROELL ◽  
LIBBEY O’FARRELL ◽  
AJIT REGMI ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
The Novel ◽  
Preclinical Models ◽  
Obesity And Diabetes
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