By Avni Dalal, ND
Our bodies rely on a delicate balance of hormones to regulate the numerous essential functions that take place, down to the second. One hormone receptor that has gained significant attention in recent years is the GLP-1 receptor. Found primarily in the gut (the distal intestine), α cells in the pancreas, and neurons of the central nervous system, this receptor plays a vital role in metabolic and hormonal balance that can support healthy glucose response throughout the body.* These hormones also help balance hunger, satiation, and energetics and thus affect metabolic processes for healthy glucose response.
Understanding GLP-1 receptors can offer valuable insights into how our bodies manage energy and why therapies targeting these receptors have become revolutionary for people managing metabolic challenges.1*
This article delves into what GLP-1 receptors are, how they work, and why they’re essential for our health.
What Are GLP-1 Receptors?
GLP-1 stands for glucagon-like peptide-1, a hormone produced when we consume food; this hormone is produced throughout the gut but also in the hypothalamus and brain in centers that affect food cravings.
This hormone interacts with GLP-1 receptors, which are specialized proteins located on the surfaces of certain cells throughout the body. These receptors act as “switches” that, when activated by certain nutrients and bitter compounds, set off a cascade of hormone release (insulin) which affects metabolic processes that influence healthy weight and glucose balance, including lowering serum glucose levels and controlling appetite by delaying gastric emptying.
GLP-1 receptors are concentrated in the following areas:
- Pancreas: GLP-1 stimulates insulin release, essential for balancing blood sugar after eating.1,2
- Brain/central nervous system: These receptors play a role in controlling appetite, making us feel full and less inclined to eat more.1,2
- Intestines: GLP-1 receptors slow the emptying of the stomach, promoting better blood sugar control and providing a more sustained release of nutrients into the small intestine.2
The Role of GLP-1 Receptors in Metabolic Regulation
One of the primary functions of GLP-1 receptors is to balance metabolic processes that include a normal glucose response. After eating, GLP-1 is released, stimulating insulin production.2 Insulin’s main purpose is to utilize blood sugar by enabling glucose to enter cells, where it is used for energy or stored for future use. At the same time, GLP-1 reduces the secretion of another hormone called glucagon, which typically raises blood sugar by prompting the liver to release stored glucose.1
Together, these actions help maintain a stable blood sugar level, particularly after meals. For individuals with conditions like type 2 diabetes, where blood sugar regulation is impaired due to insulin resistance, targeting GLP-1 receptors has been found to be a potentially effective strategy to improve glycemic control.3
Appetite Control and Weight Management
Beyond blood sugar regulation, GLP-1 receptors have a unique impact on appetite and weight management. When activated, these receptors in the brain enhance feelings of fullness and satisfaction, reducing the urge to eat.1,2 This satiety response can be beneficial for individuals who struggle with overeating or “food chatter,” as it naturally curbs the desire for excess calories.3
Additionally, GLP-1 slows down the process of emptying gastric content, meaning food moves more slowly from the stomach to the intestines. This can help prolong the feeling of fullness after eating and steadies the release of glucose (and other nutrients) into the bloodstream, supporting both weight management and blood sugar stability.1,2
Supporting Gut Health Through GLP-1 Receptors
Beyond metabolic support, GLP-1 receptors also play a role in maintaining gut health. The delayed gastric emptying effect promoted by GLP-1 ensures that nutrients are absorbed more gradually, which benefits the gut lining.4 GLP-1 also contributes to a more regulated and slower transit of nutrients to help modulate intestinal motility and reduce symptoms of diarrhea in some individuals.5
GLP-1 Receptor Agonists: Redefining Therapeutic Approaches
With the discovery of the benefits provided by GLP-1 receptors, scientists have developed medications that specifically target these receptors, known as GLP-1 receptor agonists. These medications are designed to mimic the natural effects of GLP-1 receptor activation and help people manage conditions like type 2 diabetes and obesity.1,2,3
These prescription drugs serve to release the hormone (GLP-1) that in turn releases insulin, which helps balance metabolic processes as well as glucose. Additionally, when GLP-1 receptors are activated in the brain by these drugs, the result is an increase of satiation, which can reduce the amount of food intake.
Its important to realize that food and nutrition as well as selected natural botanical plants are also able to activate GLP-1 receptors. When they do, the response also results in a release of insulin, which contributes to hormonal and metabolic balance. This is normally occurring every day in our diets. But when our bodies become resistant to the effects and benefits of the hormone response driven by GLP-1, the metabolic balance is altered. By using food and nutrients that can activate GLP-1 receptors, it’s then possible to elicit the same response as seen with prescription medications but at slower response times and of a less of a magnitude in result.
A final advantage of using a nutritional approach with dietary supplements is that these products are consumed orally and thus support a healthy digestive tract and can activate all the GLP-1 and bitter receptors through the gut. This then supports healthy digestive function and a balanced metabolic effect with few to very limited side effects.
Summary
GLP-1 receptors are a crucial part of our metabolic system, influencing blood sugar regulation, appetite control, and gut health. From exerting their effects on insulin release to impacting how full we feel after eating, these receptors have a wide-reaching impact on our health.
Exploring GLP-1 receptors offers valuable insights into the intricate mechanisms our body uses to maintain homeostasis, and as research continues, the future of GLP-1 focused treatments offers new options for improving metabolic and digestive health.*
References:
1. Zheng Z et al. Signal Transduct Target Ther. 2024;9(1):234.
2. Marathe CS et al. Diabetes Care. 2013;36(5):1396-1405.
3. Graaf Cd et al. Pharmacol Rev. 2016;68(4):954-1013.
4. Holst JJ et al. Br J Pharmacol. 2022;179(4):727-742.
5. Smits MM et al. Diabetes Obes Metab. 2016;18(3):224-235.