A Vasorelaxant is a substance or means by which tension in the vascular system is reduced, controlled, or eliminated. Vascular tension causing high blood pressure which then causes headaches, migraines, nausea, and anxiety as result of related pain.
Mechanism of Action: How CBD Works as a Vasorelaxant
Recent studies have investigated the underlying mechanisms through which CBD exerts vasorelaxant effects:
- Endocannabinoid System Interaction:
- CBD interacts with the endocannabinoid system (ECS), influencing CB1 and CB2 receptors as well as non-cannabinoid receptors.
- Although it has low affinity for these receptors directly, CBD modulates ECS activity, contributing to its vasorelaxant properties.
- Calcium Channel Modulation:
- CBD has been shown to impact calcium ion channels, which play a crucial role in muscle contraction. By reducing calcium influx into smooth muscle cells, CBD may induce relaxation of these muscles, leading to vasodilation.
- Activation of Transient Receptor Potential (TRP) Channels:
- CBD activates TRPV1 (vanilloid receptors), which are involved in the regulation of vascular tone. Activation of these channels can contribute to vasodilation and the relaxation of blood vessels.
- Nitric Oxide Pathway:
- Some studies suggest that CBD may enhance the production of nitric oxide (NO) in endothelial cells. Nitric oxide is a key molecule for vasodilation, helping relax the smooth muscle of blood vessels and improve blood flow.
Recent Studies Supporting CBD’s Vasorelaxant Effects
- Animal and Preclinical Studies:
- Research conducted on rat aortic rings has shown that CBD induces vasorelaxation in a concentration-dependent manner. This suggests that CBD can effectively relax blood vessels, potentially reducing blood pressure and improving circulation.
- Studies have indicated that CBD’s vasorelaxant effects may be partially mediated by the activation of TRP channels and the modulation of serotonin (5-HT1A) receptors, which can also play a role in vascular tone regulation.
- Human and Clinical Insights:
- While comprehensive human studies are still developing, early trials and observational studies point to CBD’s potential to help manage blood pressure. For example, a 2017 study published in the journal JCI Insight found that a single dose of CBD reduced resting blood pressure and the blood pressure response to stress in healthy volunteers.
- This reduction in blood pressure is believed to be due to CBD’s anxiolytic (anti-anxiety) and vasorelaxant properties, which help lower overall stress and cardiovascular strain.
Potential Benefits of CBD as a Vasorelaxant:
- Blood Pressure Regulation: By promoting vasodilation, CBD may help in the management of hypertension, a key risk factor for heart disease and stroke.
- Improved Circulation: Relaxed blood vessels facilitate better blood flow, which can enhance tissue oxygenation and nutrient delivery.
- Cardioprotective Effects: CBD’s potential to reduce oxidative stress and inflammation may provide further benefits to cardiovascular health, protecting against damage to blood vessel linings.
Limitations and Ongoing Research:
- Variability in Results: Some studies report varying results based on the dosage and specific conditions tested.
- Clinical Validation: While animal and preclinical studies provide promising evidence, more large-scale, double-blind, placebo-controlled clinical trials in humans are needed to confirm these findings and determine the appropriate dosing and safety.
Conclusion:
Recent studies support the potential of CBD as a vasorelaxant, showing that it can promote the relaxation of blood vessel walls and contribute to better blood flow and blood pressure management. Its effects are thought to be mediated by interactions with the endocannabinoid system, calcium channels, TRP channels, and the nitric oxide pathway. While promising, more human clinical studies are necessary to fully understand CBD’s vasorelaxant properties, optimal dosage, and long-term effects on cardiovascular health.
Christopher Stanley at the University Of Nottingham School Of Medicine has studied canabinoid receptors. In the study, he and his team activated cannabinoid receptors CB1 and CB2, along with transient receptor potential vanilloid one (TRPV1), peroxisome proliferator-activated receptor gamma (PPARᵧ) and the novel endothelial cannabinoid receptor (CBᶒ).
It was observed that, out of all the receptors involved in blood vessel constriction/activation, activation of CB1 receptors on endothelial (blood vessel) tissue helped to reduce stress on vessels that were constricted.
the action of vessels as they dilate and blood pressure reduces. The only instances when CB1 activation didn’t cause vasodilation of all the CB1 receptors was in males and in patients with type –2 diabetes or hypercholesterolemia (high levels of cholesterol).
The Study Results:
Of the 34 patients that were used in the study, 27 had cancer and 7 had inflammatory disorder. CBD that was given pre-constricted mesenteric arteries caused a vasorelaxation of 40%. When added to un-contracted arteries, CBD had no effect on baseline tone.
The study showed evidence on the effects of CBD on human mesenteric arteries that express CB1 activation. This suggested that CB1 is a target for CBD in human mesenteric vessels. A second antagonist (LY320135) was applied to the CB1 receptors, which also found to be an inhibitor of the response, also indicating CB1 receptor activation in vasorelaxation.
The endocannabinoid receptors proved to be an active component in blood vessel constriction and relaxation. In a constricted vessel, activation of CB1 receptors with CBD caused the vessels to relax and dilate; the desired response to increased blood pressure. The use of CBD can lead the way to providing an alternative and safer treatment for high blood pressure, an often fatal condition.