A Look At The Influence Of CBG On Alpha Adrenoreceptors

Uncovering CBG’s Impact on Alpha Adrenoreceptors: A Deep Dive into the Science

CBG, or cannabigerol, is a lesser-known but increasingly studied cannabinoid found in the cannabis plant. Unlike its more well-known counterparts like Δ9-THC and CBD, CBG is considered a precursor molecule, serving as the building block for other common phytocannabinoids. 

Despite its unique origins, CBG has exhibited properties similar to Δ9-THC and CBD, specifically in its interactions with cannabinoid receptors. However, about CBG on alpha adrenoreceptors, CBG also stands out for its distinct effects on α-1 and α-2 adrenoceptors.

A growing body of research suggests that CBG may have therapeutic benefits for certain neurological and inflammatory disorders, digestive issues, pain, and blood pressure, as well as showing promise as an antibacterial agent. 

As the interest in CBG continues to grow, it is crucial to explore further its pharmacology, potential uses, and potential hazards. In this examination, we explore CBG’s role as an agonist of α-1 and α-2 adrenoceptors and the potential therapeutic role CBG could play due to this interaction.

Cannabinoids in Medicine 

The use of Cannabis sativa, or marijuana, for therapeutic and medicinal purposes can be traced back to ancient civilizations. Historically, it was used to treat various ailments, such as gout, malaria, digestive disorders, and menstrual pain. 

Western medicine also recognized the potential benefits of marijuana, with William O’Shaughnessy introducing its use for treating rheumatism and seizures. However, the use of medicinal marijuana declined and was eventually banned by the Controlled Substances Act of 1970.

Since the ban, only a limited amount of cannabinoid drugs have been authorized for human use – nabilone in 1985, dronabinol in 1986, and Sativex, available exclusively in Europe since 2010. More recently, however, Epidiolex was approved for limited medical use in 2018. 

Despite the limited number of approved drugs, a growing number of countries have legalized the use of medical marijuana for treating various medical conditions. However, the evidence supporting marijuana as a medicine is often based on anecdotal or small studies.

The Formation or Production of CBG

Despite being naturally present in the hemp and cannabis plants, Cannabigerol (CBG) is more commonly produced through a complex synthesis process. 

The steps required to make CBG often starts with the utilization of precursor molecules such as geranyl-pyrophosphate and olivetolic acid. Combined under the right conditions, these two forms of cannabigerolic acid (CBGA).

Cannabigerolic acid (CBGA) plays a vital role in forming other cannabinoids found in the cannabis plant. Through a series of chemical reactions, CBGA is converted into Δ9-tetrahydrocannabinolic acid (Δ9-THCA), cannabidiolic acid (CBDA), and cannabichromenic acid.

While CBGA is present in small amounts in most cannabis strains, certain strains have been known to have higher concentrations due to the suppression of specific synthesis enzymes. Furthermore, all cannabinoids, including CBG, are initially produced in an acidic form and must be decarboxylated by heat to activate their medicinal properties.

Growing Interest in Cannabinoid Pharmacology is Leading to Incredible Breakthroughs in Science 

With the recent deregulation of hemp-derived cannabinoids like CBD, CBG, cannabichromene (CBC), and cannabinol, there has been an increase in the study of their pharmacology. Each of these compounds has unique effects on the body despite having CBG as a common precursor.

For example, Δ9-THC produces a euphoric feeling and stimulates appetite. At the same time, CBD is not euphoric and is believed to have anti-epileptic and anti-inflammatory properties (among other use cases).

However, much is still to learn about the less-studied CBG and CBC. Still, it is expected that they have distinct pharmacological properties due to their different chemical structures. Despite the growing interest in cannabinoid pharmacology, most research has focused on Δ9-THC and CBD, leaving other cannabinoids largely unexplored.

The Unique Pharmacologic Properties of CBG

CBG is unique in its pharmacological properties as it sits between Δ9-THC and CBD. Research has shown that CBG has a lower binding affinity to CB1/CB2 receptors than Δ9-THC but is more similar to Δ9-THC than CBD. 

According to a 2012 study by Granja et al., CBG displayed minimal binding capabilities when tested on human cell cultures regarding CB1 and CB2 receptors. Despite this, further research is necessary to fully comprehend the in vivo effects and function of CBG on cannabinoid receptors.

CBG has also been found to be a highly effective agonist at the α-2 adrenoceptor, with a nanomolar to sub-nanomolar affinity (Cascio et al., 2010). These areas of knowledge gaps are crucial to be studied further.

The Influence of CBG on Alpha Adrenoreceptors

Research published in the British Journal of Pharmacology demonstrates that cannabigerol can interact with alpha(2)-adrenoceptors, bind to cannabinoid CB(1) and CB(2) receptors, and also exhibit antagonist activity towards CB(1) and 5-HT(1A) receptors.

Similarly, the influence of CBG on alpha adrenoreceptors particularly a-1 and a-2 receptors may also influence other catecholamines, such as dopamine. Current research studying alpha-receptor stimulation’s therapeutic applications focuses on potential benefits such as improved blood pressure, sedation, digestive responses, pain relief, and more. 

What does this mean for you?

On the topic, the influence of CBG on alpha adrenoreceptors, alpha-adrenoreceptors are partly responsible for neurotransmissions, the regulation of the sympathetic nervous system, and the activation of neurotransmitters, including epinephrine and norepinephrine.

Alpha 1-adrenergic receptors are also responsible (in part) for the contraction and stimulation of smooth muscles and several metabolic processes. In this way, CBG is thought to increase physical and mental alertness and energy and aid in digestive issues and digestion through influences on certain smooth muscle tissues.

Unlike ‘stimulants,’ it is thought that CBG’s role at a-1 receptors may aid in mediating dopamine release (the ‘feel good’ hormone). This may aid in boosting energy while also improving mood and dampening any symptoms of anxiety often associated with traditional stimulants.

At the a-2 receptor, CBG may influence its capacity to suppress the activity of the sympathetic nervous system via its Gi (inhibitory) activity. This may translate to a sense of calm and well-being, reducing stress.

Current medical research looking at a-2 agonists has focused on their ability to produce sedative, anti-hypertensive (lower blood pressure), and analgesic (pain-relieving) functions. Although more research is necessary, CBG may prove to be a good candidate for all or one of these use cases.

Summary Discussion 

The studies mentioned and a growing body of evidence have demonstrated CBG’s potential as a therapeutic or medicinal aid to improve health and wellness for millions of individuals worldwide.

Although more research is necessary, the current body of scientific literature supports that CBG may be effective as:

• A neuroprotective agent to prevent loss of cognitive ability as we age 
• Neuromodulation may be effective in treating diseases such as Parkinson’s or multiple sclerosis 
• Improved tissue recovery and healing concerning gastrointestinal issues 
• Reduced inflammation – which may be helpful for those with chronic conditions 
• Improvements in metabolic syndrome (i.e., diabetes); and
• As an antibacterial agent 
• Muscle relaxation 
• And more…

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