Endocannabinoid reuptake inhibitor
Encyclopedia
Endocannabinoid reuptake inhibitors (eCBRI), similar to cannabinoid reuptake inhibitors (CBRI), are substances which limit or completely stop the reabsorption of endocannabinoid neurotransmitters into their corresponding pre-synaptic neurones.
and Cannabidiol
. 'Endo' is a prefix used to describe a cannabinoid that is naturally found within an animal. In retrospect, an endocannabinoid reuptake inhibitor is a substance that when ingested by an animal prevents its natural cannabinoids from being reabsorbed into the neurones they come from.
. Following the increase of neurotransmission in the endocannabinoid system is the stimulation of its functions which, in humans, include: suppression of pain perception (analgesia), increased appetite
, mood
elevation and inhibition of short-term memory
.
. A study done in 2004 on rats with thyroid tumors showed that reuptake inhibition of the endocannabinoid system using VDM-11
and AA-5-HT reduced the ultimate size of the tumors in the treated rats. These findings suggest that the use of cannabinoids and/or eCBR inhibitors could be used to effectively treat tumors and/or cancer, which only adds to the controversy around cannabinoids and the cannabis plant as medicine.
As one might expect, combining a cannabinoid receptor antagonist
with an eCBRI reverses the effects of the reuptake inhibitor, and therefore could hinder treatment. Cannabinoid receptor antagonists aren't something common, so normally this isn't something to worry about. But if smoked cannabis or cannabis extract is to be used as a treatment, it would be necessary to cultivate varieties with little to no amounts of these compounds, as they are found in low concentrations in most varieties. One example of these antagonist compounds which is found in the cannabis plant is THCV (tetrahydrocannabivarin).
Etymology
There are several parts to the phrase endocannabinoid reuptake inhibitor. Firstly, a reuptake inhibitor is a substance that prevents its respective neurotransmitters from being reabsorbed into the pre-sypnatic neurones, which makes them continually recycle themselves, thus creating a large increase in neurotransmission. Next, a cannabinoid is simply a class of closely related substances such as TetrahydrocannabinolTetrahydrocannabinol
Tetrahydrocannabinol , also known as delta-9-tetrahydrocannabinol , Δ1-THC , or dronabinol, is the main chemical psychoactive substance found in the cannabis plant. It was first isolated in 1964. In pure form, it is a glassy solid when cold, and becomes viscous and sticky if warmed...
and Cannabidiol
Cannabidiol
Cannabidiol is a cannabinoid found in Cannabis. It is a major constituent of the plant, representing up to 40% in its extracts.It has displayed sedative effects in animal tests...
. 'Endo' is a prefix used to describe a cannabinoid that is naturally found within an animal. In retrospect, an endocannabinoid reuptake inhibitor is a substance that when ingested by an animal prevents its natural cannabinoids from being reabsorbed into the neurones they come from.
Pharmacology
The inhibition of endocannabinoid reuptake raises the amount of those neurotransmitters available in the synaptic cleft and therefore increases neurotransmissionNeurotransmission
Neurotransmission , also called synaptic transmission, is the process by which signaling molecules called neurotransmitters are released by a neuron , and bind to and activate the receptors of another neuron...
. Following the increase of neurotransmission in the endocannabinoid system is the stimulation of its functions which, in humans, include: suppression of pain perception (analgesia), increased appetite
Appetite
The appetite is the desire to eat food, felt as hunger. Appetite exists in all higher life-forms, and serves to regulate adequate energy intake to maintain metabolic needs. It is regulated by a close interplay between the digestive tract, adipose tissue and the brain. Decreased desire to eat is...
, mood
Mood
Mood may refer to:*Mood , a relatively long lasting emotional state*Grammatical mood, one of a set of morphologically distinctive forms that are used to signal modality*Mood , a city in Iran*Mood District, a district in Iran...
elevation and inhibition of short-term memory
Memory
In psychology, memory is an organism's ability to store, retain, and recall information and experiences. Traditional studies of memory began in the fields of philosophy, including techniques of artificially enhancing memory....
.
Use in medicine
Other than toxicity research and recreational use, eCBRIs could have some potential in fighting tumors and possibly cancerCancer
Cancer , known medically as a malignant neoplasm, is a large group of different diseases, all involving unregulated cell growth. In cancer, cells divide and grow uncontrollably, forming malignant tumors, and invade nearby parts of the body. The cancer may also spread to more distant parts of the...
. A study done in 2004 on rats with thyroid tumors showed that reuptake inhibition of the endocannabinoid system using VDM-11
VDM-11
VDM-11 is a potent cannabinoid reuptake inhibitor. It is light-sensitive and therefore must be stored within an inert gas such as argon, in a dark place and at an ideal temperature of -20ºC. This gold-colored substance is rarely found outside research laboratories.-See also:* Endocannabinoid...
and AA-5-HT reduced the ultimate size of the tumors in the treated rats. These findings suggest that the use of cannabinoids and/or eCBR inhibitors could be used to effectively treat tumors and/or cancer, which only adds to the controversy around cannabinoids and the cannabis plant as medicine.
As one might expect, combining a cannabinoid receptor antagonist
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
with an eCBRI reverses the effects of the reuptake inhibitor, and therefore could hinder treatment. Cannabinoid receptor antagonists aren't something common, so normally this isn't something to worry about. But if smoked cannabis or cannabis extract is to be used as a treatment, it would be necessary to cultivate varieties with little to no amounts of these compounds, as they are found in low concentrations in most varieties. One example of these antagonist compounds which is found in the cannabis plant is THCV (tetrahydrocannabivarin).
List of various eCBR / CBR Inhibitors
- AM404AM404AM404, also known as N-arachidonoylethanolamide, is an active metabolite of paracetamol , responsible for all or part of its analgesic action.-Pharmacology:...
- O-2093
- OMDM-2
- UCM-707
- VDM-11VDM-11VDM-11 is a potent cannabinoid reuptake inhibitor. It is light-sensitive and therefore must be stored within an inert gas such as argon, in a dark place and at an ideal temperature of -20ºC. This gold-colored substance is rarely found outside research laboratories.-See also:* Endocannabinoid...
See also
- Endocannabinoid systemEndocannabinoid systemThe endocannabinoid system refers to a group of neuromodulatory lipids and their receptors that are involved in a variety of physiological processes including appetite, pain-sensation, mood, and memory; it mediates the psychoactive effects of cannabis and, broadly speaking, includes:* The...
- Reuptake inhibitorReuptake inhibitorA reuptake inhibitor , also known as a transporter blocker, is a drug that inhibits the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron, leading to an increase in the extracellular concentrations of the neurotransmitter and therefore an...
- Cannabinoid receptor antagonistCannabinoid receptor antagonistThe discovery of the endogenous cannabinoid system led to the development of CB1 receptor antagonists. The first cannabinoid receptor "antagonist," rimonabant, was described in 1994. Rimonabant blocks the CB1 receptor selectively and it has been shown to decrease food intake and regulate...