Cannabinoid Receptors Flashcards
Outline the steps taken and understanding the endocannabinoid system
Cannabinoid receptor discovery
Synthesis of specific agonists and antagonists
Discovery of the Endo cannabinoid system
True or false: cannabinoids are highly hydrophilic
False, they are highly lipophilic
How were cannabinoids first thought to exert their effects?
By disrupting the cell membrane in a non-specific manner
What were the two major findings related to the mechanism of cannabinoid action?
Cannabinoids act via G proteins
And the discovery of high affinity binding sites for cannabinoid molecules
When was Delta nine THC identified as the primary psychoactive component of cannabis?
1964
When was the CB1 receptor identified?
1988
When was the CB1 receptor cloned from a rat?
1990
When was the CB1 receptor cloned from a human?
1991
When was the CB2 receptor identified?
1993
Where are CB1 receptors located throughout the body? (Six)))
Brain
Liver
Reproductive system
Cardiovascular system
Skeletal muscle muscles
G.I. tract
Give examples of CB1 receptor function in the brain
Learning, memory, cognition
Motor control
Anxiety and depression
Appetite and food intake
Reward and addiction
Neuro protection
Neural development
Sleep
Give examples of CB1 receptor function in the liver
Ascites formation
Lipogenesis
Fibrosis
Insulin resistance
Give examples of CB1 receptor function in the reproductive system
Fertility regulation, embryo implantation
Embryonic development
Give example examples of CB1 receptor function in the cardiovascular system
Negative inotropy
Vasodilation
Cardiac function
Give example examples of CB1 receptor function in skeletal muscle
Energy metabolism
Muscle fibre formation
Give examples of CB1 receptor function in the G.I. tract
G.I. motility
Enteroendocrine function
Intestinal barrier function
Energy balance
Give examples of other CB1 receptor functions
Nociception
Immune modulation
Nausea and emesis
Intraocular pressure
Bone remodelling
Bronchodilation
Cancer
Is there a high or low concentration of cannabinoid receptors in the brain stem?
Low
What is a possible explanation as to why cannabis use is not associated with sudden death due to respiratory depression?
Due to the low concentration of receptors in the brain stem
What cannabinoid receptor is found predominantly in the central nervous system?
CB1
Where do CB2 receptors occur?
Immune system and other tissues, such as bone, adipose cells, and the G.I. tract.
What are some of the most abundant G protein linked receptors in the brain?
CB1 receptors
What does the localization of CB1 receptors mode of action suggest?
Primary function of these receptors might be to inhibit neurotransmitter release
What three things does CB1 receptor activation lead to and what is the overall effect of this?
Inhibition of cAMP
Inhibition of voltaGE sensitive calcium channels
Activation of potassium channel opening
These signalling events combined to exert a powerful inhibitory effect on neurotransmitter release