The endocannabinoid system Flashcards
Cannabis sativa produce?
About 70 compounds which are chemically related to delta9-THC (tetrahydrocannabinol)
Cannabinoids?
Chemically related to tetrahydrocannbinol that is produced from cannabis sativa
Marijuana and hashish are?
Causes what effect?
Cannabis product
Psychotropic effects
Attributes to delta9-THC
Drug harm potential?
Dependent on the scientific dependence of it.
Illustrated in a harm vs addictive graph.
Cannabis is less harmful than alcohol
Localisation of cannabinoids binding sites?
The molecules in the cannabis binds to receptors.
The receptors they bind to are distributed throughout the brain including the cerebellum and hippocampus.
The large range of receptors they bind to means?
These drugs mediate a variety of different brain systems
Can modulate a variety of processes
CB1?
Mainly in CNS and some peripheral tissue such as adipose tissue, heart and liver.
Couple ot Gi/o family and inhibit adenylate cyclase activity upon activation.
CB1 receptor activation modulates calcium or potassium condutance
What does the CB1 receptor modulate?
Supresses neuronal excitability and neurotransmitter release
Modulates NO production
Na channel conductance
CB2?
Primarily in cells of the immune system, in the spleen, tonsils and thymus.
Couple to Gi/o and inhibit adenylate cyclase activity upon activation
CB1 and CB2 receptor formation?
7TMs domains.
GPCR.
CB3?
Evidence suggest this unknown receptor exists
CB1 receptor distribution in the brain?
Distribution suggest high or exclusive expression in GABAergic cell.
Sections of the basal ganglia and hippocampus
GABAergic cells?
Cells that synthessi GABA
Involved in inhibition
Endocannabinoids metabolism?
AS10
Dedegration reactions
DSI?
Depolarisation-induced suppression of inhibition
IPSP on a CA1 hippocampal cell are inhibited for a brief period following stimulation.
Modulatated by CB1
Retrograde signalling?
Retrograde transmission of endocannbinoids to the presynpatic receptor
Inhibits calcium influx and decreases GABA release.
Name the 3 neurotransmission strategies?
Retrograde: normal chemical synpase
Bidirectional: electrical synpase
Anterograde: endocannabinoid-mediated
AS11
Retrograde signaling by endocannabinoids?
Anterograde.
Act on the GABAergic synpase and GLUTergic synpase.
AS12
Name the 7 chronic effects on endocanniboids?
- Respiration
- Cardiovascular
- Immune system
- Reproduction
- Emotion
- Intellect
- Psychological
What are the acute effects of endocannabinoids?
The stimulation leads to tranquility
Impaired short-term memory and learning
Anxiety, fear and pain at high dosage.
Sedation
DSI stands for?
depolarised-induced suppression of inhibition
AS12
DSE stands for?
Depolarisation-induced suppression of excitation
Role of the endocannbinoid system?
Important in the fear, anxiety and panic.
Can do a auditory fear conditioning test model in rodents
ECS and food?
Increases appetite.
Therefore can make an antagonist drug to suppress appetite.
Effects of CB1 stimualtion?
Increase insulin resistance.
Decrease HDL-cholesterol.
Increase in triglerides
Decrease in glucose uptake.
Decrease in adiponectine.
Food is eaten for its gustatory rewarding properties
Rimonabant?
Effective and promising drug.
Inverse agonist of the CB1 receptor.
Produces consistent weight loss.
Why is an inverse agonist of CB1 not a good drug to use?
As CB1 is a pleiotropic target
Therefore it adversely affecting all the other neuronal controlled systems.
Analgesic effect of ECS?
Rebound hyperalgesia: wont feel pain until the effects leave and will have a rebound pain (which will be must higher than the original)
Potential for abuse (the same with all opioid-based analgesics)
What is it called when 2AG is converted to glycerol and arachildonic acid?
MAGL
