THC Flashcards
THC effects
many – analgesic; euphoriant or sedative; anxiolytic or anxiogenic; appetite stimulant; hallucinogen
Possible clinical use of THC
glaucoma (THC reduces intraocular pressure); anorexia; and to reduce nausea associated with chemotherapy.
What is the most pharmacologically active compound in cannabis?
Delta-9 THC
Where is THC metabolized?
Metabolized by liver, becomes 11-hydroxy-delta9 THC. This metabolite is psychoactive, and fat soluble
What is the half life of THC?
Very long ½ life of 20-96 hr for THC, about 50 hr for some of its metabolites
What receptors does cannabis act on?
Acts in the brain at a CB-1 receptor; presynaptic; reduces Ca2+ influx to reduce neurotransmitter release
Where are endocannabainoids produced?
Post-synaptically
How does THC exactly work at the CB-1 receptor?
Receptor is linked to G-proteins; some directly decrease Ca2+ influx; others increase K+ currents via change in cAMP (second messenger)
Why are there cannabinoid receptors in the brain?
Because there are endocannabinoids; best known is anandamide; implicated in brain control of stress, pain and nausea, and learning (LTP)
What is the consequence of there being more CB1 receptors in GABA terminals than glutamate ?
means GABA terminals are going to be more responsive for low level CB1 agonism and thus there is more GABA antagonism. When you ingest THC, you end up antagonizing GABA.
Acomplia
CB1 inverse agonist. A subgroup of people taking it became so anxious and stressed out, that they committed suicide.
