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From least to most THC
marijuana, sinsemilla, hashish, hash oil
What increased over time while other decreased?
THC percentage/potency increased, cannabidiol (CBD) decreased as CBD is psychotropically inactive
Gateway Hypothesis
marijuana and alcohol can lead to using more serious drugs, against changing schedule
Low vs high doses
relaxation vs excitation
Route of administration and differences
smoked and IV similar, short and immediate while oral is slower but longer
Synthetic cannabinoids (SCBs) vs THC
SCBs are direct agonists to cannabinoid receptors while THC are partial agonists
CB1 vs CB2
CB1 most abundant GPCR
CB1 mechanism
CB1 inhibits glutamate and inhibits GABA
CB1 acts on the pre or post synaptic terminal
pre
Glutamate mechanism
activates postsynaptic mGluR, stimulates 2-AG production via PLC-B and DGL, activates presynaptic CB1 receptors, decreases glutamate release, 2-AG action terminated by MGL/MAGL which converts 2-AG to arachidonic acid
Cannabis use decreases what
grey matter
GAT211 is a
positive allosteric modulator
AM251
CB1 receptor inverse agonist
AM374
FAAH enzyme blocker, elevated anandamide levels
AM404
anandamide tranport inhibitor
AM630
CB2 receptor inverse antagonist
CP55,940
high efficacy agonist at CB1 and CB2 receptors, more potent than THC
GAT211
CB1 receptor positive allosteric modulator
HU-210
CB1 receptor agonist (very potent)
Nabilone
THC partial CB1 receptor agonist
Spice/K2
synthetic high efficacy CB1 receptor agonist
SR141716A (Rimonabat)
inverse agonist at CB1, withdrawn due to suicide ideation side effects
WIN55,212-2
CB1 receptor high efficacy agonist
Opium
natural form
Opiate
derived from opium, morphine an example, NOT fentanyl, if not found in poppy, not an opiate
Opioid
all substances, overarching term
All receptors play a role in what but not what
analgesia not reward
most to least important receptors
mu, delta, kappa
Increasing Ca entry and K efflux
decreased likelihood of releasing neurotransmitter
Preferential form monomer vs dimer
monomer
Opioid is trying to activate or inhibit cAMP
inhibit cAMP
B-endorphins act on
MOR
Met-enkephalin and Leu-enkephalin act on
DOR mostly, sometimes MOR
Dynorphin A, B, and neoendorphin act on
KOR