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47 Cards in this Set

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  • Back
hallucinegens/psychotomimetics- produce what effects (4)
produce delirium, true hallucinations (neurons being excited)), loss of contact with reality, death
psychotomimetics/hallucinegens- hollister's definition (4)
upon a single effective dose:

cause changes in thought, mood and perception with little memory impairment

produce little stupor/narcosis or excessive stimulation (amphetamines)

produce minimal autonomic side fx

are non addicting
why study these agents? (4)
hallucinegens as as tools for studying psych diseases (LSD for schizo)

basic neurochemical mechanisms in the brain

NT functoin
GPCR research
classes of psychotomimetic agents (6)
LSD
phenylethylamine
indole alkylamines (serotonergic)
phenylcyclohexyl (PCP)
N-methyl 3 piperidyl benzilate (Anticholinergic)
canniboids
LSD
name the type of activity it has as well
indole alkylamine (serotonergic)
PCP (phenylcyclohexyl)
mimics what structure
phenylethylamine
(mimics DA/NE structure)
classical hallucinogen properties (3)
meet hollister definition
bind to 5HT2 receptor
recognized by DOM trained animals (behavioral)
dissociative agent properties (3)
blocks or reduces signals to cortico/conscious mind

detachment from environment

inhibits sensations from physical senses
animal vs human studies for psycho agents (4)
human subjects should be best suited to provide most reliable assessment of actoins/potency of psychotomimetic agents- but...

case studies not that well controlled (limited pops, few drug doses, anecdotal)

very few approved clinical studies in humans for psycho agents

therefore we rely heavily on animal studies
drug discrimination paradigm (testing method?) properties (3)
1) used for a variety of psychoactive agents
2) does not represent a model of psychomimetic activity
3) general applicability and is used to study stimulants, barbs, CNS agents, etc.
describe drug discrimination paradigm general concept (2)
animals trained to discriminate the stimulus of a training drug (known MoA agent) vs vehicle (saline, DMSO, water)

then animals are taught to associate the effect of training drug with one specific lever, and one lever for vehicle
DDP - describe how animals are trained (4)
2 levers in training boxes

lever A if saline will give animal food

lever B will give food if animal is injected with LSD

now you can test an unknown substance to see if it produces pharmacologically similar effects to training drug
DDP- accuracy rate
dose dependency?
trained animals respond 80% of the time or better to the appropriate drug

dose dependent- lower drugs = more mistakes, so can correlate # of mistakes to potency of drug via dose response curve
DDP challenge drug
drug with unknown MoA- want to see if it gives similar stimulus effect
what is stimulus generalization?
important note: if similar stimulus effect to training drug is instigated we call it stimulus generalization. this does NOT mean they have the same MoA.
non-classical hallucinogens
canniboids

PCP
3 common species of marijuana
cannabis sativa
cannabis indica
cannabis ruderalis
3 major presentations of pot- order in level of potency from highest to low
hashish- pure resin- most potent
ganja- flowering tops of plants- second most potent
bhang- leaves and stems- least potent
major active constituent of canniboid/pot
delta 9 THC
delta 8 THC
less potent version of delta 9 THC
major metabolite of THC
activity
11 hydroxy delta 9 THC

retains some activity
THC absorption (3)
most rapid through inhalation
absorbed through gut

absorbed by body tissue then released slowly back into recirculation (hence why it lasts so long in your body)
how long dose THC stay in body
D2O (deterium) labeled delta 9 THC has been detected even after 2 weeks in body after a single dose
THC tolerance and addiction
delta 9 THC dose develop but does not lead to physical dependence (addiction- as in you get withdrawals)
negative effects of MJ (4)
marijuana can impair memory, performance and learning- produces an amotivational sequence
CP55940
cannabinoid mimic made by pfizer- induces appetite but never marketed
win 55,212-2 - category of compound
activity
not really cannabinoid. it is an aminoalkylindole that produces similar fx to THC
SR14617A - what's it do? (3)
inverse agonist at cannbinoid receptor (produces opposite effect)

attenuates TCH effect

used for weight loss (appetite suppressed)- but if you stop taking it you gain all the weight back
indole structure
know
AE of SR14617A (3)
depression
suicide
if used in clinically silent MS pt resulted in sx manifestation that resulted from disruption of normal neuroprotective mechanisms
MoA of cannibinoids (receptors affected) (2)
affects CB1 and 2 receptors
CB1 vs CB2
CB1 is found in brain
CB2 is found in periphery and believed to have immunomodulation effects
endogenous cannibinoid (CB1) ligands (3) and potency relative to THC
anandamide- less potent
docosatetraenoylethanolamide- more potent
homo-gamma-linolenylethanolamide (least potent)
stability of endogenous CB1 ligands vs THC
not as stable? listen again
how is delta 9 THC metabolized?
potency
OH on C11- more potent
most potent THC derivatives (SAR)
delta 8 THC with 2 methyl groups on alklyl chain
delta 8 THC DMH (dimethyl) metabolism
hydroxyl group on C11 to 11 hydroxy delta 8 DMH
adding hydroxy group to THC- effect on potency
makes it more potent
what compound is this
potency?
delta 8 thc metabolite

more potent (due to OH)
compound? potency?
hydroxy dimethyl version of delta 8 THC
MOST potent
compound?
potency?
more potent
metabolite of delta 9 THC
compound/potency
delta 9 THC
least potent
potency
compound
2nd most potent
delta 8 THC DMH
non cns related disorders treated with weed (5)
alleviate IOP in glaucoma
spasticity in MS
tourette's

immune disorders (CB2 related)

weight loss...maybe
CNS related disorders that can be treated with weed (5)
neuropathic pain
parkinson's disease
epilepsy
drug abuse
psych disorders