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47 Cards in this Set
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hallucinegens/psychotomimetics- produce what effects (4)
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produce delirium, true hallucinations (neurons being excited)), loss of contact with reality, death
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psychotomimetics/hallucinegens- hollister's definition (4)
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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 |
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why study these agents? (4)
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hallucinegens as as tools for studying psych diseases (LSD for schizo)
basic neurochemical mechanisms in the brain NT functoin GPCR research |
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classes of psychotomimetic agents (6)
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LSD
phenylethylamine indole alkylamines (serotonergic) phenylcyclohexyl (PCP) N-methyl 3 piperidyl benzilate (Anticholinergic) canniboids |
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LSD
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name the type of activity it has as well
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indole alkylamine (serotonergic)
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PCP (phenylcyclohexyl)
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mimics what structure
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phenylethylamine
(mimics DA/NE structure) |
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classical hallucinogen properties (3)
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meet hollister definition
bind to 5HT2 receptor recognized by DOM trained animals (behavioral) |
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dissociative agent properties (3)
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blocks or reduces signals to cortico/conscious mind
detachment from environment inhibits sensations from physical senses |
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animal vs human studies for psycho agents (4)
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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 |
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drug discrimination paradigm (testing method?) properties (3)
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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. |
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describe drug discrimination paradigm general concept (2)
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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 |
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DDP - describe how animals are trained (4)
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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 |
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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 |
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DDP challenge drug
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drug with unknown MoA- want to see if it gives similar stimulus effect
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what is stimulus generalization?
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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.
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non-classical hallucinogens
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canniboids
PCP |
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3 common species of marijuana
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cannabis sativa
cannabis indica cannabis ruderalis |
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3 major presentations of pot- order in level of potency from highest to low
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hashish- pure resin- most potent
ganja- flowering tops of plants- second most potent bhang- leaves and stems- least potent |
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major active constituent of canniboid/pot
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delta 9 THC
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delta 8 THC
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less potent version of delta 9 THC
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major metabolite of THC
activity |
11 hydroxy delta 9 THC
retains some activity |
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THC absorption (3)
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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) |
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how long dose THC stay in body
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D2O (deterium) labeled delta 9 THC has been detected even after 2 weeks in body after a single dose
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THC tolerance and addiction
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delta 9 THC dose develop but does not lead to physical dependence (addiction- as in you get withdrawals)
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negative effects of MJ (4)
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marijuana can impair memory, performance and learning- produces an amotivational sequence
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CP55940
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cannabinoid mimic made by pfizer- induces appetite but never marketed
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win 55,212-2 - category of compound
activity |
not really cannabinoid. it is an aminoalkylindole that produces similar fx to THC
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SR14617A - what's it do? (3)
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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 |
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indole structure
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know
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AE of SR14617A (3)
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depression
suicide if used in clinically silent MS pt resulted in sx manifestation that resulted from disruption of normal neuroprotective mechanisms |
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MoA of cannibinoids (receptors affected) (2)
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affects CB1 and 2 receptors
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CB1 vs CB2
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CB1 is found in brain
CB2 is found in periphery and believed to have immunomodulation effects |
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endogenous cannibinoid (CB1) ligands (3) and potency relative to THC
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anandamide- less potent
docosatetraenoylethanolamide- more potent homo-gamma-linolenylethanolamide (least potent) |
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stability of endogenous CB1 ligands vs THC
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not as stable? listen again
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how is delta 9 THC metabolized?
potency |
OH on C11- more potent
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most potent THC derivatives (SAR)
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delta 8 THC with 2 methyl groups on alklyl chain
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delta 8 THC DMH (dimethyl) metabolism
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hydroxyl group on C11 to 11 hydroxy delta 8 DMH
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adding hydroxy group to THC- effect on potency
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makes it more potent
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what compound is this
potency? |
delta 8 thc metabolite
more potent (due to OH) |
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compound? potency?
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hydroxy dimethyl version of delta 8 THC
MOST potent |
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compound?
potency? |
more potent
metabolite of delta 9 THC |
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compound/potency
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delta 9 THC
least potent |
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potency
compound |
2nd most potent
delta 8 THC DMH |
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non cns related disorders treated with weed (5)
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alleviate IOP in glaucoma
spasticity in MS tourette's immune disorders (CB2 related) weight loss...maybe |
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CNS related disorders that can be treated with weed (5)
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neuropathic pain
parkinson's disease epilepsy drug abuse psych disorders |