L20 Flashcards
a hallucinogen is a psychoactive agent that causes causes changes in perception (hallucinations)
Also associated with __,__,__
a hallucinogen is a psychoactive agent that causes causes changes in perception (hallucinations)
Thoughts, emotions, consciousness
most hallucinogen drugs alter function of the __ (predominantly ___) or ____ systems
most hallucinogen drugs alter function of the monoaminergic or glutmatergic systems
Hallcuinogen criteria
1. changes in thought, perception, and mood should
____
2. intellectual or memory _____ should be ____
3. stupor, narcosis, or excessive stimulation should/should not be an integral effect
4. autonomic nervous system side effects should be _____
5. addictive craving should be _____
Hallcuinogen criteria
1. changes in thought, perception, and mood should
predominate
2. intellectual or memory impairment should be minimal
3. stupor, narcosis, or excessive stimulation should not be an integral effect
4. autonomic nervous system side effects should be minimal
5. addictive craving should be absent
classic psychedelics eg
LSD, psilocybiin, mescaline
common mechanism of action for classic psychedelics
5HT2a r
Lysergamides •Discovered accidentally by the pharmacologist
Dr. Albert Hofmann
•ergot alkaloids are compounds that are
produced by a__ that grows on __
fungus
rye
ergot alkaloids good –
potential treatment for –
vasoconstrictors,
migraine
t/f: •pure ergot derivative not very stable in solution,
t
•The lower the dissociation
constant (Ki), the more__ LSD binds to that
receptors
strongly
Hallucinogenic effects
mediated by __
5HT-2a
LSD is a high affinity
__ __ at 5-
HT2a receptors
partial agonist
t/f: all 5HT-2a agonist are
hallucinogenic
why
f
Biased agonism.
LSD activates __ __
instead of phospholipase C, like__ does
phospholipase A2
serotonin
pretreatment with a 5HT2a
antagonist (__)
blocked__ effects
of LSD
Ketanserin
hallucinogenic
Hallucinogen persisting perception disorder (HPPD):
distressing visual hallucinations that appear following drug use
•__dose of LSD can lead to profound tolerance that
lasts for several__
Single
days
•Tolerance is accompanied by__ of 5-__but not other 5-HT receptors.
downregulation
HT2
\_\_ of LSD with other hallucinogens acting at serotonin receptors (psilocybin, DMT)
•Cross-tolerance
Psilocybin structure
structural homology with
an indole molecule (6 membered benzene ring
fused to a five membered pyrrole ring) with an amine
group
5ht
naturally occurring hallucinogen
compound produced by psilocybin
mushrooms
Psilocybin
• used by humans in religious ceremonies
for thousands of years
Psilocybin
Psilocybin effects when iingested
euphoria, visual and mental hallucinations, changes in perception and distorted sense fo time, spiritual experiences • adverse reactions of nausea and panic attacks
Psilocybin prodrug metabolization
dephosphorylated to psilocin in the body