Medchem Lecture 15

Front 1

Psychotomimetic/hallucinogenic agents are those that on administration of a single effective dose consistently produce changes in thought, mood, and perception with little memory impairment

Back 1

definition of hallucinogens

Front 2

These are LSD-like agents that share common stimulus properties and may act via a common mechanism of action

Back 2

classical hallucinogens

Front 3

These act by different mechanisms and produce distinct effects common to members within each group

Back 3

non-classical hallucinogens

Front 4

Two major non-classical hallucinogens (psychoactive drugs of abuse)

Back 4

cannabinoids (marijuana) and PCP

Front 5

The three major species of the cannabis plant

Back 5

Cannabis
1. sativa
2. indica
3. ruderalis

Front 6

Principle active ingredient in (cannabinoid) plants is

Back 6

THC

Front 7

THC is rapidly and efficiently absorbed by what route of administration?
*found in marijuana

Back 7

inhalation

Front 8

Does THC lead to physical dependence?

Back 8

NO

Front 9

What are the two population of cannabinoid receptors?

Back 9

CB-1 and CB-2

Front 10

These receptors are G protein–coupled, seven-helix transmembrane-spanning and are cloned.

Back 10

CB-1 and CB-2 cannabinoid receptors

Front 11

This cannabinoid receptor may mediate the psychoactive effects of THC-related agents and are found primarily in the brain

Back 11

CB-1

Front 12

This cannabinoid receptor may be involved in immunomodulatory actions and are found exclusively in the periphery

Back 12

CB-2

Front 13

Does cannabidiol produce THC-like stimulus effects?

Back 13

NO

Front 14

What drug was introduced as a dissociative anesthetic during the late 1950's?
*now a nonclassical hallucinogen

Back 14

Phencyclidine (PCP, "angel dust")

Front 15

PCP-like states were theorized to provide a good model for investigating what mental disorder?

Back 15

schizophrenia

Front 16

What routes of administration is PCP usually taken in?

Back 16

inhalation, injection, or smoking

Front 17

PCP behaves as this type of antagonist

Back 17

NMDA

Front 18

NMDA receptors have been implicated in seizures so PCP and related arylcycloalkylamines have been explored as these potential drugs

Back 18

antiepileptics

Front 19

PCP appears to produce effects similar to those of

Back 19

amphetamine-like stimulants and central depressants

Front 20

PCP has both direct and indirect effects on these systems

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dopaminergic

Front 21

This produces some effects reminiscent of those produced by PCP

Back 21

NANM (N-Allylnormetazocine)

Front 22

What receptors does PCP bind to

Back 22

σ receptors

Front 23

σ receptors were renamed

Back 23

NANM-PCP receptors, or σ/PCP receptors

Front 24

This nonclassical hallucinogen antagonizes the effects of the excitatory amino acid NMDA and is a noncompetitive NMDA receptor antagonist

Back 24

PCP

Front 25

What type of receptor is the NMDA receptor

Back 25

ligand gated ion channel receptor that regulates the flow of cations Na and Ca

Front 26

What mental disease is PCP closely related to

Back 26

schizophrenia

Front 27

This type of hallucinogen bind at the 5-HT2 serotonin receptors and are recognized by DOM-trained animals in tests of stimulus
generalization

Back 27

classical hallucinogens

Front 28

What is the general structure for classical halluciogens

Back 28

Ar-C-C-N
*Ar=substituted phenyl 3-indooyl, C-C=ethyl/branched chain, N=primary/secondary/tertiary amine

Front 29

What are the two main structural classes of classical hallucinogens

Back 29

1. indole-alkylamines
2. phenyl-alkylamines

Front 30

What are the four subclasses of indole-alkylamines

Back 30

a. N-substituted tryptamines
b. α-alkyl-tryptamines
c. ergolines (lysergamides)
d. β carbolines (potentially)

Front 31

What are the two subclasses of phenyl-alkylamines

Back 31

a. phentlethylamines
b. phenylisopropylamines

Front 32

What is one of the best-investigated hallucinogens in the indole-alkylamine class and N-alkyltryptamine subclass?

Back 32

N,N-dimethyltryptamine (DMT)

Front 33

What is the onset and duration of action of DMT

Back 33

onset=5 minutes
duration of action=30 minutes

Front 34

These two N-alkyltryptamines are inactive as psychoactive substances because they are not very lipophilic to penetrate the BBB

Back 34

N-monomethyltryptamine and tryptamine

Front 35

________ and _________ are found in the skin of certain frogs and may have given rise to the phenomenon of "toad licking"

Back 35

Bufotenine and 5-OMe DMT

Front 36

________ is widely found in certain species of mushrooms and has given rise to the term "shrooms"

Back 36

Psilocin

Front 37

Is tryptamine psychoactive

Back 37

NO

Front 38

Because of the introduction of an α-methyl group to α-methyltryptamine (α-MeT), which enhances lipophilicity and protects against metabolism, the drug becomes twice as potent as this

Back 38

DMT

Front 39

LSD is considered what type of hallucinogen

Back 39

classical

Front 40

This indole-alkylamine, ergoline is perhaps the best known and one of the most potent classical hallucinogens

Back 40

LSD (lysergamides)

Front 41

LSD actions in humans can be divided into three major categories:

Back 41

1. perceptual (altered shapes and colors, heightened sense of hearing)
2. psychic (alterations in mood, visual hallucinations, altered sense of time)
3. somatic (nausea, blurred vision, dizziness)

Front 42

Of the two phenylalkylamines, which is more potent?

Back 42

phenylisopropylamines

Front 43

These represent the largest group of classical hallucinogens

Back 43

phenylethylamines and phenylisopropylamines

Front 44

The phenylethylamines are the _________ counterparts of the phenylisopropylamines

Back 44

α-desmethyl

Front 45

In classical hallucinogens It is believed that this subtype plays a predominant role in the behavioral actions of these agents

Back 45

5-HT2A

Front 46

Stimulants can be divided into to general categories:

Back 46

1. stimulant or behavioral stimulant
2. analeptics

Front 47

This type of stimulant typically refers to agents with a central stimulatory effect for which the actions are manifested mostly in motor activity

Back 47

behavioral stimulants

Front 48

This type of stimulant refers to agents that have a stimulant effect primarily on autonomic centers, such as those involved in the regulation of respiration and circulation

Back 48

analeptics

Front 49

Amphetamine and cocaine are examples of this type of stimulant

Back 49

behavioral stimulants

Front 50

Styrchnine and caffeine are examples of this type of stimulant

Back 50

analeptics

Front 51

The simplest unsubstituted phenylisoprprylamine is

Back 51

1-phenyl-2-aminopropane, or
amphetamine

Front 52

What is the half life of amphetamine

Back 52

7 hours

Front 53

What phases of metabolism does amphetamine undergo?

Back 53

phase I and II

Front 54

The phase I metabolism of amphetamine analogues is catalyzed by what two enzyme systems

Back 54

cytochrome P450 and flavin monooxygenase

Front 55

This is an indirect-acting dopaminergic and noradrenergic agonist, meaning it causes an increase in synaptic concentrations of the neurotransmitters

Back 55

amphetamine

Front 56

The central stimulant actions of amphetamine primarily involve this system
*enhances the release of this and prevents the reuptake into terminals

Back 56

dopamine system

Front 57

Chronic administration of high doses of amphetamine may result in this

Back 57

amphetamine psychosis

Front 58

2R-carbomethoxy-3S-benzyloxy-1R-tropane is also commonly known as

Back 58

cocaine

Front 59

Cocaine possesses _______actions and is a local anesthetic

Back 59

vasoconstrictor

Front 60

Cocaine has been shown to block the reuptake of _______, ________ and __________

Back 60

norepinephrine, serotonin, and dopamine

Front 61

Designer drugs are also called

Back 61

controlled substance analogues

Front 62

This is the end result of the application of structure-activity-relationships at the clandestine level

Back 62

designer drugs

Front 63

blue mystic, ecstacy and love drug are all examples of

Back 63

designer drugs

Front 64

Release of neurotransmitter from presynaptic terminals results in the activation of
postsynaptic neurotransmitter receptors that can be coupled to complex effector mechanisms.
Through modulation of postsynaptic pathways, the state of the neuron can be altered such
that neurons become more or less responsive to the neurotransmitter. This process can be referred to as

Back 64

functional plasticity

Front 65

One recent finding in the treatment of drug abuse involves the regulation of _______, an integrator of intracellular signaling

Back 65

DARPP-32

Front 66

Agents that decrease pain are referred to as

Back 66

analgesics or antinociceptives

Front 67

This class of drugs to relieve pain has primarily a peripheral site of action and are useful for mild to moderate pain, often having an anti-inflammatory effect

Back 67

NSAIDs

Front 68

This class of drugs to relieve pain inhibits pain transmission by inhibition of voltage-regulated sodium channels and are highly toxic when used in concentrations sufficient to relieve chronic or acute pain in ambulatory patients

Back 68

local anesthetics

Front 69

This class of drugs to relieve pain act as inhibitors of NMDA activated glutamate receptors in the brain and are effective analgesic agents when used alone or in combo with opioids

Back 69

dissociative anesthetics (ketamine)

Front 70

This antiseizure drug drug inhibits voltage regulated Ca ion channels and is useful in treating neuropathic pain

Back 70

pregabulin

Front 71

These will cause a decrease in pain perception

Back 71

CNS depressants

Front 72

These antidepressant drugs are useful either alone or in combo with opioids in treating certain cases of chronic pain

Back 72

inhibitors of serotonin and NE reuptake
SSRIs and SNRIs

Front 73

Severe acute or chronic pain generally is treated most effectively with these

Back 73

opioid agents

Front 74

Opioid analgesics use the juice (opium) from unripe seed pods of this plant

Back 74

poppy plant

Front 75

The opioids peptides isolated from mammalian tissue are known collectively as this word which is derived from a combo of endogenous and morphine

Back 75

endorphins

Front 76

The endogenous opioids exert their analgesic action at these two sites

Back 76

spinal and supraspinal

Front 77

What are the three major types of opioid receptors

Back 77

µ, κ, and δ

Front 78

Edomorphin-1 and endomorphin-2 are endogenous opioid peptides with a high degree of selectivity for which opioid receptor

Back 78

µ

Front 79

All of the opioid alkaloids and most of their synthetic
derivatives are this type of agonists

Back 79

µ-selective agonists

Front 80

Ethylketazocine and bremazocine are 6,7-benzomorphan
derivatives with which opioid receptor selectivity

Back 80

κ opioid receptor selectivity

Front 81

Enkephalins, the natural ligands at δ (DOP) receptors, are only slightly selective for this receptor over µ
receptors.

Back 81

δ receptor

Front 82

It has been proposed that a deficiency exists in this self reward system of individuals who have a predisposition to abuse addictive drugs

Back 82

opioid mediated self reward system

Front 83

In the self-reward system, any agent that promotes stimulation of this type of receptor in the nucleus accumbens potentiates self reward and has the potential to be abused

Back 83

type-1 dopamine (D1) receptors