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NUTR 512 > Lec 3 & 4 - Hallucinogens, stimulants and sedatives > Flashcards

Lec 3 & 4 - Hallucinogens, stimulants and sedatives Flashcards

1
Q

5 classes of Neurotransmitters

A
  • acetylcholine
  • amino acid (glutamate, GABA, glycine)
  • monoamines (indolamines, catecholamines)
  • purines (adenosines)
  • peptides (opiod)
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2
Q

acetylcholine

  • found in (3)
  • used for
  • receptors
A

Found in:

  • brain, motor neuron,
  • Autonomic NS
    - parasympathetic: ganglion
    - sympathetic: both ganglionic and termina

Used for: Alzheimer and dementia
Receptors:
- ionotropic: nicotinic R
- metabotropic: muscarinic R

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3
Q

Fly agaric: uses
compound? what does it do? Which receptor? Risk?

What’s main compound?

A

uses: entheogenic, expectorant, hallucinogen

muscarine found in traces

  • mimics ACh action, non-selective agonist of muscarinic ACh R
  • profound activation of parasympathetic NS
  • NOT DEGRADED by acetylcholinesterase

Main compound: muscimol

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4
Q

ionotropic receptor

A

ion-gated channel, simple (ex: nicotinic)

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5
Q

metabotropic receptor

A

more complex, with G-protein (ex: muscarinic)

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6
Q

muscimol
recepto?
symptoms?

A

muscimol + predrug IBOTENIC ACID (not metabolized version)

  • selective GABA receptor agonist
  • responsable for drunkenness, sedative, hallucinogen activity
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7
Q

ibotenic acid
Receptor?
Symptoms?

A
  • muscimol pre-drug, agonist of NMDA metabotropic glutamate receptors
  • nausea, cramps, vomiting when eat AManita
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8
Q

glutamate

  • found in
  • used for
  • receptors
A
  • found in CNS everywhere
  • used to treat sclerosis (ALS): excites motor, sensory and cognitive neurons
  • receptors: (excitory)
    • ionotropic: NMDA receptor (ibotenic acid)
    • metabotropic: group I, II, III
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9
Q

role of NMDA receptors?

extrasynaptic, synaptic?

A

–> excitotoxicity
NMDA receptors play crucial role in health and function of neurons
- extrasynaptic NMDA receptos responsible for excitotoxicity and cell death
- synaptic NMDA R contribute to health and logevity of cells

risks links with excitotoxicity: stroke, traumatic brain injury, alzheimer…

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10
Q

Gamma- -aminobutyric Acid (GABA)
found in
- used for
- receptors

(subunits? two types? React to what?)
PAM

A 
- everywhere in CNS
used for: 
- anxiety, rehab
- inhibit sensory and cognitive neurons
- sedation, muscular/CV relaxation, inhibits pain, reflexes 
Receptors: (inhibitory)
5 subunits
many binding sites for drugs
  • ionotropic: GABAa receptor
    Chlorine, responsible for sedative effects of GABAa agonists
    • Metabotropic: GABAb receptors
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11
Q

PAM

A

PAM: increase proba that agonist will bind (Gaba to GABAa)

GABAa:
Barbituates and benzodiazepines (PAM)

sedative, hypnotic, antxiolytic, muscle relaxant

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12
Q

Glycine
found in
- used for
- receptors

A
  • found in spinal cord: inhibit spinal cord interneurons
  • used to treat plasticity
  • receptors: ionotropic: Cl- channels
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13
Q

Monoamines (2 types)

enzyme degrading?

A
  • indolamine: serotonin (from tryptophan)
  • catecholamines: dopamine, norepinephrine, epinephrine (from tyr)

both degraded by same enzyme: monoamine oxidase

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14
Q

Ayahuasca (2 main components

1st one does 2 things
2nd one: properties, how to take it, receptors?

A

Harmine:

  • MAOI inhibits breakdown of monoamine transmitters (5Ht, DO) + hormones (melatonin, EP, NOR)
  • -> more 5HT and DO: anti-depressant
  • diabetes: induces proliferation of a-b cells in pancreas (glucagon et insulin)

DMT (dimethyltryptamine)

  • hallucinogenic properties
  • cannot be eaten bc monoamine oxidase in stomach –> sniffing it
  • agonist of 5HT receptors
  • DMT can accumulate in crebreal cortex, amygdala,
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15
Q

serotonin

type of monoamine?
found where? (2)

produced by what?

used for

receptors

A

indolamine

found in

  • brain: limbic fct (emotions, mood)
  • guts to help with bowel mvts (produced by enterochromaffin cells lining digestive tract) –> brain gut axis! link between depression and gut health (more nerves in gut than spinal cords)

used for depression and sleep (converted to melatonin)

Receptors:

  • ionotropic: 5HT 3: excitatory
  • matebotropic: 5HT 1-7 excitatory, inhibitory
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16
Q

serotonin receptors

A

–> neurotransmitters that can influence:

  • GABA: leads to inhibition
  • Glutamine: excitatory
17
Q

serotonin levels
low (5)
high (3)
normal (2)

A

low:
- depression,
- anxiety,
- increased pain sensitivity
- bad sleep
- fatigue

high

  • medical emergency
  • possibl edeath
  • caused by SRIs, OTC supplements (Sero reuptake inhib)

normal:

  • happiness
  • relaxation
18
Q

serotonin agonists

A

DMT, LSD, ergotamine

19
Q

dopamine

type of monoamine?
where?
used for?
receptors?

A

catecholamine

found in brain and brainstem

  • substantia nigra: reward, addiction
  • hypothalamus: inhibits prolactin release

used for: schizophrenia, psychosis, parkinson’s disease

receptors:
- ionotropic: none
- metabotropic: D1 and D2

20
Q

dopaminic pathways

A 
dopamine = nT used by 
- reward pathways (mesolimbic and mesocortical one)
  o memory
  o motivation and emotions
  o reward and desire
  o addiction
  • tuberoinfundibular
    o hormonal regulation
    o maternal behaviour
    o pregnancy
  • nigrostriatial pathways
    o motor control
    o death of neurons in here: Parkinson
21
Q

dopamine levels:

low, high for each pathway?

A

nigrostriatal (mvt)

  • low: parkinson, EPS
  • high: chorea, TICS, athetosis

mesocorticolimbic (mood, reward)

  • anhedonia
  • high: psychosis, euphoria, hallucination

tuberoinfundubular

  • low: hyperlactinemia
  • high: inhibit prolactin
22
Q

coca and cocaine

what does it do?

how?

A
  • stimulant
  • cocaine: mix leaves with solvent, mash it
    o loss of contact with reality
    o euphoria
    o increase dopamine: risk of addiction
  • blocks reuptake of monoamine nT so DO concentration increases
  • leads to increased available synaptic transmitters
  • chronic use leads to decreased availability of D2 receptors
23
Q

norepinephrine

type of monoamine?
where?
used for?
receptors?

A

catecholamine

found in brain

  • locus ceruleus: cortex, arousal, attention
  • ANS: sympathetic neurons (effector organs, postganglions neurons)

used for: ADHD, anxiety, cardiac failure

receptors:
- ionotropic: none
- metabotropic: alpha 1 et beta 1 (excitatory), A2 et B2 (inhbitory)

24
Q

ephedra

effects?

mechanism?

A

Stimulant:

ephedrine alkaloids cause:
- CNS stimulation
- cardiac stimulation
- tachycardia
- elevated blood pressure 
can also have sleep problems, anxiety, headaches.. banned in US

mechanism: like amphets

  • enters presynaptic neuron through NET (norepinephrine transporter)
  • enters vesicule through vesicular monoamine transporter (VMAT)
  • released into cytoplasm and synaptic cleft with NET
25
Q

purine (adenosine)

where?
used for?
receptors? (special about them? )

role in sleep

A

found in (everywhere)

  • brain, heart, kidneys, adipose tissue (metabotropic R)
  • neurons and glial cells in CNS? PNS (ionotropic receptors)

used for tachycardia

receptors:

  • iono: P2X (binds to ATP)
  • metabo: P1, P2Y
  • -> oldest and most abundant in all living organisms
26
Q

circadian rythm
sleep pressure

adenosine

A

cortisol keeps us awake (stress hormone), melatonin is sleep hormone

sleep pressure: chemical build up in brain (adenosine)
–> adenosine is sleep regulator substance

mediated by A1 and A2 receptors

27
Q

caffeine

antagonist, agonist?
mechanism?

where can you find caffeine?

overdose?

A

stimulant

  • antagonist for all adenosine receptors
  • A2 receptor: alertness, so antagonist effect and stay alert

blocks binding of adenosine, not feeling tired.
Norepinephrine supposed to bind to receptors and act as stimulant, but if too much coffee, less NO –> addictive

coffee, tea, cocoa, yerba maté, guarana

overdose: >400 mg.
symptoms: restless, fidgeting, anxiety, insomnia, increase pee, rapid heart beat, irritability

28
Q

herbal sedatives

mechanisms? (3)

A

either
- facilitate neuron inhibition
o GABA receptor agonist (benzos, barbs)
o either block reuptake of GABA or increase release

  • inhibit neuronal excitation
    o glutamate receptor antagonists
    o NMDA receptor involved in memory
  • block voltage-gating ion channels
29
Q

herbal sedative: valerian

mechanisms

A

valerian:
- additive effects of several compounds.
- monoterpenes, sesquiterpenes, alkaloids
- mechanisms:
o facilitate GABA release
o inhib GABA breakdown
–> AGONIST
- used for mild stress, sleepin gaid, anxiety, mood disorders

30
Q

herbal sedative: chamomille

mechanisms

A

apigenin mechanisms:

  • monoamine transport activator
  • ligand for benzodiazepine receptors (GABAa)
  • antagonist of NMDA receptor
31
Q

herbal sedative: kava

mechanisms (4)

A

kavain mechanisms

  • facilitate GABA transmission
  • inhibits Na+ channels (voltage gated ion channel) and release of glutamate
  • inhibit monoamine oxidase B: reduce inflammation
  • eicosanoids: inhibit cyclooxygenase (COX), suppress thromboxane A synthesis –> increase GABA function

NUTR 512 (5 decks)

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