Lecture 3: Plants that affect acetylcholine receptors Flashcards

1
Q

Organs and glands activated by the sympathetic nervous system

A

brain, muscles, the pancreas, thyroid gland and adrenal glands

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2
Q

Organs and glands affected by the parasympathetic gland

A

the liver, kidneys, pancreas, spleen, stomach, small intestines and colon

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3
Q

Hormones and substances elevated by the sympathetic nervous system

A

insulin, cortisol, and the thyroid hormones

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4
Q

hormones and substances elevated by the parasympathetic nervous system

A

pancreatic enzymes, bile and other digestive enzymes

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5
Q

types of amino acid neurotransmitters

A

Glutamate, GABA, Glycine

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6
Q

types of monoamine neurotransmitters

A
  1. Indolamines: Serotonin (a hormone, NOT a NT)

2. Catecholamines: Dopamine, Norepinephrine, Epinephrine

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7
Q

type of purine neurotransmitter

A

Adenosine

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8
Q

type of peptide neurotransmitter

A

Opioid

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9
Q

Where is acetylcholine found

A

1) motor neuron
2) brain
3) autonomic nervous system
- sympathetic: Ganglion NT
- parasympathetic: Both ganglion and terminal

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10
Q

Function of acetylcholine

A

a neurotransmitter in the autonomic nervous system, both as an internal transmitter for the sympathetic nervous system and as the final product released by the parasympathetic nervous system.

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11
Q

Acetylcholine receptors

A

1) ionotropic: nicotinic receptors

2) metabotropic: muscarinic receptors

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12
Q

nicotinic receptors vs. muscarinic receptors

A

nicotinic: opens very simple and fast. Ligand binds - open - response
muscarinic: ligand - conformational change - activation of G protein subunits - release of secondary messengers - response

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13
Q

Tobacco scientific name(s)

A

1) Nicotiana rustica (Aztec tobacco)

2) Nicotiana tabacum

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14
Q

Tobacco - parts used

A

Leaves

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15
Q

Tobacco - Bioactive compound

A

Nicotine

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16
Q

Nicotine mechanism

A
  • acts as a receptor agonist at a a7 nicotinic acetylcholine receptor
  • it may also function by inhibiting acetylcholinesterase
  • a7 directly stimulates the acetylcholine recptors on dopamine - containing neurons and cause an overflow of dopamine
  • it also activates the sympathetic nervous system, stimulating the release of epinephrine
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17
Q

what are PAM(s)

A

they are called positive allosteric modulators - other things required for the agonistic binding of nicotine and nicotinic acetylcholine receptors

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18
Q

development of nicotine addiction

A

1) Craving - no nicotine in the bloodstream
2) Cigarette - in the presence of nicotine, the receptor opens and lets the signal through
3) cigarette just finished - the receptor is desensitized and does not respond to more nicotine
4) long term smoking increases craving - more receptors are formed with long term exposure to nicotine, to increase sensitivity.

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19
Q

tobacco and cancer/atheroscelrosis

A
  • curing and aging tobacco leaves generates carcinogenic tobacco-specific nitrosamines (TSNAs)
  • starch is then converted to sugar, which glycates proteins; this oxidizes into advanced glycation end-products (AGEs)
  • Inhalation of AGEs is a major contributor to atherosclerosis and cancer
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20
Q

Insufflation

A

the act of blowing something onto a body cavity

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21
Q

expectorant

A

promotes the secretion of sputum (a mixture of saliva and mucus coughed up from the respiratory tract)

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22
Q

Ethneogenic

A

a drug that causes one to become inspired or to experience feelings of inspiration, often in a religious or spiritual manner

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23
Q

Fly Agaric - scientific name

A

Amanita muscaria

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24
Q

Fly Agaric - part used

A

Entire mushroom

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25
Q

Fly Agaric - bioactive compound

A

Muscarine

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26
Q

Function of muscarine

A
  • mimics the action of Ach on muscarinic acetylcholine receptors
  • Causes profound activation of the parasympathetic nervous system
  • not degraded by acetylcholinesterase
  • can cause circulatory collapse and death
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27
Q

Treatment of muscarine toxicity

A

Atropine - a competitive reversible antagonist of muscarinic receptors

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28
Q

Muscimol

A

Cause of hallucinations and toxicity - it is a potent selective GABA a receptor agonist
- responsible for the drunkenness, sedative, depressant, euphoric and dissociative effect

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29
Q

Ibotenic acid

A

cause of hallucinations and toxicity

  • potent agonist of the NMDA (N-methyl-D-aspartate) metabotropic glutamate receptors.
  • responsible for nausea, stomach cramps ad vomiting associated with Amanita ingestion
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30
Q

main psychoactive compounds of Amanita muscaria

A

muscimol and isotonic acid

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31
Q

Divination

A

represents a way to induce deep concentration and introspective thought

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32
Q

name the plants used for divination with their scientific name and main compounds

A

1) Angel’s trumpets: Brugmansia spp. ; tropane alkaloids: scopolamine, hyoscyamine, atropine
2) Jimoson weed: Daturam stramonium; tropane alkaloids: scopolamine, hyoscyamine, atropine
3) morning glory: Ipomoea tricolor; ergo line alkaloids: ergonovine, ergine

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33
Q

Jimson weed - scientific name

A

Datura stramonium

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34
Q

Jimson weed - parts used

A

Seeds/leaves

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35
Q

Jimson weed - bioactive compounds

A

Atropine, hyocamine, scopolamine

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36
Q

Fate of acetylcholine after being broken down by acetylcholinesterase

A

Choline is transported back into the axis terminal and is used to make more Ach

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37
Q

Anticholinergic Toxidrome

A

results from competitive antagonism of acetylcholine at central and peripheral muscarinic receptors

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38
Q

Anticholinergic Toxidrome symptoms

A
confusion
dry mouth
urinary retention
shaking
dilated pupils (mydriasis)
flushed skin
absent bowel sounds
tachycardia 
hyperthermia
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39
Q

Anti-cholinergic

A

inhibits the transmission of the NT acetylcholine and suppress the parasympathetic nervous system

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40
Q

anti-cholinergic substances can cause:

A

amnesia, bizarre behaviour, and the inability to distinguish reality from fantasy (hallucination)

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41
Q

tropane alkaloids are ——-

A

anti-cholinergenic

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42
Q

examples of anti-cholinegernic substances

A

1) atropine
2) scopolamine - used to treat motion sickness and post-operative nausea
3) hyoscyamine - provides symptomatic relief of spams caused by peptic ulcers, IBS, pancreatitis, and colic

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43
Q

Glycoalkaloids

  • what are they
  • mechanism
A

natural pesticides found in high concentration in leaves, flowers, and unripe fruits
mechanism: they bind strongly to cholesterol in cell membranes causing cells to leak or burst open; also block acetylcholinesterase: lead to paralysis, convulsions, respiratory arrest, and death

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44
Q

Solanine

A

the alkaloid attacked to glucose chains (glycoalkaloid)

poorly absorbed by the gut and causes GI irritation.

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45
Q

Solanine and tomatine - anti-cancer activities

A

solanine: alpha solanine has anti-proliferation and an apoptosis promoting effect on multiple cancer cels
tomatine: binding of tomatine to cholesterol may be the mechanism of inhibition of carcinogenesis.

46
Q

Chili pepper - scientific name

A

Capsicum annuum

47
Q

Chili Pepper - part used

A

fruit

48
Q

Chili pepper - bioactive compound

A

Capsaicin

49
Q

Glutamate receptor

A
  • excites the cerebral cortex, spinal cord, brain stem, hippocampus, cerebellum
  • plays a critical role in long term potentiation (memory) and neuroplasticity
50
Q

Glutamate receptors types

A

1) ionotropic: NMDA, AMPA, Kainate

2) metabotropic: Group 1,2,3

51
Q

AMPA vs. NMDA receptors

A

1) AMPA: needs only one ligand (glutamate) and there is only a Na and K influx
2) NMDA: needs 2 ligands (glycine+glutamate); needs electrostatic repulsion to unplug Mg block (charges it), Ca Na and K influx

  • in both cases, Na goes in and K goes out of the membrane
52
Q

Excitotoxicity and cause

A

results from excessive stimulation of EXTRA-SYNAPTIC NMDA and AMPA receptors
conditions linked to excitotoxicity: stroke, traumatic brain injury, MS, Alzheimer’s, spinal injuries

53
Q

Synaptic vs. extra synaptic NMDA receptors

A

extra-synaptic: responsible for excitotoxicity and cell death
synaptic: contribute to health and longevity of cells

54
Q

Curcumin and extra-synaptic NMDA receptors

A

Curcumin attenuates NMDA-induced excitotoxicity

55
Q

Turmeric -scientific name

A

Curcuma longa

56
Q

Turmeric - part used

A

rhizome

57
Q

turmeric - bioactive compound

A

curcumin

58
Q

GABA - location and function

A

found in interneurons and everywhere in the CNS

inhibited the cerebral cortex, spinal cord, brainstem and hippocampus

59
Q

GABA - treatment uses

A

1) anxiety and rehab - too little GABA can cause generalized anxiety
2) inhibits motor, sensory and cognitive neurons
3) sedation, muscular/cardiovascular relaxation, inhibits pain, reflexes

60
Q

GABA receptors

A

1) ionotropic: GABAa

2) metabotropic: GABAb

61
Q

GABA a function

A
  • helps increase intracellular Cl ions

- contains: 2 subunits of GABA, barbiturates, benzodiazepine and channel for Cl influx

62
Q

“Benzos”

A
  • a class of psychoactive drug
  • sedative
  • hypnotic
  • anxiolytic
  • anti-convulsant
  • muscle relaxant
63
Q

“Barbs”

A
  • a class of psychoactive drug
  • potentially addictive
  • CNS depressant
  • Hypnotic
  • Anxiolytic
  • Anti-convulsant
64
Q

Glycine receptors - location

A

found in the spinal cord

65
Q

Glycine - function

A

inhibits spinal cord interneurons (same impact as GABA but mostly in the spinal cord)

66
Q

Glycine - treatment use

A

spasticity (abnormal increase in muscle tone and stiffness)

67
Q

glycine receptors

A

1) ionotropic: Cl channel

68
Q

glycine receptor and strychnine:

A

receptor can be selectively blocked by the high-affinity competitive antagonist strychnine.
- selective competitive antagonist of glycine

69
Q

where is strychnine made

A

in the seeds of strychnos nux-vomica (Loganiaceae)

70
Q

Strychnine tree - scientific name

A

strychnos nux - vomica

71
Q

strychnine - parts used

A

seeds

72
Q

strychnine mode of administration

A

ingestion, inhalation, injection

73
Q

Monoamine neurotransmitters

A
  1. serotonin
  2. dopamine
  3. norepinephrine
  4. epinephrine
74
Q

Catecholamines

  • examples
  • precursor
  • degradation
A

epinephrine and dopamine

  • tyrosine
  • degraded intracellularly by monoamine oxidase
75
Q

Indolamine

  • example
  • precursor
  • degradation
A
  • serotonin
  • tryptophan
  • degraded intracellularly by monoamine oxidase
76
Q

Ayahuasca - scientific name

A

Banisteriopsis caapi

77
Q

Ayahuasca - part used

A

stems and bark

78
Q

Ayahuasca - bioactive compound

A

Harmine

79
Q

The most abundant beta-carboline in B.caapi is ——

A

Harmine

80
Q

function of Harmine

A

1) inhibits the breakdown of monoamine transmitters (serotonin, dopamine) and hormones (melatonin, epinephrine, norepinephrine)
- as monoamine oxidase inhibitors, carmine can replenish levels of serotonin and dopamine - used to be utilized as an antidepressant
2) causes proliferation of alpha and beta cells of the pancreas
- inhibits the DYRK1A enzyme pathway - suppressing and regulating cell proliferation
- increase beta cell mass in people with type 1 and type 2 diabetes *

81
Q

ingredients for preparation of Ayahuasca that cause hallucination

A
  • DMT containing plants

e. g. Charcuna, Chagropanga, Jurema preta

82
Q

Non - DMT containing plants that are used for the preparation of Ayahuasca (used instead of Psychotria)

A
  • water willow (Justicia pectoralis)
  • Angel’s trumpets ( Brugmansia)
  • Aztec tobacco (Nicotania rustica)
83
Q

DMT is a derivative of ——

A

tryptamine

84
Q

DMT is responsible for:

A

hallucinogenic properties of Ayahuasca

85
Q

DMT in the body

A

monoamine oxidase in the stomach metabolize it before entering the blood stream

86
Q

DMT mechanism of action

A
  • acts as an agonist of 5-HT2a and 5-HT2c receptor
    The 5-HT2c shows desensitization with repeated exposure to DMT (no 5-HT2a)
  • also and agonist at 5-AT1a and increases the subjective effects of DMT, suggesting a buffering effect on the hallucinogenic effects of 5-HT2c
  • accumulates in the cerebral cortex, caudate, putamen, and amygdala
87
Q

Serotonin - location

A

found in the brain and brainstem

88
Q

Serotonin - treatment

A

1) depression

2) sleep

89
Q

receptors of serotonin

A

1) ionotropic: 5H3 (excitatory)

2) metabotropic: 5HT (1-7 receptors) - can be both excitatory or inhibitory depending on the tissue

90
Q

serotonin is produced by —— in the ——.

How:

A

enterochromaffin (EC) cells , digestive tract

- gut bacteria produce short chain fatty acids like butyrate that can influence the production of serotonin

91
Q

why is the link between depression and IBS strong

A

due to the brain gut axis

there are lots of nerves in the gut

92
Q

Functions of serotonin in the Brian

A

acts as a NT that regulates:

1) mood
2) fear
3) anxiety
4) feelings of relaxation
5) mental focus
6) learning ability
7) clarity of thought

93
Q

Functions of serotonin in the gut

A

acts as a hormonal messenger that regulates:

1) satiety
2) food cravings
3) digestion
4) nutrient abs
5) peristalsis

94
Q

Ergot - scientific name

A

Claviceps purpurea

95
Q

Ergot - parts used

A

Sclerotium

96
Q

Ergot - bioactive compound

A

ergotamine

97
Q

Ergotism - cause

A

ingestion of sclerotia of the parasitic fungus Claviceps purpurea

98
Q

Ergotism - types

A

1) serotonergic stimulation of CNS - muscle spams, fever and hallucinations
2) Vasoconstriction of the vascular system - violent burning, absent peripheral pulses and shooting pain of the poorly vascularized vital organs

99
Q

Morning glory - scientific name

A

Ipomea tricolor

100
Q

Morning glory - parts used

A

seeds

101
Q

Morning glory - bioactive compound

A

Ergine

102
Q

LSD - affects

A

causes altered thoughts, feelings, hyper awareness, dilates pupils, increases blood pressure and body temperature

103
Q

how are ergot alkaloids serotogenic

A
  • similar structure to serotonin, dopamine, and epinephrine. can being to several receptors and acts as an agonist
104
Q

how do ergot alkaloids cause vasoconstriction

A

through the stimulation of the alpha - adrenergic receptors.
Inhibits the uptake of norepinephrine

105
Q

How to raise serotonin levels naturally

A
Foods ( carbs increase tryptophan transport across the bloodstream-brain barrier)
Exercise (release tryp in to the blood)
Bright light 
mooD and mindset 
Massage 
Probiotics
106
Q

St. John’s Wort - scientific name

A

Hypericum perforatum

107
Q

St. John’s Wort - parts used

A

Flowers and buds

108
Q

St. John’s Wort - bioactive compound

A

Hyperforin and Hypericin

109
Q

St. John’s Wort - complication

A

photosensitivity

110
Q

potential function of hyperforin

A

displays a similar activity to other selective serotonin reuptake inhibitors (SSRIs) and with better tolerance
- helps with depression

111
Q

St. John’s Wort mechanism in relationship to drugs

A

induces the cytochrome p450 enzymes: CYP3A4 , CYP1A2

This increases the metabolism of certain drugs; thus, decreased clinical effects and plasma concentration