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
2
Q
Organs and glands affected by the parasympathetic gland
A
the liver, kidneys, pancreas, spleen, stomach, small intestines and colon
3
Q
Hormones and substances elevated by the sympathetic nervous system
A
insulin, cortisol, and the thyroid hormones
4
Q
hormones and substances elevated by the parasympathetic nervous system
A
pancreatic enzymes, bile and other digestive enzymes
5
Q
types of amino acid neurotransmitters
A
Glutamate, GABA, Glycine
6
Q
types of monoamine neurotransmitters
A
- Indolamines: Serotonin (a hormone, NOT a NT)
2. Catecholamines: Dopamine, Norepinephrine, Epinephrine
7
Q
type of purine neurotransmitter
A
Adenosine
8
Q
type of peptide neurotransmitter
A
Opioid
9
Q
Where is acetylcholine found
A
1) motor neuron
2) brain
3) autonomic nervous system
- sympathetic: Ganglion NT
- parasympathetic: Both ganglion and terminal
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.
11
Q
Acetylcholine receptors
A
1) ionotropic: nicotinic receptors
2) metabotropic: muscarinic receptors
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
13
Q
Tobacco scientific name(s)
A
1) Nicotiana rustica (Aztec tobacco)
2) Nicotiana tabacum
14
Q
Tobacco - parts used
A
Leaves
15
Q
Tobacco - Bioactive compound
A
Nicotine
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
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
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.
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
20
Q
Insufflation
A
the act of blowing something onto a body cavity
21
Q
expectorant
A
promotes the secretion of sputum (a mixture of saliva and mucus coughed up from the respiratory tract)
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
23
Q
Fly Agaric - scientific name
A
Amanita muscaria
24
Q
Fly Agaric - part used
A
Entire mushroom
25
Fly Agaric - bioactive compound
Muscarine
26
Function of muscarine
- 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
27
Treatment of muscarine toxicity
Atropine - a competitive reversible antagonist of muscarinic receptors
28
Muscimol
Cause of hallucinations and toxicity - it is a potent selective GABA a receptor agonist
- responsible for the drunkenness, sedative, depressant, euphoric and dissociative effect
29
Ibotenic acid
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
30
main psychoactive compounds of Amanita muscaria
muscimol and isotonic acid
31
Divination
represents a way to induce deep concentration and introspective thought
32
name the plants used for divination with their scientific name and main compounds
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
33
Jimson weed - scientific name
Datura stramonium
34
Jimson weed - parts used
Seeds/leaves
35
Jimson weed - bioactive compounds
Atropine, hyocamine, scopolamine
36
Fate of acetylcholine after being broken down by acetylcholinesterase
Choline is transported back into the axis terminal and is used to make more Ach
37
Anticholinergic Toxidrome
results from competitive antagonism of acetylcholine at central and peripheral muscarinic receptors
38
Anticholinergic Toxidrome symptoms
```
confusion
dry mouth
urinary retention
shaking
dilated pupils (mydriasis)
flushed skin
absent bowel sounds
tachycardia
hyperthermia
```
39
Anti-cholinergic
inhibits the transmission of the NT acetylcholine and suppress the parasympathetic nervous system
40
anti-cholinergic substances can cause:
amnesia, bizarre behaviour, and the inability to distinguish reality from fantasy (hallucination)
41
tropane alkaloids are -------
anti-cholinergenic
42
examples of anti-cholinegernic substances
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
43
Glycoalkaloids
- what are they
- mechanism
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
44
Solanine
the alkaloid attacked to glucose chains (glycoalkaloid)
| poorly absorbed by the gut and causes GI irritation.
45
Solanine and tomatine - anti-cancer activities
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
Chili pepper - scientific name
Capsicum annuum
47
Chili Pepper - part used
fruit
48
Chili pepper - bioactive compound
Capsaicin
49
Glutamate receptor
- excites the cerebral cortex, spinal cord, brain stem, hippocampus, cerebellum
- plays a critical role in long term potentiation (memory) and neuroplasticity
50
Glutamate receptors types
1) ionotropic: NMDA, AMPA, Kainate
| 2) metabotropic: Group 1,2,3
51
AMPA vs. NMDA receptors
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
Excitotoxicity and cause
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
Synaptic vs. extra synaptic NMDA receptors
extra-synaptic: responsible for excitotoxicity and cell death
synaptic: contribute to health and longevity of cells
54
Curcumin and extra-synaptic NMDA receptors
Curcumin attenuates NMDA-induced excitotoxicity
55
Turmeric -scientific name
Curcuma longa
56
Turmeric - part used
rhizome
57
turmeric - bioactive compound
curcumin
58
GABA - location and function
found in interneurons and everywhere in the CNS
| inhibited the cerebral cortex, spinal cord, brainstem and hippocampus
59
GABA - treatment uses
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
GABA receptors
1) ionotropic: GABAa
| 2) metabotropic: GABAb
61
GABA a function
- helps increase intracellular Cl ions
| - contains: 2 subunits of GABA, barbiturates, benzodiazepine and channel for Cl influx
62
"Benzos"
- a class of psychoactive drug
- sedative
- hypnotic
- anxiolytic
- anti-convulsant
- muscle relaxant
63
"Barbs"
- a class of psychoactive drug
- potentially addictive
- CNS depressant
- Hypnotic
- Anxiolytic
- Anti-convulsant
64
Glycine receptors - location
found in the spinal cord
65
Glycine - function
inhibits spinal cord interneurons (same impact as GABA but mostly in the spinal cord)
66
Glycine - treatment use
spasticity (abnormal increase in muscle tone and stiffness)
67
glycine receptors
1) ionotropic: Cl channel
68
glycine receptor and strychnine:
receptor can be selectively blocked by the high-affinity competitive antagonist strychnine.
- selective competitive antagonist of glycine
69
where is strychnine made
in the seeds of strychnos nux-vomica (Loganiaceae)
70
Strychnine tree - scientific name
strychnos nux - vomica
71
strychnine - parts used
seeds
72
strychnine mode of administration
ingestion, inhalation, injection
73
Monoamine neurotransmitters
1. serotonin
2. dopamine
3. norepinephrine
4. epinephrine
74
Catecholamines
- examples
- precursor
- degradation
epinephrine and dopamine
- tyrosine
- degraded intracellularly by monoamine oxidase
75
Indolamine
- example
- precursor
- degradation
- serotonin
- tryptophan
- degraded intracellularly by monoamine oxidase
76
Ayahuasca - scientific name
Banisteriopsis caapi
77
Ayahuasca - part used
stems and bark
78
Ayahuasca - bioactive compound
Harmine
79
The most abundant beta-carboline in B.caapi is ------
Harmine
80
function of Harmine
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
ingredients for preparation of Ayahuasca that cause hallucination
- DMT containing plants
| e. g. Charcuna, Chagropanga, Jurema preta
82
Non - DMT containing plants that are used for the preparation of Ayahuasca (used instead of Psychotria)
- water willow (Justicia pectoralis)
- Angel's trumpets ( Brugmansia)
- Aztec tobacco (Nicotania rustica)
83
DMT is a derivative of ------
tryptamine
84
DMT is responsible for:
hallucinogenic properties of Ayahuasca
85
DMT in the body
monoamine oxidase in the stomach metabolize it before entering the blood stream
86
DMT mechanism of action
- 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
Serotonin - location
found in the brain and brainstem
88
Serotonin - treatment
1) depression
| 2) sleep
89
receptors of serotonin
1) ionotropic: 5H3 (excitatory)
| 2) metabotropic: 5HT (1-7 receptors) - can be both excitatory or inhibitory depending on the tissue
90
serotonin is produced by ------ in the ------.
| How:
enterochromaffin (EC) cells , digestive tract
| - gut bacteria produce short chain fatty acids like butyrate that can influence the production of serotonin
91
why is the link between depression and IBS strong
due to the brain gut axis
| there are lots of nerves in the gut
92
Functions of serotonin in the Brian
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
Functions of serotonin in the gut
acts as a hormonal messenger that regulates:
1) satiety
2) food cravings
3) digestion
4) nutrient abs
5) peristalsis
94
Ergot - scientific name
Claviceps purpurea
95
Ergot - parts used
Sclerotium
96
Ergot - bioactive compound
ergotamine
97
Ergotism - cause
ingestion of sclerotia of the parasitic fungus Claviceps purpurea
98
Ergotism - types
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
Morning glory - scientific name
Ipomea tricolor
100
Morning glory - parts used
seeds
101
Morning glory - bioactive compound
Ergine
102
LSD - affects
causes altered thoughts, feelings, hyper awareness, dilates pupils, increases blood pressure and body temperature
103
how are ergot alkaloids serotogenic
- similar structure to serotonin, dopamine, and epinephrine. can being to several receptors and acts as an agonist
104
how do ergot alkaloids cause vasoconstriction
through the stimulation of the alpha - adrenergic receptors.
Inhibits the uptake of norepinephrine
105
How to raise serotonin levels naturally
```
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
St. John's Wort - scientific name
Hypericum perforatum
107
St. John's Wort - parts used
Flowers and buds
108
St. John's Wort - bioactive compound
Hyperforin and Hypericin
109
St. John's Wort - complication
photosensitivity
110
potential function of hyperforin
displays a similar activity to other selective serotonin reuptake inhibitors (SSRIs) and with better tolerance
- helps with depression
111
St. John's Wort mechanism in relationship to drugs
induces the cytochrome p450 enzymes: CYP3A4 , CYP1A2
| This increases the metabolism of certain drugs; thus, decreased clinical effects and plasma concentration
