Lecture 3: Plants that affect acetylcholine receptors Flashcards
Organs and glands activated by the sympathetic nervous system
brain, muscles, the pancreas, thyroid gland and adrenal glands
Organs and glands affected by the parasympathetic gland
the liver, kidneys, pancreas, spleen, stomach, small intestines and colon
Hormones and substances elevated by the sympathetic nervous system
insulin, cortisol, and the thyroid hormones
hormones and substances elevated by the parasympathetic nervous system
pancreatic enzymes, bile and other digestive enzymes
types of amino acid neurotransmitters
Glutamate, GABA, Glycine
types of monoamine neurotransmitters
- Indolamines: Serotonin (a hormone, NOT a NT)
2. Catecholamines: Dopamine, Norepinephrine, Epinephrine
type of purine neurotransmitter
Adenosine
type of peptide neurotransmitter
Opioid
Where is acetylcholine found
1) motor neuron
2) brain
3) autonomic nervous system
- sympathetic: Ganglion NT
- parasympathetic: Both ganglion and terminal
Function of acetylcholine
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.
Acetylcholine receptors
1) ionotropic: nicotinic receptors
2) metabotropic: muscarinic receptors
nicotinic receptors vs. muscarinic receptors
nicotinic: opens very simple and fast. Ligand binds - open - response
muscarinic: ligand - conformational change - activation of G protein subunits - release of secondary messengers - response
Tobacco scientific name(s)
1) Nicotiana rustica (Aztec tobacco)
2) Nicotiana tabacum
Tobacco - parts used
Leaves
Tobacco - Bioactive compound
Nicotine
Nicotine mechanism
- 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
what are PAM(s)
they are called positive allosteric modulators - other things required for the agonistic binding of nicotine and nicotinic acetylcholine receptors
development of nicotine addiction
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.
tobacco and cancer/atheroscelrosis
- 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
Insufflation
the act of blowing something onto a body cavity
expectorant
promotes the secretion of sputum (a mixture of saliva and mucus coughed up from the respiratory tract)
Ethneogenic
a drug that causes one to become inspired or to experience feelings of inspiration, often in a religious or spiritual manner
Fly Agaric - scientific name
Amanita muscaria
Fly Agaric - part used
Entire mushroom
Fly Agaric - bioactive compound
Muscarine
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
Treatment of muscarine toxicity
Atropine - a competitive reversible antagonist of muscarinic receptors
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
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
main psychoactive compounds of Amanita muscaria
muscimol and isotonic acid
Divination
represents a way to induce deep concentration and introspective thought
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
Jimson weed - scientific name
Datura stramonium
Jimson weed - parts used
Seeds/leaves
Jimson weed - bioactive compounds
Atropine, hyocamine, scopolamine
Fate of acetylcholine after being broken down by acetylcholinesterase
Choline is transported back into the axis terminal and is used to make more Ach
Anticholinergic Toxidrome
results from competitive antagonism of acetylcholine at central and peripheral muscarinic receptors
Anticholinergic Toxidrome symptoms
confusion dry mouth urinary retention shaking dilated pupils (mydriasis) flushed skin absent bowel sounds tachycardia hyperthermia
Anti-cholinergic
inhibits the transmission of the NT acetylcholine and suppress the parasympathetic nervous system
anti-cholinergic substances can cause:
amnesia, bizarre behaviour, and the inability to distinguish reality from fantasy (hallucination)
tropane alkaloids are ——-
anti-cholinergenic
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
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
Solanine
the alkaloid attacked to glucose chains (glycoalkaloid)
poorly absorbed by the gut and causes GI irritation.