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Terms in this set (60)
Distort perception of reality, but confusion, memory loss and disorientation rarely occur. (Exception, cholinergic compounds)
Induce psychotic states, but true psychoses are different from those observed with hallucinogens.
Plant Hallucinogenic Compounds
A) Monoamine (adrenergic) targets and pathways (Indole and catechol hallucinogens)
B) Amino Acid targets and pathways
C) Cholinergic Targets and Pathways (Anticholinergic hallucinogens)
D) Other (Cannabinoids and those that bind to opioid receptors, like Salvinorin A)
A) Monoamine Hallucinogens
Indole and Catechol hallucinogens:
-targets similar pathways involving serotonin, but the compounds are structurally different. Vivid sensory effects. Perception altered, but still aware of real world. Low toxicity.
Indole Alkaloids: Have indole component to their structure. Ex: Claviceps purpurea.
Parasitic fungus: claviceps purpurea. Insects deposit spores on grain, fungus grows hyphae into ovaries of grain. Cattle and humans got ergotism, which was nervous spasms, convulsions, and gangrene.
St. Anthony's Fire
St Anthony's Shrine was a pilgrimage for those seeking a cure to St. Anthony's fire. Making the pilgrimage meant getting away from the infected grain, as well as an increase in periphery circulation, which may explain the healing.
CNS and PNS neurotransmitter involved in mood, sleep, appetite, pain, temperature, anxiety, etc.
Compounds of Ergot
Alkaloid compounds of ergot, collectively from ergoline, show antagonist and agonist action at dopamine, serotonin, and adrenergic receptors.
Uterine contractions. Ergoline causes vasoconstriction --> Extreme burning and gangrene. Seizures and hallucinations. Symptoms caused by all ergot compounds working simultaneously.
Modern uses of Ergot compounds
Reduce prolactin levels from pituitary tumors. Reduce migraines and postpartum hemmorage. Treat Alzheimers dementia.
d-lysergic acid diethylamide. Synthetic compound derived from ergoloids (like lysergic acid). Most intense of lysergic acid derivatives. Lasts 6-12 hours. Has rapid tolerance after 4 days, and is cross-tolerant with other monoamine hallucinogens. Not addictive, no withdrawal, and hard to overdose.
LSD and other indole alkaloids regulate serotonin pathways. LSD binds to serotonin-type receptors (5HT receptors). Has both agonist and antagonist effects. Tolerance occurs due to downregulation of certain serotonin receptors.
Vivid intensification of real life shapes, colours, emotions, etc. Bad trip caused by fear it will never end and bad environment. Flashbacks may occur, due to perceptive disorder.
Morning glories also contain lysergic acid, a dose is enough seed to fill a beer cap. Turbina corymbosa. Put in cold water, filtered, and drunk. Used my mexican natives, aztecs.
Another monoamine indole alkaloid
Psilocybe mexicana: A psychedilic mushroom. Psilocybin and psilocin are compounds that are stucturally similar to serotonin. They have effects similar to lysergic acid or LSD, but only last 3 hours.
Monoamine catechol hallucinogens
Peyote: Lophophora williamsii. The alkaloid compound is mescaline, but the psychoactive effects of peyote arent exactly the same as those of pure mescaline.
Pharmacology of Mescaline
Physiological effects are similar to those of the monoamine indole compounds, but structurally they are different, as these contain a catechol group. Mescaline is readily absorbed by the body, but passes through the BBB poorly. Increases pulse rate, blood pressure, and temp. Dilates pupils.
Catechol Hallucinogenic Structures
Includes dopamine, mescaline, and catechol. All contain a catechol group. Mescaline resemles norepinephrine and dopamine, catecholamine receptors. Effects are, like monoamine indole compounds, via serotonin receptor interactions. Pharmacologically similar to LSD, but weaker.
History of Peyote
Priests of aztecs, mexicans. Today Native churches eat the mescal buttons. Weightlessness, freedom of body, exaltation, etc. Peyote is prepared by cutting the top into slices. Remains psychoactive indefinitely.
Myristica fragrans: Also contains a catecholamine compound, myristicin. Powdered nutmeg is often snuffed or chewed, but bad hangover. Mace of fruit is also used.
Terpenoid compound, user experiences trance, weightlessness, colours, etc., like peyote.
B) Amino Acid targets and pathways
Includes ibotenic acid and muscimol.
Fly agaric Mushroon
Amanita muscaria. Grows under birch and fir trees. Contains multiples psychoactive compounds
Compounds of Amanita muscaria
Contains muscimol, ibotenic acid and muscarine (not psychoactive). Drying may transform ibotenic acid into muscimol.
Ibotenic Acid mechanism
Activates NMDA and some metabotropic glutamate receptors. Glutamate binds to ion channels or G-protein coupled channels. Ion channels release Ca++ or Na+, which cause excitatory responses. Therefore, glutamate is an excitatory neurotransmitter.
Most active compound in amanita muscaria. GABA is an inhibitory neurotransmitter, even though derived from glutamate. Muscimol is a GABA receptor agonist, and activates GABA receptors that are chloride channels. Produces state of confusion, disorientation, decrease in cognitive ability.
Muscarine binds to muscarinic acetylcholine receptors, and elicits an excitatory response in the vagus nerve of frogs. No psychoactive role.
Effects of the fly agaric (amanita muscaria)
Derangement of senses, manic behaviour, want for exaggerated physical activity, altered size perceptions, 12 hours later deep sleep.
C) Cholinergic Targets and Pathways
Anticholinergic Hallucinogens include Atropa belladonna, hyoscyamus niger, datura stramonium, and mandragora officinarum. All belong to the plant family Solanaceae. Each plant produces a combo of 3 compounds: Atropine, Hyoscyamine, and Scopolamine.
Anticholinergic experiences are different than monoamine experiences, as anticholinergic hallucinogens induce dream like delirium, as well as amnesia. They are also highly toxic. The compounds (scopolamine, hyoscyamine, and atropine) are all tropane alkaloids
Atropine, Hyoscyamine and Scopolamine
Produce peripheral effects through the parasympathetic nervous system. Scopolamine produces CNS and hallucinogenic effects too, and passes BBB. Alkaloid concentration highest in roots, and are toxic. Drying can lead to more atropine and scopolamine.
Historical use of Anticholinergic Plants
Witches used these tropane alkaloids to rub onto broomsticks. The alkaloids passed through skin easily, and made witches feel weightless, etc. These fat soluble alkaloids avoid toxic effect by avoiding GI tract. Also associated with lycanthropy. Dry mouth, blurred vision, etc. of this caused by the antagonist reactions of anticholinergic compounds at muscarinic receptors.
Contains mostly hyoscyamine. Few berries enough, tended by devil, dilates pupils of women, etc.
Henbane, mostly hyoscyamine. Poisonous, used for flying and prophetic dances, seeds are smoked.
Many species of datura contain all 3 alkaloids in the leaves and seeds. Treats cold and nervous disorders, datura stramonium is used for hallucinogenic properties, cultivated for scopolamine. Virgins would chew datura on inhale, their ramblings would be recorded by holy men. Also used to capture, and sprayed in the faces of people in Columbia. Datura also credited for defeat of British troops at Jamestown.
Contains all 3 alkaloids in the taproot of the plant. Associated with fertility and love.
Doctrine of Signatures
Metaphysical method of discovering use of plant. Walnuts cure head things because look like the brain, foxglove for heart problems because it looks like blood vessels on leaves, etc.
Identification of Cellular Receptors
Cellular receptors are indentified by using drugs and monitoring the effects. Ex: Muscarinic treat mimics the action of the parasympathetic nervous system at effector cells, thus called muscarinic receptors. Nicotinic action stimulates autonomic ganglia that innvervate parasympathetic and sympathetic neurons, as well as skeletal muscle.
Acetylcholine is an endogenous neurotransmitter that stimulates both nicotinic and muscarinic receptors!
Nicotinic acetylcholine receptors: ion channels involved in action potential propagation.
Muscarinic acetylcholine receptors: Couple w/ G proteins, that activate intracellular signalling pathways.
Anticholinergic Hallucinogenic Compounds
Atropine, scopolamine, hyoscyamine. Reversible competitive antagonists at muscarinic acetylcholine receptors.
To understand physiological action: 1) Understand effects of acetylcholine binding to the muscarinic receptors.
2) Determine what blocking this action would do.
Activation at Muscarinic Receptors
Located in CNS, and pre/post-ganglionic neurons of primarily parasympathetic, but also sympathetic. Cholinergic system in CNS modulates dopamine and other neurotransmitters in brain.
Parasympathetic effects: Increased salivation, gut motility, high doses: reduce heart rate and blood pressure, constrict pupils. Anticholinergic alkanoid tropanes would have the opposite effect.
Anticholinergic effects of atropine, hyoscyamine, and scopolamine.
Rapid increase in heart rate (no effect of blood pressure), reduce gut motility, decrease salivation, dilation of pupils, block mucous production.
Medicinal uses of atropine
dilates pupils, datura smoked to relieve asthma. Pre-anaesthetic for animals. Increases heart rate, and counteracts acetylcholine level-raising poisons. Atropine poisoning means excited CNS (confusion, restlessness, etc.) and then to respiratory failiure, paralysis, etc.
History of scopolamine use
Used for sedative effects in wars. Causes delirium, confusion, loss of memory, drowsiness, and death.
Natives dip corkwood tree plant into eel pools to make the eels lethargic. Dubosia.
Scopolamine demand much higher than for atropine or hyoscyamine. Can meet demand through genetic engineering, cultivation, or cell culturing.
Genetic Engineering of Scopolamine (1st way)
Produced from hyoscyamine. Step 1) Find plant with high hyoscyamine levels. Encode the plant DNA's hyoscyamine 6B (H6H) enzyme. Plant will then produced scopolamine.
Two plants used: Henbane (hyoscyamous niger) and Atropa belladonna. Henabe has both an active H6H gene, and high levels of H6H enzymes, but its hard to grow. Atropa belladonna has low levels of H6H enzymes, but is easy to grow.
Why the difference in enzyme production>
Normally an RNA polymerase binds to the promoter region of the gene, initiating transcription (the mRNA transcript is translated into protein, the active enzyme). But differences in non coding sequences in the genes effect how much transription occurs.
Production of constitutively produced H6H enzyme
Take H6H sequence from henbane, and to increase production of H6H enzyme even more, a constitutively active promoter sequence is added. This chimeric gene is then transformed into the more easily grown Atropa belladonna.
Use a bacteria that transfers its DNA to the plant, and modify the T-DNA. Thereby H6H enzyme can be passed into Atropa belladonna.
Scopolamine production method 2:
Transform hyoscyamus species with genes encoding H6H and PMT using another bacteria. This uses hairy root formation to induce desired compound production. Similar to before, but this uses several enzymes.
Method 2 continued:
This bacteria also transfers its DNA to the plant. Plant hormones change during infection, and hairy roots are produced at the site of wounding. Hairy roots can be cultured on a large scale to enhance compound production.
Scopolamine Production Summary:
1) Transfer H6H gene with constitutive promoter into Atropa belladonna using T-DNA bacteria. Plant's hyoscyamine is then converted into scopolamine.
2) Transform H6H gene into tropane alkaloid producing plant with another bacteria. Hairy roots are produced, scale up hairy roots that produce high levels of scopolamine.
Annual, very old. Bast fibers produce hemp, which is very strong. Seeds rich in oil. Used historically to easy pain, induce sleep, calm nervous disorders. Psychoactive compounds in leaves and flowering tops. Smoke contains many compounds, which constantly change while being smoked. The main psychoactive ingredients are cannibanoids, which are lipid soluble.
Major psychoactive ingredient in marijuana. Lipid soluble phenolic and terpenoid compounds. THC is the most active of the tetrahydrocannabinols. THC is concentrated in resin (sub-epidermal, young plants). THC packaged in surface trichomes.
Harvesting psychoactive ingredients from Cannabis
1) Pure resin removed from the young leaves/flowers.
2) Male plants removed, so female plants continually produce THC. Female plant material then dried.
3) Use parts of plant after the top leaves have been picked.
4) Boil whole plant in alcohol, then evaporate. What is left is thick hash oil, strongest by far.
Smoking, THC rapidly reaches brain and body, causing mild sedation, hallucination and tranquilization. Sense of mild euphoria and well being, dry, thirsty and hungry. Heart rate increases, bronchial passages relax, and its metabolized in the liver. Agonist at CB1 and CB2 receptors in brain. G-protein linked. Also a natural ligand (anandamide)
Uses of THC
Asthma, glaucoma, anorexia, nausea caused by radiotherapy, etc.
Psychoactive properties have prevented its economic use. Overall, its not that effective, possible link to cancer, and damages brochiole tubes.
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