Lecture 7 - Plants that affect purine receptors - Stimulants and Sedatives Flashcards
Where is dopamine found:
In the brain and brainstem
- substantia nigra (reward, addiction, movement)
- hypothalamus (inhibits prolactin release)
Dopamine can be used to treat:
- Schizophrenia, psychosis
- Parkinson’s disease
What are the dopamine receptors:
- ionotropic = none
- metabotropic = D1 excitatory (K+/Ca2+), D2 inhibitory (K+/Ca2+)
What are the 3 dopamine pathways in the brain:
1) Mesocorticolimbic pathway (mood/reward)
2) Nigrostriatal pathway (movement)
3) Tiberoinfundubular pathway (no prolactin)
Coca - Sheet
- Scientific name:
- Part used:
- Mode of administration:
- Bioactive compound:
- Compound class:
- Uses:
- Erythroxylum coca
- Leaves
- Chewed, insufflation, inhalation
- Cocaine
- Alkaloid
- Stimulant, increased endurance
T or F: When coca leaves are consumed, effects of stimulant are felt after a few minutes and doesn’t produce jitteriness - may be more powerful than caffeine in producing a good mood
T
Made by mixing leaves with an organic solvent and mashing them. When the solvent evaporates, a coca paste remains. The paste is further refined to _______________
cocaine hydrochloride
T or F: Cocaine causes loss of contact with reality and euphoria. Effects begin within seconds to minutes and lasts 5-90 minutes
T
Why is cocaine addictive?
Due to the effects on dopamine reward pathway., High risk of dependence.
T or F: With cocaine, there are risk of stroke, heart attack, lung problems, blood infections, sudden cardiac death
T
T or F: Cocaine blocks reuptake of monoamine neurotransmitters - dopamine, norepinephrine and serotonin
T
Cocaine leads to increased available synaptic transmitters, chronic use leads to decreased availability of ___ receptors
D2
___________ causes profound mental stimulation: increased talkativeness, flight of ideas, euphoria, and inflated self-esteem: Fatigue is offset and there’s reduced need to sleep
Cocaine
Norepinephrine is found in the ________
brain (ANS - sympathetic neurons)
Norepinephrine is used to treat:
- anxiety
- AHDD
- cardiac failure
Name the norepinephrine receptors:
-ionotropic = none
-metabotropic:
a1 + b1 = excitatory
a2 + b2 = inhibitory
Ephedra - Sheet
- Scientific name:
- Part used:
- Mode of administration:
- Bioactive compound:
- Compound class:
- Uses:
- Ephedra sinica
- Dried stems, root
- Infusion
- Ephedrine, Pseudoephedrine
- Alkaloid
- Stimulant, Thermogenic
Ephedrine is a CNS stimulant similar to ______________
amphetamines
Explain the ephedrine mechanism of action:
1) Ephedrine enters pre-synaptic neuron via the NET
2) It enters the synaptic vesicle via the VMAT
3) Norepinephrine is released into cytoplasm and released into the synaptic cleft by NET
T or F: Purines are part of our DNA
T
Purines are found in:
- Brain, heart, kidneys, and adipose tissue (P2Y & P1 receptors)
- Neurons and glial cells throughout CNS & PNS (P2X receptors)
Purines are used to treat:
Supraventricular tachycardia
Purines receptors:
- ionotropic: P2X receptors (ATP)
- metabotropic: P1 receptors (Adenosine) and P2Y receptors
__________ receptors are the oldest and most abundant in all living organisms
Purinergic
The ionotropic P2X receptor binds ____ and evolved over a billion years ago
ATP
In _____, ATP and adenosine play an important role in sleep
CNS
Extracellular adenosine levels in basal forebrain are _____ during sleep and _____ during sleep deprivation
lower
higher
___________ is a sleep-promoting substance - decreases the activity of cholinergic neurons
Adenosine
T or F: An increase in adenosine reflects an increased breakdown of cellular ATP
T
Adenosine regulation of sleep is mediated by ___ and ____ receptors
A1 and A2
T or F: Caffeine is a CNS stimulant
T
Caffeine acts as an _____________ for all adenosine receptors
antagonist
Antagonistic effects of caffeine on the ______ receptor is responsible for alertness
A2A
Coffee - Sheet
- Scientific name:
- Part used:
- Mode of administration:
- Bioactive compound:
- Compound class:
- Uses:
- Coffea arabica
- seed
- Infusion/percolation
- Caffeine
- Alkaloid
- Sitmulant
Coffee was discovered in ___________ in the 9th century
Ethiopia
T or F: Coffee drinkers tend to live longer: they have a reduced risk of CVD, T2DM and Parkinson’s disease
T
Tea - Sheet
- Scientific name:
- Part used:
- Mode of administration:
- Bioactive compound:
- Compound class:
- Uses:
- Camellia sinensis
- leaves
- infusion
- epigallocatechin gallate (EGCG)
- Catechin Polyphenol
- Antioxidant, anticancer, antimicrobial
Cocoa - Sheet
- Scientific name:
- Part used:
- Mode of preparation/administration:
- Bioactive compound:
- Compound class:
- Uses:
- Theobroma cacao
- Seeds
- Roasting
- Theobromine
- Alkaloid
- Vasodilator, diuretic, heart stimulant
Yerba Maté - Sheet:
- Scientific name:
- Part used:
- Mode of preparation/administration:
- Bioactive compound:
- Compound class:
- Uses:
- Ilex paraguariensis
- Leaves + Stem
- Infusion
- Theobromine
- Alkaloid
- Stimulant
T or F: Advocates of Yerba Maté view it as healthful, noting that it contains vitamins, antioxidants, and anti0carcinogens. Heavy use, however, has been correlated with increased incidence of esophageal cancer, which is generally thought to result from the traditional method of consumption: sipping the liquid pipping hot through a metal straw out of a heat-retaining gourd
T
Guarana - Sheet
- Scientific name:
- Part used:
- Mode of administration/preparation:
- Bioactive compound:
- Compound class:
- Uses:
- Paullinia cupana
- Seeds
- Roasted
- Caffeine
- Alkaloid
- Stimulant
Overdose of caffeine occurs above ______
400 mg
What are some symptoms associated with caffeine intoxication:
- restlessness
- fidgeting
- anxiety
- excitement
- insomnia
- flushing
- increased urination
- GI disturbance
- rapid heart beat
- rambling flow or thought and speech
___________ plants that induce CNS depression must either facilitate neuron inhibition or inhibit the neuronal excitation
Herbal sedatives
Herbal sedatives can act as (3):
1) GABA receptor agonists
2) Glutamate receptor antagonists
3) Blocking of voltage-gated ion channels
Valerian - Sheet:
- Scientific name:
- Part used:
- Mode of preparation/administration:
- Bioactive compound class:
- Compound class:
- Uses:
- Valeriana officinalis
- Root & Rhizomes
- Decoction
- Valerenic acid
- Sesquiterpene
- Sedative
T or F: Valerian’s bioactivity may be due to additive / synergistic effects from several compounds
T
The synergistic effects of Valerian come from several compounds that fall in 3 main phytochemical categories:
- Monoterpenes
- Sesquiterpenes
- Alkaloids
Explain the 2 likely mechanism of action of Valerian:
1) Facilitates GABA release and reversal of uptake
2) Inhibition of GABA breakdown
Chamomile - Sheet
- Scientific name:
- Part used:
- Mode of preparation / administration:
- Bioactive compound:
- Compound class:
- Uses: sedative
- Matricaria recutita
- Dried flowers
- Infusion
- Apigenin
- Flavonoid
T or F: If you take to much Apigenin, that might impact your estrogen levels (keep estrogen level high)
T
Sedative and anxiolytic effects of Chamomile are likely mediated by the ability of Apigenin to:
-bind benzodiazepine receptors on GABAa
Kava - Sheet
- Scientific name:
- Part used:
- Mode of preparation/administration:
- Bioactive compound:
- Compound class:
- Uses:
- Piper methysticum
- Rootstalk
- Infusion
- Kavain
- Kavalactone
- Sedative anxiolytic
What are Kava’s 4 main mechanisms:
1) Facilitates GABA transmission
2) Voltage-gated ion channels, inhibits Na+ channels and subsequent release of glutamate
3) Monoamine - Kavolactones inhibit monoamine oxidase B and reduce inflammation
4) Eicosanoids: kavain inhibits COX, supressing synthesis of thromboxane A2. In turn, lower thromboxane A2 increases GABA function
A neurological disorder characterized by jerky involuntary movements affecting especially the shoulders, hips and face:
Chorea
A habitual spasmodic contraction of the muscles, most often in the face:
Tics
A condition in which abnormal muscle contractions cause involuntary writhing movements. If affects some people with cerebral palsy, impairing speech and use of hands:
Athetosis
Caused increased passing of urine:
Diuretic
