10: Nootropics Flashcards
- nootropic termed by which scientific in what year?
- that scientist synthesized what? in what read?
- mechanism of action ish?
- acts on what?
- Dr. Cornelie E. Giurgia in 1972
- synthesized Piracetam in 1964
- mechanism of action is not well understood, but it isn’t a sedative or stimulant –> it is a POSITIVE ALLOSTERIC MODULATOR OF THE GLUTAMATE AMPA RECEPTOR (BOLD) that is colocalized with cholinergic receptors
- also acts on ion channels or ion carriers
only know in CAPS
what are 4 types of nootropics + examples
- RACETAMS
- originals
- piracetam, oxiracetams, phenylpiracetam, aniracetam - CNS STIMULANTS
- amphetamines (Adderall) (not natural)
- methylphenidate (Ritalin) (not natural)
- caffeine and nicotine (natural) - HERBS
- gingko biloba
- panax ginseng
- bacopa monnieri (bacopa)
- hyperzia serrata (Huperzine A)
- Plectranthus barbatus (Forskolin from indian coleus)
- Hericium erinaceus (Lion’s mane mushroom) - NUTRIENTS
- phosphatidylserine
- alpha-glycerophosphocholine
- L-tyrosine
only know the 6 herbs ish
what are 6 ways nootropics work?
(memory the titles, not too much detail)
- brain energy
- enhance metabolic activity and FA transport of/to mitochondria + enhance O2 and nutrient uptake - brain chemicals:
- supplies precursors, increases synthesis, receptor sensitivity and inhibits breakdown of neurotransmitters (ACh, DA, 5HT, NE, E, GABA) - increase cerebral blood flow
- promotes NO + vasodilation
- inhibits homocysteine and oxidative damages to cells + AGEs - brain waves:
- 5 brain waves
- some nootropics (L-theanine) can raise alpha brain waves (mild, meditative state for free-flowing creativity) - neuroprotection
- increase brain’s antioxidant capacity, help fight formation of irregular protein clusters, clearing brain tissue of neurotoxins, protecting brain against negative effects of stress - brain regeneration
- boost natural brain-boosting growth factors, provide raw neuronal building block materials, maintain brain cell membrane flexibility and plasticity
what are the main functions ish of the main neurotransmitters in brain?
ACh
DA
5HT
NE
EPI
GABA
ACh: memory, learning and basic thinking cognition
DA: mood and motivation, pleasure-reward pathway
5HT: relaxation and deep satisfaction (happy hormone)
NE: attention and intense focus
EPI: (adrenaline), intense energy
GABA: downer, sedation and calmness, inhibits excessive excitation
what are 3 categories of synthetic nootropics?
- RACETAMS
- piracetam, oxiracetams, phenylpiracetam, aniracetam - CNS STIMULANTS
- amphetamines (Adderall)
- methylphenidate (Ritalin) - EUGEROICS
- modafinil
what are 6 natural nootropics?
- gingko biloba (Gingko)
- panax ginseng (ginseng)
- bacopa monnieri (bacopa)
- hyperzia serrata (Huperzine A)
- Plectranthus barbatus (Forskolin from indian coleus)
- Hericium erinaceus (Lion’s mane mushroom)
gingko (monograph):
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: gingko biloba
- PART USED: leaves and roots
- MODE OF ADMINISTRATION: tincture, extract
- BIOACTIVE COMPOUND: ginkgolides
- COMPOUND CLASS: terpene lactone
- USES: cognitive enhancer, anxiolytic, enhances blood flow (to brain!)
what are 4 mechanisms of action of gingko?
KNOW THIS!
- cholinergic:
- increase uptake and release of Ach = increase memory - monoamine
- increase uptake of serotonin
- inhibits MAO
- reduces b-adrenergic binding and activity
- reverses age-related decline in a-adrenergic receptors - GABA
- elevates GABA levels
- increases glutamic acid decarboxylase activity = degrades glutamate - VASCULAR
- platelet activation factor inhibitor
- nitric oxide dependent vasodilation
describe gingko’s mechanism of action: cholinergic
- enhances what?
- where?
- increases what?
- short vs long term memory (VERY IMPORTANT) + where in the brain it occurs
- gingko enhances release of ACh and alters cholinergic receptors
- hippocampus: increased presynaptic uptake of choline!
- increase in choline uptake due to increase in number of uptake transporters and rate of transport
SHORT-term memory tasks increase uptake of ACh
LONG-term memory reference memory tasks cause an acute increase followed by long-lasting decrease and inhibition (?)
describe gingko’s mechanism of action: monoamines
- 4 sub + describe
- increase uptake of serotonin
- inhibits MAO (MAO metabolizes NE, 5HT, DA)
- reduces b-adrenergic binding and activity
- reverses age-related decline in a-adrenergic receptors
(no questions about adrenergic receptor)
describe gingko’s mechanism of action: GABA
(2)
- elevates GABA levels –> bilobalide (bold), a terpene lactone in Gingko, elevates GABA in hippocampus
- increases glutamic acid decarboxylase activity = degrades glutamate
*glutamic acid decarbozylase catalyzes the decarboxylation of glutamate (exciting) into GABA (relaxing)
describe gingko’s mechanism of action: vascular
(4)
know big headlines
- inhibits platelet-activating factor –> PAF is a chemical messenger with many biological roles like aggregation of blood platelets
- inhibit PAF improves microcirculation! - nitric oxide dependent vasodilation
- gingko improves sexual function by increasing NO production (involved in erections) - potent antioxidant activity
- flavonoid glycosides: kaempferol, quercetin, apigenin, luteolin, myrcetin - cerebral blood flow: increases blood flow to multiple regions in brain
ginseng (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: panax ginseng
- PART USED: root
- MODE OF ADMINISTRATION: chewed, infusion, extract
- BIOACTIVE COMPOUND: ginsengosides
- COMPOUND CLASS: steroid glycosides (cholesterol backbone)
- USES: cognitive enhance + adaptogen
ginseng: 5 mechanisms of action
- cholinergic: increased ACh release and nicotinic binding
- MONOAMINES: turnover of DA, NE and 5HT is increased or decreased depending on dose and duration of use
- NO: enhances epithelial synthesis in heart, lungs and kidney
- NEUROTROPHIC: increase nerve growth factor (NGF) expression
- Ca2+ influx: inhibits calcium channels
ginseng general effects
- lowers what?
- MAY do 5 things
- lowers inflammation (too much electrons) due to antioxidant content
MAY: - help improve memory, behaviour and mood
- help protect against oxidative damage
- improve symptoms of erectile dysfunction by decreasing oxidative stress
- protect from cancer (ginsenosides help reduce inflammation and help prevent certain cancers)
- help fight fatigue and enhance PA by lowering oxidative damage
Bacopa (Brahmi) (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: bacopa monnieri
- PART USED: leaves and stem
- MODE OF ADMINISTRATION: juice
- BIOACTIVE COMPOUND: bakosides
- COMPOUND CLASS: triterpenoid saponin
- USES: cognitive enhancer
4 mechanisms of action of bacopa
- ANTIOXIDANT/ NEUROPROTECTION
- prevent lipid peroxidation (involved in Alzheimer’s, Parkinson’s dementia…) - CEREBRAL BLOOD FLOW AND VASODILATION
- vasodilator by releasing NO in endothelium - NEUROTRANSMITTER POTENTIATION
- bacopa doubled levels of 5HT (can help enhance learning and memory). glutamate and ACh increased slightly. DA levels lowered - ADHD: (dont need to know)
- 1 study showed bacopa reduced ADHD symptoms like restlessness, poor self control, inattention and impulsivity
firmoss (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: Huperzia serrata
- PART USED: clubmoss
- MODE OF ADMINISTRATION: isolated compound
- BIOACTIVE COMPOUND: Huperzine A
- COMPOUND CLASS: sesquiterpene alkaloid
- USES: cognitive enhancer
Huperzine A (huperzia serrata)
- acts as (2) and crosses what?
used in china to treat what?
- acts as acetylcholinesterase inhibitor AND NMDA antagonist that crosses blood brain barrier!
- as an NMDA receptor (glutamate receptor) antagonist –> can help prevent neurons from cell death from excitotoxicity
- China: swelling, fever, blood disorders
indian coleus (monograph) (ON EXAM!)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: coleus foskolii (plectranthus barbatus)
- PART USED: roots
- MODE OF ADMINISTRATION: isolated compound
- BIOACTIVE COMPOUND: forskolin
- COMPOUND CLASS: labdane diterpene
- USES: cognitive enhancer
Forskolin
- from which plant?
- used for what?
- mechanism of action (2)
- synergistic with what?
- anti ___________ effects
- from indian coleus (coleus foskolii)
- used as weight loss –> may stimulate release of stored fat from fat cells (Dr. Oz lol)
UNIQUE among nootropics:
1. increases intracellular levels of cAMP through adenylate cyclase activation –> increased responsiveness to extracellular stimuli
2. inhibits acetylcholinesterase –> increased ACh levels - synergistic with artichoke extract in increasing cAMP levels
- anti-inflammatory effects
KNOW ALL THIS!
why does _______ work better with artichoke extract? (4 steps ish)
KNOW THIS!
forskolin! might work as a nootropic, but might work better as part of a “stack”
1. artichoke extract contains LUTEOLIN, a powerful phosphodiesterase (PDE4) inhibitor
2. excess PDE4 degrades cAMP (intracellular messenger within brain cells)
3. cAMP produces proteins needed for neuron and synapse growth, a process called long-term potentiation (LTP) (process where synaptic connections get stronger in response to electrical stimulation in brain
4. PDE4 inhibitor = no more degradation of cAMP = lots of cAMP for LTP!
schéma steps of how forskolin and luteolin can increase protein phosphorylation and LTP!
- agonist of ACh binds to receptor –> activates metabotropic receptor/G-protein (leads to activation of adenylate cyclase)
- Forskolin activates AC –> convers ATP to cAMP
- luteolin inhibits PDE (PDE usually converts cAMP to 5’AMP)
- more cAMP = more PKA = more protein phosphorylation + Long term potentiation!
should be able to replicate the graph!
lion’s mane (monograph)
- SCIENTIFIC NAME:
- PART USED:
- MODE OF ADMINISTRATION:
- BIOACTIVE COMPOUND:
- COMPOUND CLASS:
- USES:
- SCIENTIFIC NAME: hericium erinaceus
- PART USED: fruit body
- MODE OF ADMINISTRATION: whole plant extract
- BIOACTIVE COMPOUND: hericenon/erinacine
- COMPOUND CLASS: cyanthin diterpenoids
- USES: cognitive enhancer
mechanism of action of lion’s mane
- nericenones and erinacines isolated from cultured mycelia of lion’s mane ENHANCES NERVE GROWTH FACTOR (NGF) in vitro
- NGF is a protein that is essential tin the maintenance, survival and regeneration of neurons
*Lion’s mane could regenerate damaged nerve cells –> form new pathways, neuroplasticity
summary slide on natural nootropics
- name common name, compound, mechanism (1 to 3)
GINGKO BILOBA
PANAX GINSENG
BACOPA MONNIERI
HUPERZIA SERRATA
PLECTRANTHUS BARBATUS
HERICIUM ERINACEUS
GINGKO BILOBA
- Gingko, ginkgolides
1. increase uptake and release of ACh
2. increases uptake of 5HT
3. reverses age related decline in a adrenergic receptors
PANAX GINSENG
- ginseng, ginsengosides
1. increase uptake and release of ACh
2. increases nerve growth factor
BACOPA MONNIERI
- Bacopa, bacosides
- releases NO and promotes vasodilation and increased cerebral blood flow
HUPERZIA SERRATA
- Firmoss, Huperzine A
- Actylcholinesterase inhibitor –> increases ACh
PLECTRANTHUS BARBATUS
- Indian coleus, Foskolin (with the help of luteolin!)
1. increases cAMP levels
2. inhibits acetylcholinesterase
HERICIUM ERINACEUS
- lion’s mane, hericenone, erinacine
1. increases nerve growth factor
DEFINITIONS:
- used to enhance memory or other cognitive function
- relating to the growth of nervous tissue
- also known as wakefulness-promoting agents and wakefulness-promoting drugs. are a class of drugs that promote wakefulness and alertness
- nootropic
- Neurotrophic
- eugeroics
Definitions
- nootropic
- Neurotrophic
- eugeroics
- used to enhance memory or other cognitive function
- relating to the growth of nervous tissue
- also known as wakefulness-promoting agents and wakefulness-promoting drugs. are a class of drugs that promote wakefulness and alertness
