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NEUROTRANSMITTERS
&
THEIR MODE OF ACTION

https://www.youtube.com/watch?v=LOHKVp8hn7o&list=PLybg94GvOJ9EQp4lGx2k
xTvA4Y7HUo5VY&index=4
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INTRODUCTION
 Neurotransmitters are chemical
messengers/molecules that transmit signals from a
neuron to a target cell across a synapse.

 Target cell may be a neuron or some other kind of cell

like a muscle or gland cell.

 Necessary for rapid communication in synapse.

 Neurotransmitters are packaged into synaptic vesicles -

presynaptic side of a synapse.
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Illustration of the major elements in chemical synaptic transmission.

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A schematic representation of a chemical synapse
Axon

Pre synaptic Vesicles (containing

neurotransmitters)
knob Synaptic cleft
Receptors

Post synaptic
Receiving
knob neuron
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PROPERTIES OF
NEUROTRANSMITTERS

1) Synthesized in the presynaptic neuron

2) Localized to vesicles in the presynaptic neuron

3) Released from the presynaptic neuron under physiological

condition

4) Rapidly removed from the synaptic cleft by uptake or degradation

5) Presence of receptor on the post-synaptic neuron.

6) Binding to the receptor elicits a biological response

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ACETYLCHOLINE (ACh)
 Acetylcholine was the first neurotransmitter to be discovered.
 Isolated in 1921 by a German biologist named Otto Loewi.

 Uses choline as a precursor - cholinergic neurotransmitter.

 Used by the Autonomic Nervous System, such as smooth

muscles of the heart, as an inhibitory neurotransmitter.

 Responsible for stimulation of muscles, including the muscles of

the gastro-intestinal system.

 Used everywhere in the brain.

 Related to Alzheimer's Disease.
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Mechanism of action/purpose
  In lower amounts, ACh can act like a stimulant by releasing norepinephrine
(NE) and dopamine (DA)

 Memory

 Motivation

 Higher-order thought processes

 Sexual desire and activity

 Sleep
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Symptoms of excess

 Depression (all symptoms)

Nightmares

Mental Fatigue

Anxiety

 Inverse relationship between serotonin and acetylcholine

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Insufficiency

 Alzheimer’s/dementia

 Parkinson’s

 Impaired cognition, attention, and arousal

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Nutritional building blocks

 Foods high in choline

Meats

Dairy

Poultry

Chocolate

Peanut butter

Wheat germ

Brussels sprouts and broccoli

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DOPAMINE
 Is synthesized in three steps from the amino acid
tyrosine.
 Associated with reward mechanisms in brain.

 Generally involved in regulatory motor activity, in

mood, motivation and attention.

 Schizophrenics have too much dopamine.

 Patients with Parkinson's Disease have too little

dopamine.
Dopamine
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Mechanisms of Action
Precursor, L-DOPA is synthesized in brain and kidneys

 Dopamine functions in several parts of the peripheral nervous system

In blood vessels, it inhibits norepinephrine release and acts as a vasodilator

(relaxation).

In the pancreas, it reduces insulin production

In the digestive system, it reduces gastrointestinal motility and protects

intestinal mucosa

In the immune system, it reduces lymphocyte activity.

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Symptoms of excess
Unnecessary movements, repetitive tics

Psychosis

Hypersexuality

Nausea

Most antipsychotic drugs are dopamine antagonists

Dopamine antagonist drugs are also some of the most effective anti-nausea
agents
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Symptoms of insufficiency
Negative symptoms of schizophrenia

Pain

Parkinson’s Disease

Restless legs syndrome

Attention deficit hyperactivity disorder (ADHD)

Neurological symptoms that increase in frequency with age, such as

decreased arm swing and increased rigidity.

Changes in dopamine levels may also cause age-related changes in cognitive

flexibility.
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Age Related Changes

 Dopamine levels decline by around 10% per decade from early adulthood
and have been associated with declines in cognitive and motor performance.

 Dopamine levels are also impacted by availability of estrogen

https://www.ncbi .nlm.nih.gov/pmc /articles/PMC259 6698/
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Nutritional building blocks

 Eating a diet high in magnesium and tyrosine rich foods will ensure you’ve
got the basic building blocks needed for dopamine production.

 Here’s a list of foods known to increase dopamine:

Chicken Almonds Apples Avocado Bananas Beets Chocolate Green leafy

vegetables Green tea Lima beans Oatmeal Sesame & pumpkin seeds Turmeric
Watermelon Wheat germ
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NOREPINEPHRINE (nor adrenaline)

 Synthesized directly from dopamine.
 Direct precursor to epinepherine.

 Synthesized within vesicles.

 Norepinephrine is strongly associated with bringing our

nervous systems into "high alert."

 It increases our heart rate and our blood pressure.

 It is also important for forming memories.

Norepinephrine
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Epinephrine SCIENCES

Epinephrine (also known as adrenaline) is a neurotransmitter in the sense that,

within the brain, it help neurons to communicate with one another. However,
because epinephrine is mainly produced by the adrenal glands and has
functions peripherally (i.e., outside the brain), it can also be considered a
hormone.

As a hormone and neurotransmitter, epinephrine acts on nearly all body

tissues. Its actions vary by tissue type and tissue expression of adrenergic
receptors. For example, high levels of epinephrine cause smooth muscle
relaxation in the airways, but cause contraction of the smooth muscle that
lines most arterioles.
Epinephrine acts by binding to a variety of adrenergic receptors. Epinephrine
is a nonselective agonist of all adrenergic receptors, including the major
subtypes α1, α2, β1, β2, and β3.

Epinephrine’s binding to these receptors triggers a number of metabolic

changes. Binding to α-adrenergic receptors inhibits insulin secretion by the
pancreas, stimulates glycogenolysis (the breakdown of glycogen) in the liver
and muscle, and stimulates glycolysis (the metabolic pathway that converts
glucose into pyruvate) in muscle.

β-Adrenergic receptor binding triggers glucagon secretion in the pancreas,

increased adrenocorticotropic hormone (ACTH) secretion by the pituitary
gland, and increased lipolysis by adipose tissue.

Together, these effects lead to increased blood glucose and fatty acids,
providing substrates for energy production within cells throughout the body.
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GLUTAMATE
 It is an amino acid

 It the most commonly found

excitatory neurotransmitter in the brain.

 It is involved in most aspects of normal brain

function including cognition, memory and learning.

 Glutamate enhances neuroplasticity — the brain’s capacity

to change and grow — to help you learn, remember, and
perform other cognitive functions.
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Excess glutamate
It is associated with:

 Panic attacks / anxiety

 Impulsivity

 OCD

 Depression 

It also declines with age :

 Chang L, Jiang CS, Ernst T (January 2009). "Effects of age and sex on brain
glutamate and other metabolites". Magn Reson Imaging. 27 (1): 142–5.
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Availability declines with age

•Insomnia

•Concentration problems

•Mental exhaustion

•Low energy
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γ-AMINO BUTYRIC ACID (GABA)

 Synthesized directly from glutamate.

 GABA is the most important inhibitory neurotransmitter

 Present in high concentrations in the CNS, preventing

the brain from becoming overexcited.

 If GABA is lacking in certain parts of the brain, epilepsy

results.

GABA
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Mechanism of action/purpose

 Anti-anxiety, Anti-convulsant

 GABA is made from glutamate

 GABA functions as an inhibitory neurotransmitter

 GABA does the opposite and tells the adjoining cells not to “fire”

 Close to 40% of the synapses in the human brain work with GABA and
therefore have GABA receptors.
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Symptoms of excess
  Excess sleepiness

 Shallow breathing

 *Increased blood pressure

 Symptoms of insufficiency

Deficiency
 Anxiety

 Depression

 Difficulty concentrating

 Insomnia

 Seizure disorders
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Nutritional building blocks
  Fermented foods sauerkraut, yogurt

 Almonds & walnuts

 Cherry tomatoes

 Bananas

 Brown rice

 Potatoes

 Oats  Lentils, navy & lima beans

 Vitamin B6, if deficient, may impair the production of GABA as it is a

cofactor nutrient.
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SEROTONIN (5-HT)
 Synthesized in two steps from the amino acid
tryptophan

 Regulates attention and other complex cognitive

functions, such as sleep (dreaming), eating,
mood, pain regulation.

 Too little serotonin has been shown to lead

to depression,anger control etc.
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Mechanism of action/purpose

 Helps regulate Mood

Cardiovascular functioning

Memory

Intestinal motility

Sleep patterns

Appetite

Pain
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Where is it found
 Brain

 Gut/Intestines

Symptoms of excess (Serotonin Syndrome)

 Shivering

 Diarrhea

 Muscle rigidity

 Fever

 Seizures

 Irregular heartbeat
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Insufficiency

 Depression

 Anxiety

 Pain sensitivity

 Appetite disturbance

 Sleep disturbances
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Nutritional building blocks

 Foods rich in tryptophan, an amino acid that converts to serotonin in the
brain.

Whole-wheat

Potatoes

Brown rice

Lentils

Oats

Beans
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ENDORPHINS

Beta-endorphins are neuropeptides involved in pain management, possessing

morphine like effects, and are involved in natural reward circuits such as
feeding, drinking, sex and maternal behavior.

Beta-endorphins are primarily synthesized and stored in the anterior pituitary

gland from their precursor protein proopiomelanocortin (POMC). However,
recent studies suggest cells of the immune system are also capable of beta-
endorphin synthesis.
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Mechanism

In the peripheral nervous system (PNS), beta-endorphins produce analgesia by

binding to opioid at both pre- and post- synaptic nerve terminals, primarily
exerting their effect through presynaptic binding.

When bound, a cascade of interactions results in inhibition of the release of

tachykinins, particularly substance P, a key protein involved in the transmission
of pain.
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• Reduces Depression

• Reduces Stress & Anxiety

• Self esteem

• Pain
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1.Neurotransmitters are
synthesized from precursors

2. Stored in vesicles
3.Neurotransmitter molecules
that leak from their vesicles are
destroyed by enzymes
4.Action potential cause vesicle
to fuse with synapse and release
neurotransmitters
5.Some of it binds with auto
receptor and inhibit subsequent
neurotransmitter release
6. Rest of it bind to post
synaptic receptors.
7.Released neurotransmitters
are deactivated either by re
uptake or enzyme degradation.
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Steps in neurotransmitter processing are:

Synthesis: Neurotransmitters are synthesized by the

Presynaptic vesicles.

Storage: They are packaged inside synaptic vesicles.

Release
:They are released from presynaptic terminal by exocytosis when
calcium enters axon terminal during an action potential
Diffuse across the synaptic cleft to the postsynaptic
membrane.
Binding: They bind to receptor proteins.

Inactivation: The neurotransmitter is degraded either by being broken

down enzymatically, or reused by active reuptake.
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• When nerve impulse reaches pre synaptic knob Ca

channels open.
• Increased Ca ions fusion of vesicle
Release
presynaptic
to membrane and release of ACh into cleft.

• ACh bind to receptors in post synaptic membrane.

• Ion channels open inflow of Na and K ions
• Depolarisation and formation of action potential.
Binding • Propogation of action potential & contraction of
fibres.

• ACh is hydrolysed by acetyl cholinesterase.

• Choline taken back to presynaptic domain for
Deactivation resynthesis of Ach.
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ALCOHOL & NEUROTRANSMITTERS
SCIENCES

 It binds directly to receptors for ACh,

serotonin, GABA and glutamate.
 It enhances the effects of the GABA,
which is an inhibitory
neurotransmitter.
◦ Enhancing an inhibitor make things
sluggish.
◦ The neuron activity is diminished-
sedative effects of alcohol.
 Alcohol inhibits glutamate receptor
function.
◦ This causes discoordination, slurred speech, staggering,
memory disruption, and blackout.
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NICOTINE & NEUROTRANSMITTERS

 Nicotine imitates the action of

ACh & binds to ACh receptor.
 Like acetylcholine, nicotine leads to a burst
of receptor activity.

 Nicotine activates cholinergic neurons in many

different regions throughout your brain
simultaneously.

 This stimulation leads to:

◦ Increased release of glutamate.
◦ Stimulation of cholinergic neurons promotes the
release of dopamine. The production of dopamine
causes feelings of reward and pleasure.
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RECENT DEVELOPMENTS
 A team of scientists from University of Barcelona
in 2011, has discovered that D-aspartic acid (D-
Asp) is a novel neurotransmitter that could
potentially be used in the fight against neurological
diseases such as Parkinson's and schizophrenia.

 According to a new study led by researchers at

the Ohio State University Comprehensive
Cancer Center in 2011, doses of a
neurotransmitter dopamine might offer a way to
boost the effectiveness of anticancer drugs and
radiation therapy.
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CONCLUSION
 The ability of nervous system to orchestrate
complex behaviors, learn and remember depends on
communication between vast no: of neurons.

 Mediated by neurotransmitters.

 They play an important role in control

and coordination of body.

 Many neurological diseases and mental disorders are

due to improper functioning of neurotransmitters.
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REFERENCES
SCIENCES

 Knut Schmidt Nielsen, Animal Physiology –

Adaptation and environment, 4th edition, Cambridge
University Press, U.K

 Richard.W.Hill (1976) Animal Physiology, 2nd edition,

Harper Collin’s Publishers, New York.

 http://www.sciencedaily.com/releases/2011/12/111205
165907.htm

 http://www.columbia.edu/cu/psychology/courses/1010
/mangels/neuro/transmission/transmission.html

 http://www.chemistryexplained.com/NeNu/Neurotransmitters
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