neurotransmitter and receptors Flashcards

1
Q

what are the 5 criteria of neurotransmitters

A
  1. in terminal
  2. Ca2+ dependent release
  3. subject to inactivation
  4. synaptic mimicry
  5. receptors exist
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2
Q

how are amino acid NT the workhorses of the CNS

A
  • predominant type of NT
  • 90% of synapases involve 4 AA - glutamate, aspartate, GABA, or glycine
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3
Q

whats the overall role of AA NT

A

can be excitatory (Glu, Asp) or inhibitory (GABA or Gly)

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4
Q

AA NT receptors

A
  • most work through ionotropic (ion channel) receptors
  • some use metabotropic receptors
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5
Q

AA NT inactivation

A

rapid uptake

  • back into vesicle
  • in glial cell - can stay there or go back to neuron
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6
Q

what is glutamate

A
  • major excitatory NT
  • widely distributed through the CNS
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7
Q

glutamate receptors

A
  • ~13 types of receptors
  • metabotropic - at least 8 varieties
  • ionotropic - 3 major classes
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8
Q

what are the 3 major classes or ionotropic glutamate receptors

A
  • NMDA
  • AMPA
  • Kainate
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9
Q

which ionotropic glutamate receptor is of the greatest interest and why

A

NMDA b/c it is heavily involved in learning and memory

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10
Q

What is GABA

A
  • major inhibitory NT in CNS
  • widely distributed through the CNS (important in inhibitory control of interneurons)
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11
Q

what is the name of the enzyme used to synthesize GABA

A

glutamic acid decarboxylase (GAD)

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12
Q

what are the two families of GABA receptors

A
  • GABA(A) receptors
  • GABA(B) receptors
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13
Q

GABA(A) receptors

A

allow Cl- ions into neuron resulting in membrane hyperpolarization

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14
Q

GABA(B) receptors

A
  • G-protein coupled
  • connected to K+ channels to cause membrane hyperpolarization
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15
Q

AA NT location importance

A

drugs acting on these transmitters/their receptors can exert GLOBAL effects on overall CNS function

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16
Q

what is increasing the overall INHIBITION of the CNS useful for

A

sedation, anethesia, anxiolytics, seizure control

  • ketamine
  • benzodiazepines and barbiturates (enhance GABA(A) receptor)
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17
Q

what is the enzyme used to synthesize acetylecholine

A

choline acetyletransferase

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18
Q

how is acetylecholine inactivated

A

acetylcholinesterase (breaks down ACh)

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19
Q

what are the two types of ACh receptors

A
  • nicotinic Ach receptor (ionotropic)
  • muscaromoc ACh receptor (metabotropic)
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20
Q

location of cholinergic neurons

A

specific circuits throughout brain

21
Q

what are some CNS functions of ACh

A
  • behavioral arousal
  • attention
  • REM sleep
  • memory
  • learning aggression
  • grand mal seizures
  • sensory perception
  • energy conservation
  • mood
  • motor coordination
22
Q

Ach is a prominent NT of the:

specific nervous system

A

autonomic nervous system

23
Q

what is the action of acetylecholinesterase inhibitors

A

excessive buildup of ACh in the synapse is dangerous!

24
Q

what are acetylecholinesterase inhibitors - irreversible inhibitors (organophosphates)

A

many products used in industry and agriculture (and war)

  • insecticides
  • poisonous gases

poisoning is very common

  • physiologic excess of AChE exist in the body
  • profound effects when 80-90% of enzyme is inactivated
  • exposure is cumulative
  • many agents penetrate skin
25
Q

what is myasthenia gravis

A

an autoimmune disease with decreasing numbers of nicotinic receptors at neuromuscular junction

26
Q

what are the 3 types of catecholamines

A
  • dopamine
  • norepinephrine
  • epinephrine
27
Q

what is a type of indoleamines

A

serotonin and melatonin

28
Q

what is the catecholamine precursor

A

tyrosine

29
Q

what is the rate limiting step and nonsecific decarboxylase of catecholamine synthesis

A

tyrosine 5-hydroxylase; aromatic amino acid decarboxylase

30
Q

what are the enzymes needed to make norepinephrine and epinephrine

A

dopamine-B-hydroxylase; phenylethanolamine-N-methyl transferase

31
Q

what is the rate limiting step in serotonin synthesis

A

tryptophan

32
Q

what are the rate-limiting steps and nonspecific decarboxylase for serotonin synthesis

A

tryptophan 5-hydroxylase; aromatic amino acid decarboxylase

33
Q

what are the rate-limiting steps in breakdown of catecholamines and serotonin and what is the same nonspecific enzyme? what is the additional enzyme needed for catecholamine breakdown

A

monoamine oxidase; aldehyde dehydrogenase; catechol-O-methyl transferase

34
Q

what are the two MAO subtypes

A

MAO-A and MAO-B

35
Q

preferences of MAO

A
  • both subtypes capable of metabolizing all catecholamines and serotonin
  • serotonin, norepinephrine, and epinephrine broken down by MAO-A
  • dopamine broken down equally by both MAO-A and MAO-B
36
Q

MAO is a ____ enzyme and is ____ the mechanism for removal of monoamines from the synapse

A

mitochondrial, NOT

37
Q

catecholamine and indoleamine inactivation

A

rapid reuptake via specific transporters

38
Q

dopamine: location and function

A
  • hypothalamic regulation of hormones
  • substantia nigra to basal ganglia play major role in movement
  • midbrain projections to cortex and limbic system involved in schizophrenia, central “reward” pathway, working memory
39
Q

what is parkinsons disease and how is it characterized

A
  • progressive neurodegenerative disorder
  • fatigue, lethargy, changes inmental alertness, tremors, bent posture, difficulty initiating voluntary movement
40
Q

what does a marked loss of dopaminergic neurons in substantia nigra do

A

signs of parkinson’s disease

41
Q

norepinephrine: location and function

A
  • role in attention
  • involvement with control of feeding
  • connection to mood
  • cell bodies of NE neurons reside in pons and medulla (locus coeruleus LC, lateral tegmental area LTA, dorsal medullary DM)
42
Q

serotonin: location and function

A
  • distribution in the body
  • 90% present in the enterochromaffin cells of the GI tract
43
Q

serotonin: location and function - CNS

A
  • Raphne nuclei: all CNS serotonin is in the raphe and projects widely throughout
  • fire in a highly regulated, pacemaker-like manner
44
Q

what does the neuroanatomy and firing pattern of serotonin imply

A

broad homeostatic functions

45
Q

what is the main function of serotonin

A

mood

46
Q

what has low serotonin been associated with

A
  • depression
  • panic
  • anxiety
  • obsessive-compulsive behaviors
47
Q

what is a drug used to tx low serotonin

A

Prozac - selective serotonin reuptake inhibitor (SSRI)

48
Q

what do SSRI do

A

inhibiting SERT prolongs action of serotonin (5-HT) in synapse