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40 Cards in this Set

  • Front
  • Back
Define the criteria for accepting a substance as a (classical) neurotransmitter
1. localization- localized to the presynaptic element & present w/i presynaptic neuron
2. release- released from presynaptic element upon activation of terminal & depolarization of neuron
3. identity- action on target cells is same as effects on presynaptic neuron by transmitter
Describe the distribution of Glutamate
-most prevalent fast excitatory transmitter in CNS
-used by about 1/2 neurons in brain
Describe the synthesis of Glutamate
Its derived from a-ketoglutarate by GABA transaminase, which is also a precursor for the inhibitory neurotransmitter g-aminobutyric acid (GABA).
-derived from glutamine & converted to glutamate & ammonia by mitochondria
Describe the inactivation mechanisms of Glutamate
-reuptake directly by presynaptic terminal transporters
-indirectly through astrocyte transporters
-converted back to glutamine & transported back to terminal
Describe the functions of Glutamate
-role in learning & memory
-Ca2+ ion entry through NMDA activated channels in ischemic tissue
^can exacerbate injury & increase cell death
-associated w/ excitotoxicity
Describe the distribution of GABA
-primary inhibitory neurotransmitter in brain
-found in high amnts in substantia nigra stratum, lentiform nuclei, hypothalmus, hippocampus, periaqueductal gray
Describe the synthesis of GABA
-GABA is synthesized from glutamate by glutamic acid decarboxylase.

-It is also converted from glutamine-->glutamate
--> GABA
Describe the inactivation mechanisms of GABA
The recycling mechanisms are therefore similar to glutamate, except for the additional step of conversion back to glutamate from glutamine in both neurons and astrocytes.
Describe the functions of GABA
-transmitter for Purkinje cells of cerebellum
-linked to chloride ion channels, usually hyperpolarizes, occasionaly excitatory
-associated w/ drug effects: anesthetics, caffeine, alcohol
What AA neurotransmitter is implicated in epilepsy, bipolar disorder, schizophrenia, & anxiety disorders
GABA
Describe the distribution of Acetylcholine
-in CNS & PNS
-CNS: motor & preganglionic autonomic neurons use it.
-excitatory & inhibitory properties
-ionotropic & metabotropic receptors.
-broadly projecting ACh systems that are part of conscious arousal.
Describe the synthesis of Acetylcholine
synthesized from choline and acetyl Coenzyme A by choline acetylase
Describe the inactivation mechanisms of Acetylcholine
After release, acetylcholine is broken down by acetylcholinesterase to choline and acetic acid. Both components are transported into the terminal and recycled
Describe the functions of Acetylcholine
involved in diverse functions from memory to muscle contraction
What does the loss of acetylcholine containing neurons in the nucleus basalis (brain) lead to?
Alzheimer's disease
Describe the distribution of Dopamine & Norepinephrine
-throughout nervous system
-both excitatory & inhibitory
Describe the synthesis of Dopamine & norepinephreine
tyrosine-->dopamine-->norepinephrine
Describe the inactivation mechanisms of Dopamine & norepinephrine
-inactivation and recycling by catechol-O-methyl transferase (COMT) on the post synaptic membrane and monoamine oxidase (MAO) in the presynaptic terminal cytoplasm.
Describe the functions of Dopamine & norepinephrine
-modulate consciousness, sleep, & motor activity in brain
-motor functions, rewarding behaviors/addiction
Why are most of the enzymes involved in this pathway significant?

tyrosine-->dopamine-->norepinephrine
-->epinephrine
tyrosine--(amino acid hydrolase)--> DOPA
DOPA--(dopa decarboxylase)--> dopamine
dopamine--(dopamine b-hydroxylase)--> NE
NE--(phentolamine N- methytransferase)--> EPI

*are modifiable by pharmocologic or toxic agents.
What neurotransmitter is involved in Parkinson disease?
dopamine
Many antipsychotic drugs have their primary actions on ____________ receptors
catecholamine
Describe the distribution of serotonin
excitatory & inhibitory
Describe the synthesis of serotonin
synthesized from tryptophan by subsequent actions of tryptophan hydroxlase, and 5-hydroxytryptophan decarboxylase.
Describe the inactivation mechanisms of serotonin
-broken down by monoamine oxidase and or transported back into the presynaptic terminal.
Antidepressents work through inhibiting the reuptake of ____________ or through inhibiting monamine oxidases (MAOI)
serotonin (SSRIs)
Describe the functions of serotonin
- sleep/wake cycles, emotional behavioral states & prominent component of platelets (vasoconstriction).
-associated with the action of may hallucinogens (LSD, mescaline, ecstasy).
Describe the distribution of histamine
-excitatory
-component of mast cells and basophils (vasodilation) and involved in gastric secretion.
Describe the synthesis of histamine
synthesized from histidine by histidine decarboxylase.
Describe the inactivation mechanisms of histamine
-broken down by histamine N methyltransferase and diamine oxidase.
Antihistamines are generally receptor blockers.
Describe the functions of histamine
Centrally, it is associated with sleep/wake cycles an the maintenance of a conscious state
Describe the properties of neuropeptides in the CNS
-located in the CNS and PNS
*substance P, b-endorphin, enkephalins and vasoactive intestinal polypeptide (VIP).
-all metabotropic and G-protein coupled
-Release is often non-synaptic or as a co-transmitter
-Centrally, neuropeptides are prominent in the hypothalamus, also found in the brainstem and basal ganglia.
*oxytocin & vasopressin
Describe the functions of neuropeptides in the CNS
-many have primary functions related to enteric nervous system
-major roles in autonomic function (oxytocin, vasopressin)
-pain (substance P)
-pain/pleasure (b-endorphin & enkephalon)
-circadian rhythm (VIP)
Describe the properties of purines in the CNS
-ATP & Adenosine are synthesized & recycled through the same pathways for energy metabolism in mitochondria.
-ATP is often a co-transmitter packaged with other neurotransmitters (noradrenaline & neuropeptide Y)
Describe the functions of purines in the CNS
-released from sympathetic perivascular nerve fibers and act on vascular smooth muscle, constricting or relaxing depending on receptor
-act on purine autoreceptors to effectively regulate their own release and that of any cotransmitter
Describe the properties of nitric oxide as a transcellular messenger in the CNS
-gasotransmitters
-interact as cotransmitter
-sympathetic enzymes present in neurons of brain

*Nitric oxide responses are mediated through a cGMP mechanism in both neurons and neuroglia
Describe the functions of nitric oxide as a transcellular messenger in the CNS
-mediate numerous effects in body tissue particularly related to vascular smooth muscle.
- a neuromodulator at the synaptic level in both a feed forward and feedback (retrograde) regulation of synaptic activity.
Describe the properties of endocannabinoids as a transcellular messenger in the CNS
-synthesized from arachidonic acid derivatives
-degraded by fatty acid amide hydrolase and monacylglycerol lipase.
-act through two primary receptors CB1 (nervous system, and organs) and CB2 (immune system
Describe the functions of endocannabinoids as transcellular messenger in the CNS
-In the nervous system, modulate synaptic transmission as a retrograde feedback effect.
-effect physiological processes associated w/ appetite, pain sensation, mood and memory
What is retrograde transmission?
-proccess of feedback from postsynaptic cell
-postsynaptic cell responds to synaptic activation by releasing a second chemical messenger capable of affecting the presynaptic nerve terminal or neuron.

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