Neurotransmitters Flashcards
How is acetylcholine formed?
Acetyl CoA + choline = CoA + ACh
Acetylcholine is recycled by the enzyme ____. What does it do?
acetylcholinesterase.
AChE breaks apart ACh into acetate and choline. Choline is taken back by presynaptic cell and then re-synthesized into ACh in presynaptic cell
Nicotinic receptor is an ___ ___ receptor that is stimulated by ___ and blocked by ____
Nicotinic receptor is an IONOTROPIC ACECTYLCHOLINE receptor that is stimulated by NICOTINE and blocked by CURARE
Muscarinic receptor is a ____ ____ receptor that is stimulated by ___ and inhibited by ____
Muscarinic receptor is a METABOTROPIC ACETYLCHOLINE receptor that is stimulated by MUSCARINE and inhibited by ATROPINE
botulinum toxin
ACh ANTAGONIST, prevents release by terminal buttons
black widow spider venom
triggers release of ACh
hemimcholinium
inhibits uptake of CHOLINE
neostigmine
inhibits the activity of AChE
atropine
drug that blocks MUSCARINIC ACh receptors
Curare
drug that blocks NICOTINIC ACh receptors
2 types of monoamines and their examples
- indolamines: serotonin
2. catecholamines: dopamine, NE, E
What is the precursor of catecholamines?
L-Dopa
Why use L-Dopa for Parkinson’s disease treatment?
because of its effect as a DOPAMINE AGONIST
nigrostriatal system
a dopaminergic system of neurons originating in the SUBSTANTA NIGRA and terminating in the NEOSTRIATUM (caudate nucleus and putanem)
Mesolimbic system
system of dopaminergic neurons originating in the VENTRAL TEGMENTAL AREA and terminating in the NUCLEUS ACCUMBENS, AMYGDALA, and HIPPOCAMPUSA
Mesocortical system
system of dopaminergic neurons originating in the VENTRAL TEGMENTAL AREA and terminating in the PREFRONTAL CORTEX
symptoms of Parkinson’s disease and causes
symptoms: tremors, rigidity of the limbs, poor balance, difficulty initiating movements
causes: DEGENERATION OF NIGROSTRIATAL SYSTEM due to:
- unknown etiology
- viral encephalitis
- brainstem trauma/vascular damage
AMPT
DOPAMINERGIC drug that blocks the activity of tyrosine hydroxylase and thus interferes with the synthesis of catecholamines
tyrosine becomes L-Dopa via:
tyrosine hydroxylase
L-Dopa is decarboxylated to form ____ via ____
L-Dapa is decarboxylated to form DOPAMINE via DOPA DECARBOXYLASE
reserpine
dopaminergic drug that interferes with the storage of monoamines in synaptic vesicles
apomorphine
dopaminergic drug that blocks dopamine autoreceptors at low doses; at higher doses it blocks postsynaptic receptors as well
where are nicotinic receptors usually found?
typically in striated muscle at motor end plate
monoamine oxidase (MAO)
dopaminergic drug
- class of enzyme that destroys monoamines: dopamine, NE, and serotonin
- a drug which inhibits MAO can be used to treat depression, as it would inhibit the breakdown of monoamines
deprenyl (he didn’t talk about in class, but it’s on slides)
dopaminergic drug that blocks the activity of MAO-B; acts as a DOPAMINE AGONIST
chlorpromazine (he didn’t talk about in class, but it’s on slides)
dopaminergic drug that reduces the symptoms of schizophrenia by blocking dopamine D2 receptors
methylphenidate
drug that inhibits the reuptake of dopamine.
Therefore, it is a dopamine agonist, as it causes it to linger in synapse and energize behaviour
Why are receptors needed on the presynaptic membrane?
for negative feedback loop. To inhibit further secretion of dopamine. Activation of these receptors inhibits further release of NTs.
Epinephrine is secreted by the ___ ___
adrenal medulla
Norepinephrine is synthesized in ____
neurons
locus coeruleus
dark-coloured group of noradrenergic cell bodies located in the PONS near the ROSTRAL end of the floor of the FOURTH VENTRICLE
axonal varicosity
enlarged region along the length of an axon that contains synaptic vesicles and releases NTs or neuromodulators
idazoxan
drug that blocks presynaptic noradrenergic alpha-2 receptors and hence acts as an agonist, fascilitating the synthesis and release of NE
Which NT can cross the blood-brain barrier? NE or E?
NE. Epinephrine CANNOT cross BBB
Serotonin is also known as ____
5-hydroxytryptamine (5-HT)
PCPA
drug that inhibits the activity of TRYPTOPHAN HYDROLASE and thus interferes with synthesis of 5-HT
Fluoxetine (Prozac)
drug that inhibits the reuptake of 5-HT (serotonin)
fenfluramine
drug that stimulates the release of 5-HT
mechanism of tryptophan to serotonin
tryptophan becomes 5-HTP via tryptophan hydroxylase.
5-HTP becomes 5-HT via 5-HTP decarboxylase
what brain regions secrete serotonin
substantia nigra and Raphe nucleus
how do humans acquire tryptophan?
through diet only. Cannot be synthesized in body
LSD stimulates ___ receptors
5HT2A. hallucinogenic effect.
MDMA (ecstasy)
drug that serves as a NE and serotonin AGONIST.
Has an excitatory hallucinogenic effect
Most important NT in the CNS:
glutamate
what does AMPA receptor do?
Opens Na+ channel when bound to glutamate. Stimulated by AMPA
NMDA receptor is a specialized ____ receptor that controls a ___ channel that is normally blocked by ___ ____
NMDA receptor is a specialized IONOTROPIC receptor that controls a Ca2+ channel that is normally blocked by Mg+ IONS.
___ is an indirect agonist of the NMDA receptor
GLYCINE.
Presence of glycine sensitizes channel
___ is an indirect antagonist of NMDA receptor
ZINC
Calcium channel of NMDA receptor only opens when it is not blocked by ___
Mg2+ ions
When is Mg2+ removed from Ca2+ channel of NMDA receptor?
when the membrane is DEPOLARIZED
Is the NMDA receptor voltage- or ligand-dependent? Explain
BOTH.
ligand: glutamate
voltage: membrane must depolarize for magnesium ion to be removed from from receptor’s central pore
What occurs when Mg2+ is removed from NMDA central pore?
NMDA channel can open in response to glutamate, letting both Ca2+ and Na+ influx
an increase in postsynaptic Ca2+ triggers an intracellular signaling cascade that ultimately leads to the insertion of additional ______ ____ into postsynaptic membrane, which strengthens the synapse
AMPA receptors
AMPA receptors open in response to
glutamate
How does the opening of postsynaptic NMDA receptors cause changes in synapse strength?
When postsynaptic Ca2+ levels rise, CALMODULIN binds calcium, forming a calcium/calmodium complex which activates CaMKII. CaMKII promotesthe insertion of additional AMPA receptors, which increases rate of ion flow
AP5
drug that blocks the glutamate binding site on NMDA receptors
PCP
drug that binds with the PCP binding site of the NMDA receptor. Serves as an indirect antagonist
Most important inhibitory NT in the brain?
GABA
Benzodiazepine
category of anxiolytic drugs; indirect AGONIST for GABAA receptor. Causes Cl- channel to open for longer
Anxiolytic effects
anxiety-reducing effect
why is alcohol + anxiolytic drugs a bad idea?
because GABA receptors have alcohol and barbtuate sites.
Too profund of a neurological effect
Allyglycine
drug that inhibits the activity of GAD and thus BLOCKS THE SYNTHESIS OF GABA
Muscimol
direct agonist for the GABA binding site on the GABAA receptor
Bicuculline
direct antagonist for the GABA binding site on the GABAA receptor
Glycine
glycine is an important inhibitory NT in the LOWER BRAIN STEM and SPINAL CORD
Strychnine
a direct antagonist for the glycine receptor
endorphins are a class of ____
peptides
endogenous opioid
- class of peptide secreted by the brain that acts as OPIATES
- REDUCE PAIN
What does the fact that the body responds to opioids plants extract suggest about the human body?
that humans produce chemicals similar to these
enkephalin is an ___ ___
endogenous opioid
naloxone is a drug that blocks ___ ___
opiate receptors
what is one of the primary sites for the reward effects of opiate drugs in the brain?
mu receptor
endocannabinoid
- a lipid
- endogenous ligand for the cannabinoid receptors, which also binds with THC (active ingredient of marijuana)
The active ingredient in marijuana
THC
THC activates ___ receptors in the brain
CB1
anandimide
important cannabinoid
FAAH
- fatty acid amide hydrolase
- enzyme that destroys anandamide after it is brought back into the cell by anandamide transporters
rimonabant is a drug that bocks ___ receptors
CB1
MAFP
drug that inhibits FAAH, preventing the breakdown of anandamide
Are CB1 and CB2 refceceptors ionotropic or metabotropic?
metabotropic
CB1 receptos are found in the ___ and CB2 receptors in the ___
CB1 receptos are found in the CNS and CB2 receptors in the PNS
Positive effects of cannabinoids
beneficial effects in glaucoma, asthma, and nausea in cancer tratment
neg effects of cannabinoids
impaired visuomotor coordination, attention and memory, evidence of IQ depression in prolonged use
adenosine
- nucleoside
- combination of ribose and adenine
- serves as a neuromodulator in the brain
caffeine
drug that blocks adenosine receptors
nitric oxide (NO)
gas produced by cells in the nervous system
-used as a means to communicate between cells
nitric oxide synthase
-enzyme responsible for the production of nitric oxide
nitric oxide synthase is inactivated by ___
L-NAME
Cholinergic projections in rat brain
- from the DORSOLATERAL PONS to substantia nigra, thalamus, deep cerebellar nuclei, tectum, pontine reticular formation, locus coeruleu, vestibular nuclei, Raphe nuclei, medullary reticular formation
- from the BASAL FOREBRAIN to the neocortex
- from the CAUDATE NUCLEUS, PUTAMEN, AND NUCLEUS ACCUMBENS
- from the MEDIAL SEPTUM to the olfactory bulb, the neocortex, hippocampus, and lateral hypothalamus
Dopaminergic projections in rat brain
- from SUBSTANTIA NIGRA to globus pallidus and caudate nucleus and putamen
- from VENTRAL TEGMENTAL AREA to lateral habenula, thalamus, amygdala, nucleus accumbens, hippocampus, lateral septum, anterior olfactory nucleus, olfactory tubercle, and neocortex
Noradrenergic pathways in a rat brain
- from LOCUS COERULEUS to cerebellum, tectum, spinal cord, hypothalamus, preoptic area, basal ganglia, hippocampus, amygdala, septum, olfactory bulb, and neocortex
Serotonergic projections in rat brain
- from RAPHE NUCLEI to substantia nigra, cerebellum, spinal cord, spinal trigeminal nucleus, tectum, habenula, thalamus, basal ganglia, hypothalamus, amygdala, septum, hippocampus, olfactory tubercle, olfactory bulb, neocortex.