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135 Cards in this Set
- Front
- Back
___ is required after neurotransmitter release to keep the axon terminal a constant size
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membrane endocytosis
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4 drugs that alter synaptic transmission at the presynaptic terminal
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vesamicol
bafilomycin omega-conotoxin hemicholinium |
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6 families of neurotransmitters
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biogenic amines
ACh purinergic amino acids peptides unconventional |
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3 kinds of biogenic amine neurotrans
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catecholamines
HA 5-HT |
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3 catecholamines
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E
NE DA |
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4 AA neurotrans
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Glu
Asp Gly GABA |
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2 unconventional neuro trans
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NO
CO |
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metabotropic Rs work via
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G proteins
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ionotropic Rs are ___s or ___s of proteins with ___ TM domains. the ___ domains line the pore, whose ion specificity is determined by ___
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tetramers
pentamers 4 TM2 charged AAs facing the pore |
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the ___th intracellular loop of a metabotropic R has ___ and is important for ___.
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3rd
variable size G-protein coupling |
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NMDA, AMPA and kainate are ionotropic/metabotropic Rs for ___
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ionotropic
Glu |
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Gly only has ___ Rs. ____ AChRs are ionotropic, ___ AChRs are metabotropic.
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ionotropic
nicotinic muscarinic |
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serotonin Rs are all ___ except for one kind of ___. catecholamine Rs are all ___.
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metabotropic
5-HT3R metabotropic |
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___ is the most important excitatory neurotrans in brain. another excitatory neurotrans is __.
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Glu
Asp |
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2 inhibitory neurotrans
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GABA
Gly |
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Glu is converted to GABA by ___
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glutamic acid decarboxylase (GAD)
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alpha-ketoglutarate and GABA are converted to ___ (2) by ___
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Glu
succinic semialdehyde GABA transaminase |
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Gln is converted to Glu by ___
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glutaminase
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AMPA and kainate Rs are important for ___ transmission and are/aren't highly Ca2+-permeable
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fast
aren't |
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NMDARs are important for ___ and are/aren't highly Ca2+-permeable
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LTP
are |
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metabotropic Glu Rs are coupled to ___ (2)
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Gq
Gi |
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in addition to Glu, ___ can also activate NMDA channel. ___ (2) are co-agonists.
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Asp
Gly D-Ser |
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because of their high ___ permeability, NMDA channels can cause ___
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Ca2+
excitotoxicity |
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____ blocks the NMDAR ion channel at ___ voltages. ___ (2) block it generally. ___ antagonizes the Glu-binding site.
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Mg2+
hyperpolarized PCP MK-801 AP-5 |
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normal Glu transmission triggers ___ flux through AMPARs. when ___ depolarization of postsynaptic cell happens, ___ inhibition of NMDAR is lost. this causes ___, which drives ___ to provide ___ feedback. this process is called ___.
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Na+
sustained Mg2+ Ca2+ influx PKC NOS positive LTP |
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NMDARs require ___ for efficient channel opening.
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co-agonists
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2 NMDAR co-agonists. ___ is stronger.
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d-Ser
Gly d-Ser |
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d-Ser is made from ___ by ___.
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Ser
Ser racemase |
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___ may be effective for treating schizophrenia
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d-Ser
|
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___ is an anesthetic which binds to the same site as PCP. it can cause increased ___ (2). it causes broncho___.
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ketamine
blood pressure intracranial pressure dilation |
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memantine is a ___ (2) inhibitor of NMDAR. it is used to prevent ___ in Alzheimer's.
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low-affinity
non-competitive excitotoxicity |
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___ is the critical biosynthetic enzyme for making GABA.
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GAD
|
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____ is the main postsynaptic GABA R. GABA release is regulated by ___.
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GABA_A
GABA_B |
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GABA neurons are prominent in ___
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cortex
|
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GABA_A receptors are ionotropic/metabotropic
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ionotropic
|
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4 drugs which interact with GABA_A
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barbiturates
benzodiazepines ethanol (withdrawal) neuroactive steroids |
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2 toxins which interact with GABA_A
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picrotoxin
bicuculin |
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GABA_B is ionotropic/metabotropic
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metabotropic
|
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GABA_B is coupled to ___
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G_i
|
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___ is a muscle relaxant which agonizes GABA_B
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baclofen
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benzodiazepines (BDZ) work by agonizing/antagonizing GABA_A. an example is ___.
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antagonizing
flumazenil |
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___ is a GABA_A agonist isolated from the ___ mushroom. it can cause ___
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muscimol
amanita hallucination |
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___ is a GABA_B antagonist
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saclofen
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barbitutrates act by increasing ___ of GABAR. BDZs act by increasing ___.
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channel opening time
channel opening frequency |
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BDZ increase/decrease GABA binding
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increase
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BDZ can be used as ___
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anticonvulsant
|
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___ is a BDZ with a short t1/2
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midazolam
|
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BDZs decrease ___ (2).
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BP
respiratory drive |
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___ is a BDZ antagonist. it is sometimes used to prevent ___.
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flumazenil
alcohol withdrawal |
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barbiturates cause more/less sedation than BDZ
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more
|
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in contrast to BDZs, barbiturates cause ___.
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general anesthesia
|
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2 barbiturates with anticonvulsant properties
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phenobarbital
mephobarbital |
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___ is a truth-serum barbiturate
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thiopental
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barbiturates are more/less addictive than BDZs
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more
|
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bicuculine and flumazenil increase/reduce ethanol consumption in rodents
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reduce
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2 antiepileptic drugs which inhibit GABA-T
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valproate
vigabatrin |
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___ is an antiepileptic drug which inhibits GABA reuptake
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tiagabine
|
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4 drugs for simple and complex partial seizures
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lamotrigine
oxcarbazepine gabapentin topiramate |
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2 drugs which work for absence, myoclonic, atonic seizures
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lamotrigine
valproate |
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___ is the main inhibitory neurotrans in brainstem and SC
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Gly
|
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GlyRs are ionotropic/metabotropic and trigger ___ current
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ionotropic
Cl- |
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GlyRs are blocked by ___.
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strychnine
|
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GlyRs are agonized by ___
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taurine
beta-Ala |
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Y is converted to ___ by ___.
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DOPA
Y hydroxylase |
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DOPA is converted to ___ by ___.
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DA
DOPA decarboxylase (AAADC) |
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DA is imported to vesicles by ___.
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VMAT (vesicular monoamine transporter)
|
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DA is converted to ___ by ___.
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NE
DBH (DA beta hydroxylase) |
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rate-limiting step of catecholamine synthesis is ___
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Y hydroxylase
|
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Y hydroxylase activity is increased by ___
Y hydroxylase activity is decreased by ___ (2) |
phosphorylation
metyrosine end--product inhibition |
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in brain NE is produced in ___
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locus ceruleus
pons medulla |
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NEergic neurons in locus ceruleus project to ___
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whole brain
|
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NEergic neurons in pons/medulla project to ___ (2)
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HTh
spinal cord |
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in brain E is produced in ___
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medulla
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Eergic neurons in medulla project to ___
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spinal cord
|
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___ blocks NE reuptake
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desimpramine
|
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___ (3) are alpha2 agonists. they cause ___ (3)
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clonidine
romifidine xylazine sedation reduced BP reflex tachycardia |
|
in the brain, DA is produced in ___ (3)
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nigro-striatum
ventral tegmental area tubero-infundibulum |
|
___ are the DAergic cells that degenerate in PD. they control ___.
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nigro-striatal
movement |
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DAergic neurons in VTA project to ___ (3)
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mesolimbic areas
mesocortex locus ceruleus |
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tubero-infundibular DAergic neurons project via ___ to ___. they control ___.
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median eminence
pituitary PRL secretion |
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VTA DAergic neurons projecting to ___ areas, specifically ___, control reward and pleasure.
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mesolimbic
nucleus accumbens |
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DA increases/decreases appetite
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decreases
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D2 R blockers act as ___ (2) and can cause ___
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tranquilizers (neuroleptic)
antipsychotics parkinsonism |
|
amphetamines act via ___
4 side effects are ___ |
NE and DA reuptake inhibition
appetite suppression sterotyped behavior psychosis diarrhea |
|
alpha1 receptors signal via ___
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G_q -> PLC
|
|
alpha2Rs signal via ___
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G_i
|
|
betaRs signal via ___
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G_s
|
|
adrenoceptors present in the brain (3)
|
alpha1
alpha2 beta1 |
|
___ is a beta1 agonist
___ is a beta2 agonist ___ is a beta antagonist |
isoproteronol
albuterol propranolol |
|
___ is an alpha antagonist and is used in ___.
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phentolamine
hypertensive crisis |
|
there are ___ DAR subtypes, which are grouped into ___ (2)
|
5
D1-like D2-lie |
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___ (2) are D1-like DARs and signal via ___.
___ (4) are D1-like DARs and signal via ___. |
D1
D5 G_s D2_short D2_long D3 D4 G_i |
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___ is an antipsychotic D2 antagonist
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haloperidol
|
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in PD it's important to discontinue ___ (2) slowly. otherwise ___ (2) can happen.
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L-DOPA
anticholinergics immobilization neuroleptic syndrome |
|
3 positive symptoms of schizophrenia
these are caused by increased activity in ___ system |
delusions
hallucination aggressiveness mesolimbic |
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2 negative symptoms of schizophrenia
these are caused by decreased activity in ___ system |
cognitive decline
apathy mesocortical |
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identical twin concordance is ___% for schizophrenia
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48
|
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3 atypical antipsychotic drugs
these work by blocking ___ (3) |
risperidone
olanzapine clozapine 5-H2R M1R H1R (HA) |
|
3 side effects of typical antipsychotics
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parkinsonism
increased negative symptoms hyperprolactinemia |
|
4 risperidone side effects
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extrapyramidal
dizziness hyperactivity orthostatic hypotension |
|
olanzapine side effects
|
orthostatic hypotension
akathisia constipation |
|
clozapine side effect
|
agranulocytosis
|
|
___% of serotonin is in brain
|
1
|
|
in 5-HT synthesis, W is converted to ___ by ___
|
5-OH-W
W hydroxylase |
|
5-OH W is converted to ___ by ___
|
5-HT
AAADC |
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rate limiting step in 5-HT synthesis
|
W hydroxylase
|
|
W hydroxylase activity is increased by ___
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phosphorylation
|
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unlike Y hydroxylase, W hydroxylase has no ___
|
end-product inhibition
|
|
in the pineal gland, 5-HT is converted to ___, which regulates ___
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melatonin
circadian rhythm |
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in the brain, 5-HT is made in ___
|
raphe nuclei
|
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the ___ raphe neurons project to ___
the ___ raphe neurons project to ___ |
dorsal
median brain caudal spinal cord |
|
T/F: 5-HT controls thermoregulation
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true
|
|
5-HT is reuptaken by ___ and degraded by ___
|
SERT
MAO-A |
|
5HT1(A/B/D)R signals via
|
G_i
|
|
5HT2R and 5HT1CR signal via
|
G_q -> PLC
|
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5HT3R is a ___ and is ___tropic.
it causes ___. |
heterotetramer
iono nausea |
|
5HT4R, 5HT%R, 5HT6R signal via
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G_s
|
|
LSD acts on ___R.
this receptor is antagonized by ___. |
5HT2A
trazodone |
|
LSD causes sympathetic/para activation
|
symathetic
|
|
ecstasy is aka ___.
it acts via ___. |
methylene dioxymethamphetamine (MDMA)
5-HT reuptake inhibition |
|
prolonged use of MDMA can cause destruction of ___
|
5-HTergic neurons
|
|
4 side effects of MDMA
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hyperthermia
dehydration hyponatremia serotonin syndrome |
|
serotonin syndrome includes (4)
|
tachycardia
sweating mydriasis myoclonus |
|
2 kind of cholinergic connections in brain
|
projection
local circuit |
|
ACh projection neurons originate in ___ (2)
|
basal forebrain
pons |
|
local circuit ACh neurons are present in ___
|
striatum
|
|
nicotinic AChR is a ___ and is ___tropic. it is antagonized by ___toxin
|
pentamer
iono bungaro |
|
muscarinic AChR is ___tropic.
M1, M3, M5 AChRs signal via ___. M2, M4, AChRs signal via ___. |
matabo
G_q -> PLC G_i |
|
3 AChRs in the brain
|
M1
M3 M4 |
|
MAChR is agonized by ___ (2)
|
muscarine
pilocarpine carbachol betanechol |
|
MAChR is antagonized by ___ (2)
|
atropine
scopolamine |
|
3 AChEIs used in Alzehimer's
___ is less CNS specific and is ___toxic |
tacrine
donepezil rivastigmine tacrine hepato |
|
3 uses of scopolamine
|
antiemetic
amnesia sedation |
|
atropine can cause ___ in high doses
|
stimulation
|
|
___s irreversibly inhibit AChE
|
organophosphate
|