Pharm NT I Flashcards

1
Q

what are the classes of NT

A

amino acids
small molecule
peptides
endocannabinoids

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2
Q

what are the excitatory aa NT

A

glutamate and aspartate

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3
Q

what are the inhibitory aa NT

A

GABA and Glycine

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4
Q

What are the small molecule transmitters

A

Ach
Monoamines
histamine

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5
Q

what are the monoamines

A
catecholamines: dopamine and norepi
and serotonin (5-HT)
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6
Q

what are the peptide NT

A

opiods
tachykinins
others

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7
Q

what are the opioid NT

A

enkephalins
endorphins
dynorphins

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8
Q

what are the tachykinins

A

substance P

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9
Q

Where are small moleules NT made

A

in the nerve terminals then loaded into vesicles ATP dependent

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10
Q

where are peptides made

A

cell body and packaged there

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11
Q

depolarization to the presynaptic nerve acticates what

A

vCaCh causing fusion vesicles and release

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12
Q

drugs that act in CNS modify what

A

the chemical synaptic transmission

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13
Q

presynaptic sites of drug action include what

A

NT synthesis, storage, metabolism and release

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14
Q

what is the primary postsynaptic site of drug action

A

NT receptor

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15
Q

what are the 3 criteria for classical NT

A

localization
release
synaptic mimicry

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16
Q

what is an exception to the synaptic mimicry rule

A

sometime more than one substance transmits information so no single agonist or antagonis can mimic stimulation

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17
Q

what messengers are not synthesized or stored in presynatpic terminal

A

endocannabinoids

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18
Q

what ion channels modulate neuronal firing rate

A

Ca and K

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19
Q

What are ionotropic R

A

ligand gated ion channels

causes conformational change that opens channel or closes it

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20
Q

what causes EPSP

A

influx Na or Ca

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21
Q

what causes IPSP

A

efflux of K or influx Cl

22
Q

what NT activate ionotropic R

A
glutamate
GABA
Ach
Glycine
Serotonin
23
Q

how to metabotropic R work

A

GPCR that indirectly modulate ion channels

24
Q

major functional effects GPCRs

A

signal amplification

25
What are the second messengers in GPCRs
adenylate cyclase and cAMP DAG IP3 ion Ca K Na or Cl
26
what NT activate metabotropic R
``` glutamate GABA Ach dopamine Norepi Serotonin Histamine Neuropeptides Endocannabinoids ```
27
does glutamate cross bbb
no | but it is made in brain from glucose
28
what inactivates glutamate
taken up by glial cells and converted to glutamine then transported to glutamatergic nerve cells and converted back to glutamate
29
What R does glutamate activate
ionotropic | non-NMDA and NMDA
30
what R mediate most EPSP in prain
the AMPA or non NMDA GluR1 2,3,4 ligand gated Na K Ch glutamate!!!
31
overstimulation NMDA R in brain cause what
Ca influx triggering cell death | especially in ischemia and hypoxia
32
what ion blocks NMDA channels until depolarized
Mg
33
what is PCP
phencyclidine "angel dust" ketamine
34
how does PCP work
noncompetetice antagonist at NMDA R | high does cause dissociative anesthesia
35
R subtypes for the NMDA R
NR1, 2A,2B,2C,2D
36
what metabotropic R does glutamate activate on postsynapse
decrease K conductance increasing IP3 and DAG
37
effects of glutamate on presynaptic GPCR
dec Ca (inhibitiory) dec cAMP
38
what can cause the aura of migraine headaches
excessive glutamate release
39
why is NMDA R antagonist memantine used to Tx severe dementia in alzheimers
glutamade R mediated excitotoxicity may contribute to pathogenesis of the disease
40
synthesis of GABA
locally from glucose, pyruvate, sometimes other aa
41
inactivation GABA
rapid reuptake from plasma membrane transporters | also taken up by glial cells
42
GABAa activates what R
ionotropic | ligand Cl Ch (hyperpolarization IPSP)
43
GABAb
metabotropic post synaptic (inc K) presynaptic (dec Ca inhibitory)
44
what balances excitatory activity of glutamate
GABA inhibition
45
GABA dysfunction leads to
hyperexcited states
46
where do benzodiazepines and barbituates work
GABAa | so enhance inhibitory effects of GABA
47
what are the benzodiazepines
alpazolam diazepam midazolam clonazepam
48
benzodiazepines are used to Tx
anxiety disorder, panic, sedation and sleep disorders
49
what is phenobarbital
barbituate
50
what is phenobarbital used for
sedative hypnotics and antiepileptics