central noradrenergic and serotoninergic systems/ MOOD DISORDERS Flashcards
List the sites of CNS drug action (7)
1) conduction
2) synthesis and storage
3) release and reuptake
4) degradation
5) receptors
6) ion channels
7) second messengers
name the monoamines
%of synapses, brain conc, function, primary receptor class
- catecholamines: DA,NE, EPI
- indoleamines: serotonin
- 2-5 synapses
- low conc
- slow change in excitability(sec)
- GPCRS
acetylcholine
%of synapses, brain conc, function, primary receptor class
- 5-10 synapses
- low conc
- slow change in excitability
- GPCRS
name the amino acids (inhibitory & excitatory)
- inhibitory: GABA& glycine
- 15-20 synapses
- high conc
- rapid inhibition (msecs)
- ion channels
2.excitatory: Glutamate& aspartate
- 75-50 synapses
- high conc
- rapid excitation
- ion channels
DA receptors
D1-5
all are GPCRS
NE/EPI receptors
a1&2
b1,2,3
all are GPCRS
5-HT receptors
5-HT1A
5-HT1B
5-HT1D –>Gi, inhibitory
5-HT2A
5-HT2B
5-HT2C –>Gq, excitatory
5-HT3 (LG) !!! –> excitatory
5-HT4 –> Gs, excitatory
5-HT5 –> Gi–> inh
5-HT6-7 –> Gs–> excit
all GPCRS except 5HT3
Ach receptors
Muscarinic M1 Muscarinic M2 Muscarinic M3 Muscarinic M4 Nicotinic
all GPCRS except nicotinic
Glutamate receptos
NMDA
AMPA
Kainate Metabotropic
all LG except metab!!!
GABA receptors
GABA A: LG
GABA B: G
MAO (4)
1) cofactor: FLAVIN
located in the outer membrane of mitochondria
2) convert amine into aldehyde (followed by aldehyde dehydrogenase to acids or aldehyde reductase to glycol)
3)-MAO A: NE & 5HT
inhibited by CLORGYLINE
-MAO B: DA
inhibited by DEPRENYL
4) PTS treated with MAOi for HTN or depression may have severe HTN after ingestion of foods with high amounts of tyramine
COMT
1) enzyme can metabolize both intra and extracellularly
2) requires Mg2+ and substrate of S-adenosylmethionine
monoamine metabolites formed in the CNS
1) NE–> MHPG (MAO & COMT)
2) DA–> HVA (MAO &COMT)
3) 5HT–>5HIAA (MAO)
CNS functions regulated by NE
1) arousal
2) mood
3) blood pressure control
CNS functions regulated by 5HT
1) sleep
2) mood
3) sexual function
4) appetite