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DRUGS > Drugs 3 - Catecholamines > Flashcards

Drugs 3 - Catecholamines Flashcards

1
Q

Noradrenaline cell bodies:

A

around 10,000 in the medulla and pons. mainly the locus coreleus but also solitary nucleus and lateral tegmental area

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2
Q

Noradrenaline projections

A

LTA and SN to the spinal cord. locus coreleus to the amygdala, hypothalamus and thalamus cerebellum and cortex

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3
Q

Noradrenaline transmission

A

almost paracrine from noradrenergic viscosities rather than nerve terminals. occur along the length of a population of neurons effecting all cells they pass.SYNAPSES EN PASSANT

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4
Q

Noradrenaline reuptake

A

both synaptic degradation (MAO and COMT) and transporters (NET)

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5
Q

Noradrenaline receptors

A

a1/2 b1/2/3

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6
Q

Noradrenaline a1

A

cAMP (-)

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7
Q

Noradrenalinea2

A

autorecptor IP3 (+)

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8
Q

Noradrenaline B1

A

cAMP (+)

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9
Q

Noradrenaline B2

A

cAMP (+)

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10
Q

Noradrenaline B3

A

cAMP(+) periphery only

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11
Q

functions of Noradrenaline receptors

A

autonomic function (HR, blood pressure and motor) and cognitive function (mood, fear, attention) TPJ = circuit breaker

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12
Q

Drug targets:

A

–synthesis –reuptake (NET) –a2 –a/1b1/2/3 –MAO –vesicular packaging and release (reserpine)

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13
Q

what is responsible for Noradrenaline vesicular packaging and release

A

reserpine

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14
Q

what is NA synthesised from

A

tyrosine

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15
Q

Dopamine is synthesised in

A

cells in the Substantia nigra and ventral tegmentum

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16
Q

how do dopaminergic cells differ from adrenergic ones

A

they don’t contain phenylethanolamine N-methyltransferase

17
Q

dopaminergic pathways

A

meso limbic
meso cortical
nigrostriatal
tuberohypophoseal

18
Q

mesocortical pathway

A

from VTA to frontal lobe -the reward pathway. when we plan an action and its successful we reward ourselves with dopamine

19
Q

mesolimbic pathway

A

VTA to the amygdala and nucleus accumbens

20
Q

tuberophypophoseal

A

VTA to the pituitary, median eminence, hippocampus, hypothalamus - very short

21
Q

Nigrostriatal

A

SN to BG - movement, 75% of dopaminergic cells. 1 SN cell has 500,000 striatal synapses

22
Q

Dopamine functions

A

reward, movement, cognitive functions and modulation of other modulators (NA by locus coreleus and ACh) attention

23
Q

Dopamine modulation of ACh

A

Acts in the prabrachium presnaptically to increase ACh release (cog enhancement - attention and arousal)

24
Q

Dopamine receptors

A

Genreally post synaptic. D1 and D2 change levels of cAMP which acts with PKA to convert darpp to phospho darpp. phosphodarpp inhibits protein phophotase 1. PP1 strips other proteins and phosphotase enzymes to decrease activity.
This process is amplified so a little receptor inout has a big effect.
d1 and 2 generally found on different cells

25
Q

D1

A

excitatory. D1, D5. increase cAMP

26
Q

D2

A

inhibitiory, decrease cAMP,

d2,3,4

27
Q

Seratonin synthesised

A

from tryptophan (diet) in the raphe nuclei (medula and pons)

28
Q

serotonin projections

A

project back to spine medulla and cerebellum. Mainly forward to cortices and to hippocmapus, striatum, thalamus, hypothalamus, amygdala through same bundle as NA.

29
Q

serotonin metabolism

A

broken down by MAO to aldehydes then to v. soluble easily removable substrate by aldehyde dehydroxylase. No COMT involvement because its not a catecholamine

30
Q

serotonin receptors

A

all GPCRS except 5HTR-3. 1-7. Huge diversity is very good for drug targets.

31
Q

5HTR-1

A

presynaptic autoinhibitor

32
Q

5HTR-2

A

pre and post synaptic in cortex

33
Q

5HTR-3

A

ligand gated in cortex

34
Q

5HTR-4

A

limbic system and basal ganglia. also increases presynaptically increases ACh release so cog enhancement

35
Q

5HTR-5

A

No one knows!

36
Q

5HTR-6

A

hippocampus, cortex, limbic system

37
Q

5HTR-7

A

hippocampus, cortex, amygdala and thalamus - also GABA modulation

38
Q

Dopamine metabolism

A

MAO –> aldehyde

Aldehyde dehydroxylase + COMT –> HVA (verysoluble and easy to remove)

39
Q

serotonin dopamine and ach receptors also found

A

on the area postremma for vomiting

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