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PHAR222 > L16 CNS > Flashcards

L16 CNS Flashcards

1
Q

The CNS spinal cord and brain has

A
  • 100 Bil neurons and non-neuronal cells (glia)
  • Trillions of synapses
  • Synaptic plasticity
  • Brain areas that form neuronal circuits
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2
Q

Types of drugs that act clinically on the brain

A
  • Antidepressants
  • Anxiolytic
  • Analgesics
  • Anaesthetics
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3
Q

Two types of neuronal communications

A
  • Electrical coupling through gap junctions
  • CHemical signalling through NT and synapses
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4
Q

NT

A
  • Chemical messengers
  • Relay info from neurons to muscles or between neurons
  • Has more than one lomecular targets and their locations
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5
Q

4 Main neuronal communication targets

A
  • 4) degradation of surplus transmitter
  • 9) interaction iwth postsynaptic receptors
  • 11) reuptake of transmitter or degradation products
  • 13) interaction with presynaptic receptors
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6
Q

2 important receptor superfamilies

A
  • Ligand gated ion channels (ms)
  • G protein coupled receptor (s)

Both found in cell membranes

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7
Q

What receptor type is a GABA(A) receptor

A

ligand-gated ion channels

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8
Q

What receptor type is a µ opioid receptor

A

G-protein coupled receptor

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9
Q

What is this

  • Release of transmitters (ms)
  • Fast synaptic transmission
A

L-g ion channels

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10
Q

What is this

  • Slow synaptic transmission
  • Neuromodulation
A

G protein-coupled receptor

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11
Q

4 types of mediators

A
  • Small-molecule mediators
  • Neurotrophins
  • Neuropeptides
  • Lipid Mediators
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12
Q

Mediator

Small-molecule example, target and drug class

A
  • GABA and serotonin
  • LGIC and GCPR
  • Gaba = Anxiolytics
  • Serotonin= Antidepressants
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13
Q

Mediators

Neurotrophin: example, target and drug class

A
  • Brain-devrived neurotrophic factor
  • Kinase-linked receptors
  • Antidepressants
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14
Q

Neuropeptides: example, target and drug class

A
  • Endorphines
  • GPCR
  • Opioid analgesics
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15
Q

Lipid mediators: example, target and drug class

A
  • Prostaglandins
  • GPCR
    Non-opioid analgesics
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16
Q

NT on molecular targets can be

A
  • exciatotry
  • Modulatory
  • Inhibitory
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17
Q

Types of small NT

A
  • GABA (1º inhibitory NT)
  • Serotonin
  • Glutamate (1º excitatory NT)
  • Dopamine
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18
Q

GABA has what types of receptor superfam

A

LGIC and GPCR

19
Q

Serotonin has what types of receptor superfam

A

LGIC and GPCR

20
Q

Glutamate has what types of receptor superfam

A

LGIC and GPCR

21
Q

Dopamine has what types of receptor superfam

A

G-protein coupled receptor

22
Q

GABA(A) receptor info

A
  • LGIC
  • 19 subunits but mainly 2 alpha, 2 beta and a 3rd (to make up 5)
23
Q

GABA B1 =

A

ligand binding

24
Q

GABA(B) receptor info

A
  • Heterodimer of B1 and B2
  • B1 = ligand binding
  • B2 = signalling transduction
25
Q

GABA B2 =

A

signalling transduction

26
Q

Where can GABA(A) be found

A
  • Synapse
  • Extrasynaptically (outside synapse)
27
Q

Serotonin receptor (5-HT3)

A
  • LGIC
  • Excitatory
  • Involved in throwing up
28
Q

Serotonin (5-HTx)

x = 1, 2, 4-7

A
  • All GPCR
  • Inhibitory
  • Coupled to G(ai)
29
Q

Glutamate and glutamate receptors

A
  • NMDA - glutamate and glycine are co-agonist
  • Apart of LGIC
  • has synaptic plasticity

Other = AMPA/ Kainate (LGIC)

29
Q

5-HT(1A) receptor infor

A
  • Somatodendric on 5HT neurons in raphe nuclei -> cause negative feedback
  • Located postsynaptically in many brains regions
  • Antidepressant effect (med)
  • inhibitory; coupled to Gi

Cell bodies in pon, upper medulla, project to cerebellum medulla and SC

30
Q

Types of dopamine receptors

A
  • D1 (D1 and D5)
  • D2 (D2, D3 and D4)
31
Q

D1 types info

A
  • High expression in nigrostriatal, mesolimbic and mesocortical areas
  • Posyn D1 will ↑ locomotor activity
32
Q

D2 type receptors

A
  • Presyn: ↓ firing rate of NT release
  • Postsyn: ↓ locomotor activity
  • Postsyn: Inhibit prolactin secretion from pituitary gland
33
Q

Dopamine 4 pathways (big)

A
  • Substania nigra to striatum: motor control (nigrostriatal)
  • Vental tegmental area to amygdala, NAc: mesolimbic path - memory, emotion and reward
  • Ventral tegmental area to prefrontal cortex: mesocortical pathway - executive function and emotion
  • Hypothalamus to pituitary gland: (tuberohypophyseal) endocrine control (inhib prolactin)
34
Q

D

Substania nigra to striatum:

A

motor control (nigrostriatal)

35
Q

D

Vental tegmental area to amygdala, NAc:

A

mesolimbic path - memory, emotion and reward

36
Q

D

Ventral tegmental area to prefrontal cortex:

A

mesocortical pathway - executive function and emotion

37
Q

D

Hypothalamus to pituitary gland:

A

(tuberohypophyseal) endocrine control (inhib prolactin)

38
Q

Antipsychotics

A
  • D2 antagonist
  • Chronic = hyperprolactinemia
  • ⤷ : ↑ prolactin secretion
  • Extrapyramidal effects like akathisia
39
Q

D2 antagonist

A

Antipsychotics

Metaclopramide

40
Q

Metaclopramide

A
  • D2 antagonist
  • Antimetic effects on GI tract and CTZ
  • Extrapyramidal adverse on brain
41
Q

Metaclopramide PCD

A
  • antagonist of D2
  • Affinity and no efficacy
42
Q

Metaclopramide PCK

A
  • metabolised by CYP2D6
  • LopP-2.6 therefor lipophilic and cross BBB

PHAR222 (25 decks)

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