L16 CNS Flashcards

(43 cards)

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
GABA B2 =
signalling transduction
26
Where can GABA(A) be found
* Synapse * Extrasynaptically (outside synapse)
27
Serotonin receptor (5-HT3)
* LGIC * Excitatory * Involved in throwing up
28
Serotonin (5-HTx) | x = 1, 2, 4-7
* All GPCR * Inhibitory * Coupled to G(ai)
29
Glutamate and glutamate receptors
* NMDA - glutamate and glycine are co-agonist * Apart of LGIC * has synaptic plasticity | Other = AMPA/ Kainate (LGIC)
29
5-HT(1A) receptor infor
* 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
Types of dopamine receptors
* D1 (D1 and D5) * D2 (D2, D3 and D4)
31
D1 types info
* High expression in nigrostriatal, mesolimbic and mesocortical areas * Posyn D1 will ↑ locomotor activity
32
D2 type receptors
* Presyn: ↓ firing rate of NT release * Postsyn: ↓ locomotor activity * Postsyn: Inhibit prolactin secretion from pituitary gland
33
Dopamine 4 pathways (big)
* 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
# D Substania nigra to striatum:
motor control (nigrostriatal)
35
# D Vental tegmental area to amygdala, NAc:
mesolimbic path - memory, emotion and reward
36
# D Ventral tegmental area to prefrontal cortex:
mesocortical pathway - executive function and emotion
37
# D Hypothalamus to pituitary gland:
(tuberohypophyseal) endocrine control (inhib prolactin)
38
Antipsychotics
* D2 antagonist * Chronic = hyperprolactinemia * ⤷ : ↑ prolactin secretion * Extrapyramidal effects like akathisia
39
D2 antagonist
Antipsychotics | Metaclopramide
40
Metaclopramide
* D2 antagonist * Antimetic effects on GI tract and CTZ * Extrapyramidal adverse on brain
41
Metaclopramide PCD
* antagonist of D2 * Affinity and no efficacy
42
Metaclopramide PCK
* metabolised by CYP2D6 * LopP-2.6 therefor lipophilic and cross BBB