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Neuroscience > L5 - basic concepts in neuropharmacology > Flashcards

L5 - basic concepts in neuropharmacology Flashcards

1
Q

what affects the fraction of receptors in the R* state

A

drugs

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2
Q

receptor with constitutive activity

A

no ligand bound but equilibrium lies more towards activated state

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3
Q

non-zero baseline on graph

A

shows receptor with constitutive activity

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4
Q

agonist ligand - greater affinity for…

A

R* state (activated)

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5
Q

full receptor agonists reach

A

receptor saturation

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6
Q

inverse agonist

A

equilibrium held towards R state

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7
Q

antagonist ligand

A

prevents ligand binding therefore no downstream signalling

reversible or irreversible

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8
Q

reversible antagonist ligand

A

competes for agonist binding site

reversible binding

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9
Q

irreversible antagonist ligand

A

change conformation of receptor
reduces ability of agonist to bind
strong covalent bond - remains bonded until internal recycling

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10
Q

affinity

A

how well a drug binds to its receptor

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11
Q

efficacy

A

how well a receptor-bound drug elicits a response

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12
Q

potency

A

amount of drug required to elicit a response

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13
Q

allosteric modulators

A

impact receptor function by binding at an alternative receptor site

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14
Q

2 binding sites

A

orthosteric (enogenous)

allosteric site

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15
Q

how do you change the affinity of the orthosteric ligand

A

elicit conformational change of receptor so drug binds more/less easily

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16
Q

positive allosteric modulation

A

binding of ligand to receptor enhances signalling

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17
Q

when you change the efficacy of the orthosteric ligand

A

binding is unaffected

downstream signalling is affected (potential larger maximal response)

18
Q

neurotransmitter

A

biochemical that mediates fast-acting direct communication between two neurons

19
Q

neuromodulator

A

biochemical that modulates activity of neurons and neural networks by changing the ability of neurons to respond to neurotransmitters

20
Q

examples of amino acid neurotransmitters

A

glutamate
gaba
glycine
aspartate

21
Q

exmaples of biogenic amine neurotransmitters

A

ACh
histamines
monoamines

22
Q

types of monoamine neurotransmitters

A

serotonin

catecholamines (dopamine, adrenaline, noradrenaline)

23
Q

how does nitric oxide signalling modulate neurotransmission

A

Ca2+ influx downstream of ion channel
causes activation of nNOS
increased intracellular NO concentration

24
Q

nNOS

A

neuronal Nitric Oxide Synthase

25
Q

glial cells release transmitters that modulate neurotransmission

A

gliotransmitters

neurotransmitters

26
Q

ionotropic receptors

A

ligand gated ion channels
transmembrane
mediate fast-transmission (open quickly)

27
Q

examples of ionotropic receptors

A

nicotinic ACh R
5-GT
glycine receptors

28
Q

ionotropic glutamate receptors

A

NMDA
AMPA
Kainate

29
Q

NMDA receptor

A

ionotropic glutamate receptor with Mg2+ block

30
Q

glycine is an +ve allosteric modulator to…..

A

NMDA

31
Q

metabotropic receptors

A

couple via 2nd messengers
GPCR, RTK
indirectly open ion channels
2nd fastest

32
Q

when ligand binds to RTKs

A

transautophosphorylation at Tyr residues

SH2 domains recruited

33
Q

cytokine receptors

A

-ve feedback
bind to cytokines and transduce their signals
cytokines are neuromodulators
slower transmission

34
Q

put the receptors in order of speed of transmission

x4

A

ionotropic
metabotropic
cytokine
hormone

35
Q

hormone receptors

A

e.g. glucocorticoid/oestrogen receptor

36
Q

when does receptor desensitisation occur

x2

A

at high levels of agonist exposure

due to chronic exposure to agonist ligand

37
Q

mechanisms causing reduced response to ligand binding to receptor (receptor desensitisation)
x3

A

uncoupling
receptor internalisation
reduced receptor expression

38
Q

receptor desensitisation can lead to….

A

drug tolerance

39
Q

arrestins effect on GPCRs

A

proteins that mediate homologous desensitisation of GPCRs

cause uncoupling and receptor internalisation

40
Q

tachyphylaxis

A

acute sudden decrease in response to drug after administration

41
Q

tolerance

A

decreased response to drug after chronic use

42
Q

addiction

A

behavioural manifestation of tolerance

Neuroscience (14 decks)

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