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Foundations 2 Desai > Receptor Families > Flashcards

Receptor Families Flashcards

1
Q

What is the mechanism of strychine?

A

competitive inhibitor of glycine channels

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2
Q

List the receptor families in order of fastest to slowest desensitization.

A
  1. ligand gated (AMPA is fastest)
  2. GPCR (B arrestin leads to internalization of GPCR receptors)
  3. RTKs
  4. cytoplasmic glucocorticoid
    receptors
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3
Q

What is the difference between cys loop families and non cys loop families?

A

have 5 subunits with four membrane spanning domains

cys loop families have a loop of 13 AAs held together by cysteine in alpha subunit

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4
Q

What is the mechanism of Zolpidem?

A

not benzodiazepine, but allosteric activator of GABAa used to induce sleep

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5
Q

What RTK pathway do cytokines use and what are the results?

A

JAK/STAT pathway, increases gene transcription and coordinates immune response

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6
Q

What is the mechanism of drugs with -sons or -ones suffix?

A

activates cytoplasmic glucocorticoid receptors

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7
Q

Why is Zolpidem Swati’s favorite drug?

A

because it induces sleep and is effective for years (as an allosteric activator)

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8
Q

What is the mechanism for drugs with a -setron suffix?

A

competitive inhibitor of serotonin 5-HT3 channels used to treat nausea and vomiting

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9
Q

Which receptor desensitizes the fastest?

A

AMPA

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10
Q

What is the mechanism of drugs with an -azepam and -azolam suffix?

A

benzodiazepines (ex: diazepam) are allosteric activators of GABAa receptors that are used to treat anxiety

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11
Q

What are the four excitatory ligand gated receptors?

A

nicotinic, serotonina 5-HT3, P2X ATP and Glutamate

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12
Q

List the receptor families from fastest to slowest.

A

ligand gated channels
GPCRs
tyrosine kinases (RTKs)
cytoplasmic/nuclear receptors

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13
Q

How do GPCRs lead to relaxation of smooth muscle and contraction of cardiac muscle?

A

activation of a3 G protein which activates adenylyl cyclase which activates cAMP which activates PKA and leads to protein phosphorylation

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14
Q

What is the mechanism of tetanus toxin?

A

blocks pre synaptic release of glycine

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15
Q

What are the good and bad consequences of NMDA receptor activation?

A

at normal levels, mediates learning and memory

at very high levels, there is excess Ca2+ that leads to excitotoxicity and diseases like Alzheimer’s

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16
Q

What is the mechanism of the glucocorticoid receptor?

A
  1. steroid diffuses into cell and binds cytoplasmic glucocorticoid receptor
  2. receptor was bound to HSP90, which inhibited it but releases HSP90 upon binding of steriod
  3. steroid/receptor dimerizes and goes to nucleus causing changes in gene transcription
17
Q

What RTK pathway do growth factors use and what is the result of the pathway?

A

RAS/MAPK pathway which leads to increase in transcription ultimately resulting proliferation, wound healing, adhesion and migration

18
Q

What is the mechanism of memantine?

A

uncompetitive inhibitor of NMDA receptors to treat diseases like Alzheimer’s by blocking intake of Ca2+

19
Q

Describe the inhibitory motif of GPCRs

A

subscript of 2 is used
By: stimulates K+ or inhibits Ca2+
alpha i: inhibits adenylyl cyclase
leads to neurotransmitter release

20
Q

What RTK pathway does insulin use and what are the results?

A

mainly PI-3/AKT/mTOR pathway which increases translation to increase fuel uptake and storage

21
Q

How do GPCRs lead to contraction of smooth muscle?

A

subscript of 1 or 3 is used

a2 G protein activated PLC which causes synthesis of IP3 leading to Ca2+ release and smooth muscle contraction

22
Q

What are the two types of glutamate ligand channels?

A

non-NMDA (AMPA) and NMDA

23
Q

How does AMPA function?

A

mediate fast excitatory synaptic transmission in CNS, non-selective ligand gated Na+ channels

24
Q

What type of drug does not lead to quick desensitization?

A

allosteric activators

25
Q

What is hyperkplexia?

A

familial startle disease, best known channel disease

caused by mutation in a subunit so can’t bind glycine

26
Q

What is desensitization?

A

decreasing response in continuous presence of the drug occurs
has to be above EC50

27
Q

What is the general mechanism of RTKs?

A
  1. ligand binding domain binds ligand
  2. subunits dimerize and phosphorylate each other
  3. activated RTK recruits scaffold protein
  4. scaffold protein initiates kinase-kinase-kinase activity
  5. biological response due to phosphorylation cascade
28
Q

What are the inhibitory ligand gated receptors?

A

Cl- channels: GABAa receptors and glycine receptor

29
Q

What is the mechanism of penicillin?

A

blocks GABAa receptors uncompetitively, can cause seizures if at toxic levels

Foundations 2 Desai (12 decks)

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