receptors

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  • Created by: Amh
  • Created on: 28-02-16 11:19
What are the 4 superfamilies of receptors
Ligand gated Ion channels,GPCR, kinase, Nuclear
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What are the main targets for drugs
enzymes, carriers, ion channels, receptors
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why is angiotensin a good example of specicifity
the peptide acts strongly vascular smooth muscle and kidneys, but not on other mooth muscle or epitelium
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how are specificity and potency related
higher specificity = lower potency. So the lower the potency of the drug the higher the dose needed leading to more side effect
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How do ligand gated ion channels bring about effect
ions cause hyper/depolarisation to bing about effect in ms, this is the fastest response
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Give an example of ligand gated ion channels
neurotransmitters AcH
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what are GPCR receptors
metabotropic receptors, change excitability this takes secs
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give an example of GPCR
Muscanaric receptors AcH
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what are kinase linked receptors how do they bring about change
pathway: ligand binding, protein phosphorylation, gene transcription, protein synthesis,
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Give an example of kinase linked receptors
cytokine receptors, Hourly basis
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nuclear receptors
take hours or days, cause changes at the DNA,
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give an example of nuclear receptors
oestrogen
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What are the structures of ligand gated ion channels
4/5 transmembrane domains n and c domain on the same side
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What is the structure of GPCRs
7 transmembrane domain, n and c on different sides
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What is the structure of kinase linked receptor
linked to a kinase (tyrosine usually) one single transmembrane domain and n and c on either side of membrane
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What is the structure of nuclear receptors
no nucler spanning domains - sinsce they are either in cytoplsm or nucleus. They have zinc fingers - important consitutent for receptor pathwaway
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What is the prototypical example of a ligand gated ion channel, and give an outline
nicotinic acetyl choline receptor nAChr. Is a pore, has a pentameric structure, diffferent subtypes based on alpha or beta or a mix. 2AcH bind, causing a conf change in alpha helices, opening the pore, allowing Na+, leading to depolaisation,
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Where are nAcH receptors found
neuromusclar junction -autonomic gangia -CNS -presynapticly located
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Card 2

Front

What are the main targets for drugs

Back

enzymes, carriers, ion channels, receptors

Card 3

Front

why is angiotensin a good example of specicifity

Back

Preview of the front of card 3

Card 4

Front

how are specificity and potency related

Back

Preview of the front of card 4

Card 5

Front

How do ligand gated ion channels bring about effect

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