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Receptors and transduction mechanisms II Chapter 12 –The Neuron by Levitan and Kacsmarek
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Metabotropic receptors (G-protein- coupled receptors, GPCR
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IN the case shown here, binding of neurotransmitter (NT) to its receptor activates a G protein that then interacts with an ion channel, causing it to open Metabotropic receptors (G-protein-coupled receptors, GPCR)
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an intracellular second messenger influences ion channel activity Second messenger-mediated receptor-channel coupling
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SLOW INDIRECT GPCR coupling These receptors are not directly coupled to their ion channels and transduce the signal via guanyl nucleotide-binding proteins (G-proteins) that activate intracellular second messenger pathways
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Why are GPCR responses slower and longer lasting than iR responses? Allows a constant modification temporal information processing
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Generic GPCR structure Why 7TMs?
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Human -adrenergic receptor TMIII – Asp (D113) binds to N-terminus of epinephrine TMV – two Ser (S204 +S207) binds to 2 OH termini
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Intracellular signal transduction by the PIP2 cascade
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mGluR1/5 Homer Ca 2+ IP 3 R
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GPCR coupling can produce diverse responses Depends on type of G-protein and type of effector Single ligand can activate multiple GPCR pathways Depends on receptor numbers
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Responses can be regulated by altering receptor numbers
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Desensitisation is a mechanism of decreasing the cellular response to transmitter Physical removal by receptor- mediated endocytosis Desensitisation is defined as the increase in agonist required to produce ahalf-maximal stimulation of effector Brought about by receptor phosphorylation
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Some types of GPCR
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group I, II and III metabotropic glutamate (mGlu) receptors Trends in Pharmacological Sciences Volume 25, Issue 5, May 2004, Pages 265-272
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Nature Reviews Drug Discovery 4, 131-144 (2005) Metabotropic glutamate receptors as novel targets for anxiety and stress disorders
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neurotransmitter pathways implicated in mediating the actions of drugs of abuse (rat brain)
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A metabotropic glutamate (mglu) receptor associated with a heterotrimeric G protein Trends in Pharmacological Sciences Volume 22, Issue 3, 1 March 2001, Pages 114-120 Residues that control the coupling of metabotropic glutamate (mglu) receptors to G proteins
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group I, II and III metabotropic glutamate (mGlu) receptors neurotransmitter pathways implicated in mediating the actions of drugs of abuse (rat brain)
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1) G protein-mediated receptor-channel coupling. IN the case shown here, binding of neurotransmitter (NT) to its receptor activates a G protein that then interacts with an ion channel, causing it to open. 2) Second messenger-mediated receptor-channel coupling: an intracellular second messenger influences ion channel activity. 3) With second messenger coupling the binding of a single transmitter can activate many channels, activate several classes of channels and affect other cellular processes not associated with ion channels.
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