Ionotropic & Metabotropic Receptors Lesson 12
Membrane Proteins: Ionophores n Ion Channels n Non-gated l always open n Gated l chemically-gated l electrically-gated l mechanically-gated ~
Chemically-Gated Channels n Ligand-Receptor binding n Ligand l neurotransmitters l drugs n Receptor proteins l ligand binds to multiple receptors l receptor subtypes l specificity ~
Ligand-Receptors Binding n Binding site l specific point of ligand & receptor n Affinity l attraction l physical & electrical fit n NT or drug binds to receptor l or activity of neuron l excite or inhibit n Drugs mimic or block NT message ~
Lock & Key Model n Receptor changes shape n Excitation or Inhibition? l Determined by nature of receptor n NOT NT ~ n NT binds to receptor l NT = key l Receptor = lock
Receptor Subtypes n Specificity n Same NT l Binds to many receptor subtypes l Produce different effects l EPSP or IPSP n All NT systems l Several subtypes each l Drug side effects ~
Receptor A NT n ligand binds to receptor l activation: EPSP or IPSP ~
Receptor B Receptor A n Same NT can bind to different -R l different part of NT ~ NT
Receptor B Receptor A n Same NT can bind to different -R l different part of NT ~ NT
Receptor B Receptor A n Same NT can bind to different -R l different part of NT ~ NT
Ionotropic receptors n Ligand-gated channels l Ion channels n NT directly controls channel l fast action l transient ~
Metabotropic Receptors n Requires energy l GTP l Neuromodulation n G protein-gated Ion Channels l Receptor indirectly controls channel l relatively fast, but slower than ionotropic ~
G protein-gated Ion Channels R G GDP
G protein-gated Ion Channels R G GTP
G protein-gated Ion Channels R G GTP Pore
Metabotropic receptors: 2d messenger systems n 2d messenger systems l Effects relatively slow l long-lasting l Signal amplification n Effects l Control channel l Alter properties of receptors l regulation of gene expression ~
2d Messenger Systems n Signal amplification l 1 NT activate enzyme l ATP 1000s cAMP 10,000s l cAMP 10,000s phosphates ~
2d Messenger Systems Receptor trans- ducer primary effector external signal: nt 2d messenger secondary effector Receptor trans- ducer primary effector external signal: nt 2d messenger secondary effector n External signal l NT = 1st messenger n Membrane-associated components l Receptor l Transducer l Primary effector n Intracellular l 2d messenger l Secondary effector ~
2d Messenger Systems R G GTP GDP * Secondary Effector Primary Effector Enzyme
2d Messenger Systems R G GTP Secondary Effector Primary Effector Enzyme
2d Messenger Systems R G GTP ATP cAMP Secondary Effector Primary Effector Enzyme
2d Messenger Systems R G GTP ATP cAMP P Secondary Effector Primary Effector Enzyme
2d Messenger Systems R G GTP ATP P Pore cAMP Secondary Effector Primary Effector Enzyme