receptor classification - pharmacodynamics

Amoridei
Mind Map by Amoridei, updated more than 1 year ago
Amoridei
Created by Amoridei over 7 years ago
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pha 340

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receptor classification - pharmacodynamics
  1. Receptor Superfamilies
    1. G-Protein Coupled Receptors
      1. has the most receptors using it
        1. Metabotropic
          1. several types of intracellular signal transduction
          2. single polypeptide chain embedded in the cell membrane
            1. traverse membrane 7 times
              1. pentamer
            2. Ion Channels
              1. voltage-gated ion channels
                1. channels open in response to changes in voltage across cell membrane
                  1. Passage of ions: Na+, K+, Ca2+, Cl-
                    1. Voltage-gated Na+ channels
                      1. single poly-peptide chain
                        1. Depolarization
                          1. each domain becomes activated
                            1. inside of cell has become more positive as each domain becomes activated
                          2. BETA SUBUNITS
                            1. regulatory, maintain appropriate structure and fxn
                      2. 4 domains V-gated channel
                        1. 6 segments in each domain
                          1. change in voltage
                            1. S4
                            2. re-entrant loop
                              1. b/t segments 5 and 6
                              2. segment 6
                                1. local anesthetics
                                  1. bind to channel
                                    1. PREVENT DEPOLARIZATION
                                      1. STOPS PAIN SIGNALS FROM BEING SENT TO CNS
                              3. Inactivating region
                                1. domains 3 and 4
                              4. lidocaine, novacaine
                                1. cell response
                                  1. prevent depolarization
                                  2. tissue response
                                    1. block action potentials
                                    2. organ response
                                      1. loss of painful sensation
                                  3. Ligand gated receptors
                                    1. aka ionotropic or ion channel receptors
                                      1. Endogenous ligands
                                        1. ACh, GABA, glutamate, serotonin, glycine
                                          1. agonists
                                          2. Na+, Cl+, K+, Ca2-
                                            1. Nicotinic Acetylcholine Receptor
                                              1. Endogenous ligand Ach
                                                1. exogenous ligand: nicotine
                                                  1. used by neuromuscular blocker drugs
                                                    1. allosteric modulators bind to sites other than the binding site to change activity of receptor
                                                    2. nerve and muscle cells, esp. neuromuscular jxn
                                                      1. M segments
                                                        1. traverse membrane
                                                          1. M1-M4
                                                          2. straightens out to allow flow of Na+
                                                        2. quickly
                                                          1. pentamer
                                                        3. Enzyme-linked Receptors
                                                        4. classification based on how cell interacts
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