Lecture 8+9 - Neurotransmitters

Inverse agonist ro 154513 ro154513 a gabaa antagonist

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Unformatted text preview: determines its overall pharmacological properDes –  Glutamate –  Glycine •  Obligatory co ­agonist •  Inhibitory NT at its own receptor –  Zinc (inverse agonist) –  Polyamine (indirect agonist) •  2 inside cell –  Magnesium (inverse agonist) –  PCP (inverse agonist) GABA (Gamma Aminobutyric Acid) •  Principal Inhibitory NT •  Biosynthesis: Glu Glutamic Acid Decarboxylase (GAD) and B6 GABA •  Removed by reuptake •  2 receptor types •  GABAA GABAC (ionotropic; Cl ­ channel) •  GABAB (metabotropic; K+ channel) GABAa Binding Sites •  GABA •  Benzodiazepine (indirect agonist) –  Probably also site for alcohol –  Endogenous inverse agonist binds here •  Barbiturate (indirect agonist) •  Steroid (indirect agonist) •  Picrotoxin (inverse agonist) Phosphate groups aZach to the receptor inside the cell and regulate receptor sensiDvity (via phosphorylaDon) to agents such as alcohol GABAergic Drugs •  Agonists (anD ­anxiety) Benzodiazepines   Barbiturates   Ethyl alcohol (ETOH)   •  Antagonists •  Picrotoxin •  Inverse agonist Ro 15 ­4513   Ro15 ­4513, a GABAa antagonist (indirect for GABA, direct for alcohol) reverses alcohol intoxicaDon Biogenic Amines •  Medium concentraDon in brain (na...
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This note was uploaded on 03/21/2014 for the course COGS 174 taught by Professor Pineda during the Winter '11 term at UCSD.

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