Home >> Flashcards >> Pharmacology >> GABAergics: Barbituates/Benzos etc
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| zwitterionic, not an alpha amino acid, agonizes GABA receptors resulting in Cl- influx |
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| imidazole ring on the top helps give it antagonist properties at benzo receptor. note that the thir aromatic ring is missing and so is the number 5 phenol group. USE: BZD overdose |
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| omega1 vs omega2 vs omega3 |
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omega1 - induces and maintains sleep
omega2&3 - associated with peripheral benzo effects aka anxiolytic, anticonvulsant, muscle relaxation, ADRs, addiction |
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Why Can Progabide get into the CNS?
Neutral end group and highly liophilic terminal groups on the other end. Hydrolyzed in CNS and delviered to site of action. |
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Traditional Benzo Structure
SAR:
Pharmacophore + 5-phenyl group
EWG on R7
R1 has alkyl or part of ring
R3 has H or OH (OH shorter acting)
R2 is an H, F, or Cl
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SAR:
Pharmacophore + 5-phenyl group
EWG on R7
R1 has alkyl or part of ring
R3 has H or OH (OH shorter acting)
R2 is an H, F, or Cl |
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Diazepam
Benzodiazepine-2-one |
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General Imiazaol- Structured Benzodiazepine
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Thiopental....
barbituate "like" but typically used in anaesthesia and pain management |
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Methyprylon
"mispelled in the notes as methylprylon" |
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