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PT2 Neuro 1-5 > med chem > Flashcards

Flashcards in med chem Deck (17)
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1
Q

drugs with 3 ring structure and urea like carbonyl

A

carbamazepine
oxcarbazepine
eslicarbazepine

2
Q

drugs with amino acid backbone and alkane group

A

gabapentin

pregabalin

3
Q

what gives Na ion channels voltage gated activity

A

helix 4

4
Q

what amino acids make up the pore in K channels

A

G-Y-G

5
Q

what amino acids make up the pore in Ca channels

A

glutamate

6
Q

what amino acids make up the pore in Na channels

A

several, lots of variation

7
Q

factors that determine ion channels selectivity

A
  1. metal ion coordination number
  2. ligand strenght
  3. pore size, rigidity, and solvent exposure
8
Q

metal ion coordination number

A

number of donor atoms attached (in our case usually water)

9
Q

drug with linker region and its importance

A

tiagabine (GABA uptake inhibitor)

-interacts with positive region of transporter, more electronegative linker the better it binds

10
Q

drug that irreversibly binds to GABA aminotransferase

A

vigabatrin

11
Q

pregabalin original design

A

to inhibit GABA aminotransferase, then thought to agonize GAD

12
Q

pregabalin function for antiseizure activity

A

binds voltage gated Ca channels and prevents glutamate release

13
Q

phase I metabolism reactions

A

oxidation, hydrolysis

14
Q

phase 2 metabolism reactions

A

conjugation to make it more polar (sulfaiton, glucuronidation, ubiquitination, etc)

15
Q

perampanel MoA

A

noncompetitive AMPA antagonist

16
Q

ex vivo experiments for perampanel

A

removed cortical neurons from rats and used them to determine effects of perampanel on AMPA receptors

17
Q

in vivo experiments for perampanel

A

induced seizures in rats and tested effects of perampanel