med chem

Question 1

drugs with 3 ring structure and urea like carbonyl

Answer 1

carbamazepine
oxcarbazepine
eslicarbazepine

Question 2

drugs with amino acid backbone and alkane group

Answer 2

gabapentin

pregabalin

Question 3

what gives Na ion channels voltage gated activity

Answer 3

helix 4

Question 4

what amino acids make up the pore in K channels

Answer 4

G-Y-G

Question 5

what amino acids make up the pore in Ca channels

Answer 5

glutamate

Question 6

what amino acids make up the pore in Na channels

Answer 6

several, lots of variation

Question 7

factors that determine ion channels selectivity

Answer 7

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

Question 8

metal ion coordination number

Answer 8

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

Question 9

drug with linker region and its importance

Answer 9

tiagabine (GABA uptake inhibitor)

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

Question 10

drug that irreversibly binds to GABA aminotransferase

Answer 10

vigabatrin

Question 11

pregabalin original design

Answer 11

to inhibit GABA aminotransferase, then thought to agonize GAD

Question 12

pregabalin function for antiseizure activity

Answer 12

binds voltage gated Ca channels and prevents glutamate release

Question 13

phase I metabolism reactions

Answer 13

oxidation, hydrolysis

Question 14

phase 2 metabolism reactions

Answer 14

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

Question 15

perampanel MoA

Answer 15

noncompetitive AMPA antagonist

Question 16

ex vivo experiments for perampanel

Answer 16

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

Question 17

in vivo experiments for perampanel

Answer 17

induced seizures in rats and tested effects of perampanel