med chem

Question 1

what is the rationale for giving levodopa

Answer 1

actively transported into the brain by large neutral amino acid transporter - dopa decarboxylase removes carboxylic acid and turns it into dopamine

Question 2

why would you administer levodopa with a dopa decarboxylase inhibitor

Answer 2

reduce the degradation of ldopa to dopamine in the peripheral - more in CNS, lower dose required and less s/e

Question 3

SAR of dopa decarboxylase inhibitor

Answer 3

must be polar
must have a hydralazine group

Question 4

how do MAO inhibitors work

Answer 4

form covalent bond with flavin co-factor
polar nucleophilic mechanism
attack of flavin carbonyl - elimination

Question 5

SAR of fluoxetine

Answer 5

secondary amide
EWG para on ring - SNRI
ortho substituent - NRI
para and ortho - SNRI

Question 6

what is the SAR of phenothiazines

Answer 6

tertiary nitrogen para on B ring essential
on subst on A ring can be at point 3 - EWG
only 3C and no branching on tertiary amine
after 3c chain - tertiary amine better than secondary - fatty acid here gives depot

Question 7

SAR for butyrophenones

Answer 7

F on benzene increases activity
=o essential
3c only and no branching
tertiary nitrogen essential

Question 8

citalopram SAR