Pda2 Test 2 Set 3

Front 1

Mechanism of tyrosine hydroxylase

Back 1

hydroxylates tyrosine @ 3'

Front 2

Mechanism of dopamine B-hydroxylase

Back 2

put OH on carbon1 in B configuration

Front 3

After NE binds to alpha/beta adrenergic receptor what happens

Back 3

G-protein produces biochemical cascade

Front 4

4 fates of NE once it is in the synapse

Back 4

1)bind to alpha2 receptor
2)bind to alpha/beta receptor on effector cell
3)reuptake
4)diffusion/metabolism

Front 5

NE

Back 5

What is this?

Front 6

tyrosine

Back 6

What is this?

Front 7

L-dopa

Back 7

What is this?

Front 8

dopamine

Back 8

What is this?

Front 9

Adrenergic Drug types (SAR's of the drugs) (4)

Back 9

1)agonist/antagonists (act directly on receptor)
2)affect storage and release from vesicles
3)affect NE biosynthesis (enzyme inhibitors)
4)affect reuptake and catabolism (enzyme inhibitors)

Front 10

Bigger groups @ R1 = higher affinity at Beta receptors, the biggest groups give affinity to Beta2 receptors

Back 10

As the substituent at R1 increases in size what happens?

Front 11

Beta receptor affinity is better than alpha receptor affinity

B/c it creates a chiral carbon that creates diastereomers w/ different activities

Back 11

As the groups at R2 increase in size what happens? AND why is it bad to mess with R2?

Front 12

If you do modify @ the R2 position which isomer has more activity and what is the name/activity of this compound?

Back 12

1R,2S or 1S,2R (erythro)

ephedrine, partial agonist and indirect agonist for NE

Front 13

an OH in R configuration

Back 13

Maximal direct agonist activity is found when C-1 has what?

Front 14

3'-5' dihydroxy b/c it is no longer a catecholamine and therefore resistant to COMT/first pass metabolism

Back 14

Which is better and why?
A 3'-4' dihydroxy or a 3'-5' dihydroxy?

Front 15

beta-2 receptors

Back 15

3'-5' dihydroxy is selective for...

Front 16

just have one OH, at 3'-OH

Back 16

In order for an agonist to have just alpha receptor activity it must...

Front 17

ONE OH at 4'

Back 17

In order for an agonist to have just beta-receptor activity what must the substitution be @ R3

Front 18

Have NO OH, a 2' OH or a 5' OH

Back 18

How do you get mixed activity for an agonist if you do an R3 substitution?

Front 19

3 direct acting phenylethanolamine agonists

Back 19

1)NE
2)E
3)phenylephrine

Front 20

4 indirect acting sympathomimetics (for phenylethanolamine)

Back 20

1)ephedrine
2)pseudoephedrine
3)phenylpropanolamine
4)amphetamine

Front 21

What type of receiever accepts imitations more easily alpha or beta recievers?

Back 21

BETA

Front 22

Imidazoline agonists
a)for alpha1
b)for alpha2

Back 22

a)naphazoline, tetrahydrozline
b)clonidine

Front 23

Alpha Adrenergic antagonists (3)

Back 23

1)phenoxybenzamine
2)tolazoline (imidazoline drug)
3)phentolamine (imidazoline drug)

Front 24

SELECTIVE alpha1 antagonists

Back 24

quinazoline derivatives

Front 25

Quinazoline derivatives (characteristics) (3)

Back 25

1)quinazoline ring system
2)piperazine ring system
3)rest of structure imparts solubility/half-life

Front 26

Naphazoline

Back 26

What is it?

Front 27

Clonidine

Back 27

What is it?

Front 28

Tolazoline

Back 28

What is it?

Front 29

Phentolamine

Back 29

What is it?

Front 30

Beta antagonists
a)1st one
b)others

Back 30

a)aryloxypropanolamines (propanolol)
b)4-substituted phenyloxypropanolamines (practolol, metoprolol)

Front 31

Metoprolol is selective for ___ and why?

Back 31

Beta1, b/c has group in para position

Front 32

How do propanolamines act as beta antagonists?

Back 32

have OCH2 added to ring to incr length of side chain making it so that it can NOT bind to Asp in AS

Front 33

Quinazoline derivative, the piperazine ring (ring in middle w/ no double bonds and N's on its ends)

Back 33

What category is this drug in and what is it's most special feature

Front 34

3 quinazoline derivative drugs

Back 34

1)prazosin
2)terazosin
3)doxazosin

Front 35

propanololamines

Back 35

What category of drug is this in?

Front 36

2 enzymes in the NE synthesis pathway that are not targeted by drugs to inhibit?

Back 36

1)dopamine B-hydroxylase
2)phenylethanolamine N-methyltransferase

Front 37

Drugs affecting NE/E biosynthesis do what?

Back 37

1)inhibit tyrosine hydroxylase
2)inhibit aromatic L-AA decarboxylase

Front 38

Drug that inhibits tyrosine hydroxylase and its use

Back 38

Metyrosine, inhibits catecholamine production when tumors in adrenal medulla

Front 39

Drug that inhibits aromatic L-AA decarboxylase and its use

Back 39

Carbidopa, keeps L-dopa around to decrease parkinson's symptoms

Front 40

Drugs affecting storage vesicles (3)

Back 40

1)reserpine
2)bretylium
3)guanethidine

Front 41

Major structural classes in adrenergic agents and their overall fxn of 3 of em

Back 41

1)Aryloxypropanolamines (beta-blockers)
2)guianidine derivatives
3)imidazoline derivatives (alpha agonists)
4)phenylethanolamine derivatives
5)phenylethylamine derivatives
6)quinazoline derivatives (alpha1 antagonists)

Front 42

If the 4' on a aryloxypropanolamines is substituted what does it do?

Back 42

makes it selective for Beta1

Front 43

If you see "oxy" in a structures name what category is it most likely?

Back 43

BETA BLOCKER

Front 44

Where is sympathetic tone dominant? (4) and effect of ganglionic blockade

Back 44

1)arterioles (vasodilation)
2)veins (dilation, pooling, decr cardiac output)
3)sweat glands (anhidrosis)
4)genital tract (impotence)

Front 45

Where is parasympathetic tone dominant? (7) and effect of ganglionic blockade

Back 45

1)heart (tachycardia)
2)iris (mydriasis)
3)ciliary muscle (cycloplegia)
4)GI (reduced tone and motility)
5)urinary bladder (urinary retention)
6)salivary glands (xerostomia)
7)genital tract (impotence)