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45 Cards in this Set

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Mechanism of tyrosine hydroxylase
hydroxylates tyrosine @ 3'
Mechanism of dopamine B-hydroxylase
put OH on carbon1 in B configuration
After NE binds to alpha/beta adrenergic receptor what happens
G-protein produces biochemical cascade
4 fates of NE once it is in the synapse
1)bind to alpha2 receptor
2)bind to alpha/beta receptor on effector cell
3)reuptake
4)diffusion/metabolism
NE
What is this?
tyrosine
What is this?
L-dopa
What is this?
dopamine
What is this?
Adrenergic Drug types (SAR's of the drugs) (4)
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)
Bigger groups @ R1 = higher affinity at Beta receptors, the biggest groups give affinity to Beta2 receptors
As the substituent at R1 increases in size what happens?
Beta receptor affinity is better than alpha receptor affinity

B/c it creates a chiral carbon that creates diastereomers w/ different activities
As the groups at R2 increase in size what happens? AND why is it bad to mess with R2?
If you do modify @ the R2 position which isomer has more activity and what is the name/activity of this compound?
1R,2S or 1S,2R (erythro)

ephedrine, partial agonist and indirect agonist for NE
an OH in R configuration
Maximal direct agonist activity is found when C-1 has what?
3'-5' dihydroxy b/c it is no longer a catecholamine and therefore resistant to COMT/first pass metabolism
Which is better and why?
A 3'-4' dihydroxy or a 3'-5' dihydroxy?
beta-2 receptors
3'-5' dihydroxy is selective for...
just have one OH, at 3'-OH
In order for an agonist to have just alpha receptor activity it must...
ONE OH at 4'
In order for an agonist to have just beta-receptor activity what must the substitution be @ R3
Have NO OH, a 2' OH or a 5' OH
How do you get mixed activity for an agonist if you do an R3 substitution?
3 direct acting phenylethanolamine agonists
1)NE
2)E
3)phenylephrine
4 indirect acting sympathomimetics (for phenylethanolamine)
1)ephedrine
2)pseudoephedrine
3)phenylpropanolamine
4)amphetamine
What type of receiever accepts imitations more easily alpha or beta recievers?
BETA
Imidazoline agonists
a)for alpha1
b)for alpha2
a)naphazoline, tetrahydrozline
b)clonidine
Alpha Adrenergic antagonists (3)
1)phenoxybenzamine
2)tolazoline (imidazoline drug)
3)phentolamine (imidazoline drug)
SELECTIVE alpha1 antagonists
quinazoline derivatives
Quinazoline derivatives (characteristics) (3)
1)quinazoline ring system
2)piperazine ring system
3)rest of structure imparts solubility/half-life
Naphazoline
What is it?
Clonidine
What is it?
Tolazoline
What is it?
Phentolamine
What is it?
Beta antagonists
a)1st one
b)others
a)aryloxypropanolamines (propanolol)
b)4-substituted phenyloxypropanolamines (practolol, metoprolol)
Metoprolol is selective for ___ and why?
Beta1, b/c has group in para position
How do propanolamines act as beta antagonists?
have OCH2 added to ring to incr length of side chain making it so that it can NOT bind to Asp in AS
Quinazoline derivative, the piperazine ring (ring in middle w/ no double bonds and N's on its ends)
What category is this drug in and what is it's most special feature
3 quinazoline derivative drugs
1)prazosin
2)terazosin
3)doxazosin
propanololamines
What category of drug is this in?
2 enzymes in the NE synthesis pathway that are not targeted by drugs to inhibit?
1)dopamine B-hydroxylase
2)phenylethanolamine N-methyltransferase
Drugs affecting NE/E biosynthesis do what?
1)inhibit tyrosine hydroxylase
2)inhibit aromatic L-AA decarboxylase
Drug that inhibits tyrosine hydroxylase and its use
Metyrosine, inhibits catecholamine production when tumors in adrenal medulla
Drug that inhibits aromatic L-AA decarboxylase and its use
Carbidopa, keeps L-dopa around to decrease parkinson's symptoms
Drugs affecting storage vesicles (3)
1)reserpine
2)bretylium
3)guanethidine
Major structural classes in adrenergic agents and their overall fxn of 3 of em
1)Aryloxypropanolamines (beta-blockers)
2)guianidine derivatives
3)imidazoline derivatives (alpha agonists)
4)phenylethanolamine derivatives
5)phenylethylamine derivatives
6)quinazoline derivatives (alpha1 antagonists)
If the 4' on a aryloxypropanolamines is substituted what does it do?
makes it selective for Beta1
If you see "oxy" in a structures name what category is it most likely?
BETA BLOCKER
Where is sympathetic tone dominant? (4) and effect of ganglionic blockade
1)arterioles (vasodilation)
2)veins (dilation, pooling, decr cardiac output)
3)sweat glands (anhidrosis)
4)genital tract (impotence)
Where is parasympathetic tone dominant? (7) and effect of ganglionic blockade
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)