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Med Chem Adrenergic
SARs and receptors for medicinal chemistry of adrenergic drugs
57
Medical
Professional
02/02/2011

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Term
COMT Substrate and reaction
Definition
OH on catechol (benzene with two OH) --> OH gets turned into O-CH3
Term
MAO substrate and reaction
Definition
Primary amine --> aldehyde
Term
Aldehyde dehydrognease substrate and reaction
Definition
Aldehyde --> carboxylic acid
Term
Reaction of catecholamine + light
Definition
Oh on catechol (benzene with two OH) become carbonyl (double bond O)
Term
alpha 1 agonists indication
Definition
shock, hypotension, nasal decongestant
Term
alpha 2 antagonist indication
Definition
None
Term
alpha 2 agonist indication
Definition
antihypertensives, glaucoma, analgesia, sedatives
Term
alpha 1 antagonist indication
Definition
antihypertensives, BPH
Term
Beta 1 antagonist indication
Definition
antihypertensives, antiarrhythmics
Term
beta 2 antagonists indication
Definition
none
Term
Beta 1 agonist indication
Definition
none
Term
beta 2 agonists indication
Definition
bronchodilators, glaucoma
Term
beta 3 agonists indication
Definition
weight loss (investigational)
Term
beta 3 antagoists indication
Definition
none
Term
Phenylepherine receptor
Definition
alpha 1 agonist
Term
metaraminol receptor
Definition
alpha 1 agonist
Term
terbutaline receptor
Definition
beta 2 agonist
Term
metaproterenol receptor
Definition
beta 2 agonist
Term
albuterol receptor
Definition
beta 2 agonist
Term
pirbuterol receptor
Definition
beta 2 agonist
Term
biloterol receptor
Definition
beta 2 agonist
Term
salmeterol receptor
Definition
beta 2 agonist
Term
oxymetazoline receptor
Definition
alpha 1 agonist
Term
tetrahydrozoline receptor
Definition
alpha 1 agonist
Term
clonidine receptor
Definition
alpha 2 agonist
Term
guanabenz receptor
Definition
alpha 2 agonist
Term
guanfacine receptor
Definition
alpha 2 agonist
Term
phenylpropanoloamine receptor
Definition
indirect adrenergic agonist
Term
pseudoephedrine receptor
Definition
indirect adrenergic agonist
Term
ephedrine receptor
Definition
indirect adrenergic agonist
Term
amphetamine + dextramphetamine receptor
Definition
indirect adrenergic agonist
Term
methamphetamine receptor
Definition
indirect adrenergic agonist
Term
methylphenidate receptor
Definition
indirect adrenergic agonist
Term
dexmethyphenidate receptor
Definition
indirect adrenergic agonist
Term
phenoxybenzamine receptor
Definition
non-selective alpha antagonist
Term
tolazoline antagonist receptor
Definition
non-selective alpha antagonist
Term
phentolamine receptor
Definition
non-selective alpha antagonist
Term
Prazosin receptor
Definition
selective alpha 1 antagonist
Term
Doxasosin receptor
Definition
selective alpha 1 antagonist
Term
Yohimbine receptor
Definition
selective alpha 2 antagonist
Term
propranolol receptor
Definition
non-selective beta antagonist
Term
pindolol receptor
Definition
non-selective beta antagonist
Term
timolol receptor
Definition
non-selective beta antagonist
Term
carteolol receptor
Definition
non-selective beta antagonist
Term
nadolol receptor
Definition
non-selective beta antagonist
Term
sotalol receptor
Definition
non-selective beta antagonist
Term
metoprolol receptor
Definition
selective beta 2 antagonist
Term
acebutolol receptor
Definition
selective beta 2 antagonist
Term
atenolol receptor
Definition
selective beta 2 antagonist
Term
bisoprolol receptor
Definition
selective beta 2 antagonist
Term
esmolol receptor
Definition
selective beta 2 antagonist
Term
labetolol receptor
Definition
mixed antagonist
Term
carvedilol receptor
Definition
mixed antagonist
Term

[image]

Effect of Changing R1 is?

Definition
Increasing size lowers alpha 1 activity. Bigger than butyl blocks alpha 1 comletely

Big and bulky groups make beta 2 selective. Very long groups make it long acting (salmeterol)
Term

[image]

Effect of changing R2?

Definition
Small R2 (methyl or ethyl) allows for alpha 1 selectivity.
For Beta selectivity, R2 MUST be H
Term
Definition
3' Hydroxy = alpha selectivity
MUST BE 3' hydroxy for alpha
3', 5' hydroxy = beta 2 selectivity
3', 4' methylhydroxy = beta
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