Med Chem of Adrenergics
Order by
11 terms
Terms | Definitions |
|---|---|
 α₁-agonist & α₂-partial agonist |  contains imidazoline ring tetrahydrozoline, oxymetazoline |
| selective α₁-agonist |  1. missing 4-OH = no COMT 2. alpha methyl slows metab phenylephrine, metaraminol |
| selective α₂-agonist |  1. phenethylamine-like 2. imidazoline ring/mimic 3. ortho EWG (chlorine) "guano is alpha's number 2" clonidine, guanabenz, guanfacine |
| selective α₁-antagonist |  1. phenethylamine-like 2. dimethoxy-phenyl-piperazine core 3. furan/tetrahydrofuran ring for solubility Ix: BPH "let my blocked A1 pipe flow w/ piperazine ring" terazosin, tamsulosin, doxazosin, prazosin |
| nonselective α-antagonist |  1. imidazoline ring w/o substitutions 2. bulk + chain + charge *tolazoline = only antagonist smaller than the agonist phentolamine, tolazoline, phenoxybenzamine |
| mixed/indirect adrenergic agonist |  1. MIXED = no hydroxyls on benzene 2. INDIRECT = no hydroxyls on benzene & no β-OH amphetamine, methamphetamine, lisdexamfetamine, phenylpropanolamine, ephedrine, pseudoephedrine, methylphenidate, dexmethylphenidate |
| nonselective β-antagonist |  1. aryloxypropanolamine (may have fused ring core) 2. β-OH 3. no p-H-bonding acceptor "selective BB start with vowels, except meto & biso" "cart ace pin pen have ISA" propranolol, pindolol, cartelol, nadolol, sotalol, timolol |
| selective β₁-antagonist |  1. aryloxypropanolamine 2. β-OH 3. p-H-bonding acceptor distant from ring *nebivolol = symmetrical, F on each ring, vasodilation acebutolol, bisoprolol, metoprolol, atenolol, esmolol |
| nonselective β-antagonist w/ α-blocking activity |  1. arylalkyl group as N-substitution = α-affinity 2. aryl substitutions do not stim ISA S,R isomer = α₁-blocker R,R = β₁/β₂/α₁-blocker labetolol, carvedilol |
| peripherial D₁-agonist w/ α₂-agonism |  two phenethylamine-like groups fenoldopam Ix: emergency HTN crisis, no renal dosing |
| selective β₂-agonist |  1. phenethylamine 2. β-OH 3. larger N-substitution = greater β affinity 4. more lipophilic & bulky the substitution = greater β₂ affinity terbutaline, albuterol, pirbuterol, metaproterenol, salmeterol |
First Time Here?
Welcome to Quizlet, a fun, free place to study. Try these flashcards, find others to study, or make your own.