Adrenergic Agonist- T1 Flashcards
alpha1- adrenergic selective agonist
phenylephrine
alpha2- adrenergic selective agonist
- clonidine
- brimonidine
- tizanidine
- alpha-methyldopa
sympathomimetic amines (4)
- addy
- methylphen
- focalin
- vyvanse
alpha adrenergic (subtype non-selective)
- oxymetazoline–> afrin
- naphazoline–> visine
beta2- adrenergic selective agonist
- albuterol
- salmeterol–> advair
- Levalbuterol
sympathetic potency at alpha receptor
epi>norepi> isoproterenol
sympathetic potency at beta receptor
isoproterenol > epi > norepi
alpha receptors tend to
restrict
beta receptors tend to
relax, except at the heart where they constrict the cardiac muscle.
signal transduction for beta-adrenoceptor: beta receptors are coupled to…
adenylyl cyclase activation–> increase in cAMP helps to mediate cardiac cells
signal transduction for beta-adrenoceptor: alpha2 receptors are…
inhibitory on beta receptors if they are found in the same location. coupled to GI and tend to inhibit adenylyl cyclase synthesis. act like muscarinic M2 receptor which oppose beta receptors and slow HR by not allowing cAMP to be produced.
beta-adrenoceptor regulation of cardiac chronotropy (HR) and isotropy(contraction): PKA-
phosphorylates voltage-dependent Ca channel and the SR Ca-ATPase. calcium influx and depolarization which increases constriction and HR. Sarcoplasm Ca-ATPase increases calcium storage. Ca coming in from the outside is a trigger for Ca release from the SR.
beta-adrenoceptor regulation of smooth muscle relaxation. PKA phosphorylates
plasma membrane and Sr-Ca-ATPase to decrease inctracellular Ca.
signaling system for alpha1-adrenoceptor mediated effects
phosphoinositide hydrolysis and Ca mobilization. when you get more IP3, you get more Ca, which results in increase contraction.
mobilization of intracellular Ca in smooth muscle: contraction via activation of MLCK
ca released in sooth muscle binds to calmodulin and then the calmodulin activates MLCK.