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30 Cards in this Set
- Front
- Back
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____ extracts tyrosine from the food we eat and sends it to the kidney, where epi is made
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Liver
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When norepi is metabolized by MAO, you lose the _____ and the carbon is ____
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Amine; oxidized
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Norepi metabolism by MAO makes an:
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Inactive metabolite
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Norepi metabolism by COMT makes an:
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Active but weak metabolite
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When norepi is metabolized by COMT, a ______ is place on the ______ position at C 3
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Methyl group; meta
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Beta 1,2,3 are positively coupled to:
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AC
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Beta 1,2,3 activation leads to ______ and production of cAMP
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Coupling with AC
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Alpha 1ABD are all on _____ receptors
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Post synaptic
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Alpha 2ABD are ________ receptors
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Pre synaptic
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Coupled with PLC
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Alpha 1a,b,d
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Stimulation of Alpha 1 ABD --> coupling with zpLC and production of second messengers:
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IP3, DAG, Ca++
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Stimulation of Alpha 2 ABD --> coupling negatively with ______ and decrease production of _______________
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AC; cAMP
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In physiologic pH, amines are ______
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Protonated (+ charge)
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Amines need ______ to have ionic interactions
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AA
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On TM3, for adrenergic receptors to be activated, must have _______ for ionic bond
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Aspartic acid
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Most potent in alpha activity
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Norepi
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Least potent in alpha activity
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Isoproterenol
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Most potent in Beta activity
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Isoproterenol
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Least potent in Beta activity
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Norepi
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Small unsubstituted amine prefer to activate tissues with ________ receptors
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Alpha
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If you increase the bulk/branch on the terminal amine, you are picking up ______ activity
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Beta
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______ receptor does not have a big pocket to be able to fit the bulky substituents
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Alpha
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Norepi: if you remove the _______ at the Beta C, you have only the ethylene bridge and you are decreasing activity
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Hydroxyl
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If you put a methoxy or methyl group on the ______ then you decrease activity by 20-40 times
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Norepi beta C
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Beta C substitution can lead to:
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R>S
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Norepi: ____ isomer is less potent,k but this is stereoselectivity, they will both produce some effect
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S
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Primary amine on norepi means:
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Alpha and beta effects
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Secondary amine on norepi means:
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Beta more than alpha effects
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Norepi: Methyl or ethyl placed on alpha C is tolerated but
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Slows metabolism by MAO
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An ethyl group on alpha C will change the selectivity to:
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Beta receptors
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