[5] Adrenergic Receptors Flashcards
Rate Limiting Step of Norepinephrine
Tyrosine Hydroxylase
Tyrosine -> DOPA
Receptors prolific in smooth muscles and blood vessels
Alpha-1
Postsynaptic effector mostly found in the heart
Beta-1
Postsynaptic effector cells especially in smooth muscles
Beta-2
Postsynaptic effector cells especially in lipocytes
Beta-3
Which has a methyl group? Epinephrine or Norepinephrine?
Epinephrine
because
NO-repinephrine
Subtypes of Beta-1 Receptors
Heart
Juxtaglomerular cell
Subtypes of Beta-2Receptors
Respiratory, uterine, and vascular smooth muscle
Skeletal Muscle
Human Liver
Function: Activation of Beta-2 in Respiratory Tissue
Smooth muscle relaxation
Function: Activation of Beta-2 in Skeletal Muscle
Potassium Uptake
Function: Activation of Beta-2 in the Liver
Activates glycogenolysis
Function: Activation of Beta-3 Receptors
Increased lipolysis
Receptor Specificity is ____ but not _____?
Relative, but not absolute
Parent Compound of Adrenergic Agents
Phenylethylamine
Effect: Increased size of alkyl substituents on Amino Group
Increased beta-receptor activity
Decreased alpha-receptor activity
A lower Kd value would mean?
Higher potency
Effect: Decreased substitution of benzene ring
Increased bioavailability and prolongs duration of action
Since they are not catecholamines, they are spared from COMT Inactivation in the Gut and Liver
Effect: Substitution on the Alpha Carbon
Prolonged action of drugs especially in noncatecholamines