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30 Cards in this Set
- Front
- Back
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What amino acid is NE derived from?
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Tyrosine!
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What decarboxylase cofactor is associated with NE biosynthesis?
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PLP
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What enzyme provides a major route of regulation/degradation for NE?
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MAO (monoamine oxidase)
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Is the following enzyme associated with biosynthesis or degradation of NE?
MAO (monoamine oxidase) |
Degradation
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Is the following enzyme associated with biosynthesis or degradation of NE?
COMT (catechol-O-methyltranserase) |
Degradation
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Are the following enzymes associated with biosynthesis or degradation of NE?
aldehyde reductase, aldehyde dehydrogenase |
Degradation
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Is the following enzyme associated with biosynthesis or degradation of NE?
Tyrosine hydroxylase |
Biosynthesis
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Is the following enzyme associated with biosynthesis or degradation of NE?
Dopamine beta-hydroxylase |
Biosynthesis
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Which type of agonist is used as a bronchodilater and to treat glaucoma?
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beta-2
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Which type of agonist is used for treatment of hypertension, glaucoma, analgesia and used as a sedative?
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alpha-2
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Which type of antagonist is used for treatment of hypertension and benign prostate hyperplasia?
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alpha-1
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Which type of antagonist is used to treat hypertension and arrythmias?
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beta-1 (beta blockers)
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Where are alpha-1 receptors found and what do they stimulate?
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Vascular smooth muscle; stimulate IP3 via Gq protein coupled receptor
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Where are alpha-2 receptors found?
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Found on vascular smooth muscle, sympathetic nerve terminals and pre-synaptic neurons
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Where are beta-1 receptors found and what do they stimulate?
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Cardiac nodal tissue, conducting system and contracting myoctyes; they stimulate contraction via a G-protein coupled receptor
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Where are beta-2 receptors found?
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Cardiac nodal tissue, conducting system and contracting myoctyes as well as vascular smooth muscle
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Why was colterol a poor drug candidate?
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It had poor bioavailability because the catechol group was rapidly metabolized via COMT and sulfotransferases.
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What structure makes a beta blocker a beta blocker (i.e. confers beta-1 specificity)?
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A single phenol ring with a para substitution
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What important intermediate do beta-haloalkylamines form?
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Aziridinium ion
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True or False: Beta-haloalkylamines react with receptors via a covalent mechanism.
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True
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What type of receptor do beta-haloalkylamines act on? Do they act as agonists or antagonists?
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Adrenergic receptors (non-selective); antagonists
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What types of substances do beta-haloalkylamines block?
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Primarily NE, but also acetylcholine, histamine and seratonin (acts as an irreversible antagonist on all of these)
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What other effect do beta-haloalkylamines have other than blocking receptors?
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They can lead to downstream protein degredation by proteasome.
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True or false: imidazolines only form covalent actions.
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False; non-covalent interactions only (and thus reversible)
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What physiologic responses do imidazolines produce?
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Vasodilation and reflex tachydardia; may promote release of NE
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Which alpha receptor are imidazolines specific for?
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Neither (trick question!)
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Why is the half-life of prazosin shorter than that of terazosin and doxazosin?
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Prazosin has a more electron rich-structure and thus is better substrate for metabolizing enzymes.
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Which receptor are the quinazolines specific for? Are they agonists or antagonists?
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alpha-1 antagonists
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Which receptor are the Ergot alkaloids specific for? Are they agonists or antagonists?
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alpha (non-specific) antagonists
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What is methylsergide used for?
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To treat migraines.
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