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68 Cards in this Set
- Front
- Back
Norepinephrine is the NT of the _______ sympathetic neurons.
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postganglionic
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T/F: Epi is released from at the synaptic cleft.
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False, epi is not released at the synaptic cleft.
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The adrenal medulla releases what two neurohormones?
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Epi and NE
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At physiologic pH NE and Epi exist in the anionic, cationis, or molecular form?
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cationic
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How are catecholamines stabilized?
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By adding antioxidants like ascorbic acid.
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What does catechol oxidize in to?
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Ortho-quinone leading to colored products.
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What is the regulatory step in the biosynthesis of NE and Epi?
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The hydrolysis of L-Tyrosine into L-Dihudroxy phenylalanine(L-Dopa) by TYROSINE HYDROLASE.
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What is biosynthesized in the neuron, Epi, NE, or DOPA?
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NE
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Describe the condition:
Pheochromocytoma |
A benign tumor/cancer in the adrenal medulla that increases the concentration of NE in the body.
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Does the R or S enantiomer of NE and Epi posess biological activity?
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The R-enantiomer
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What are the two substituents that make a benzene ring a catechol?
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Two Hydroxy grps
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Catechols can be stabilized by adding antioxidants such as...
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Vit c/ ascorbic acid, and sodium metabisulfite.
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L-Tyrosine is biosynthesized to what in the neuron?
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L-Dopa leading to Dopa and finally NE. Epi is converted fron NE in the adrenal medulla.
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S-Adenosyl methionine donates what grp to make NE into Epi?
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A methyl grp
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Tyorsine hydroxylase is regulated by high concentration of ....?
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Epi, Dopa, NE. It is also regulated by phosphorylation/dephosphorylization where the phosphorylated enzyme is active.
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S-adenosyl methionine is called what when without a methyl grp?
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s-adenosyl homocysteine.
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What does MAO stand for?
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Monoamine oxidase
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COMT
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catechol O-methyl tranferase
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Name are the receptors on the post synaptic neuron.
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alpha1, beta1, and beta2
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Describe the responsibility of Alpha 2 receptors on presynaptic neurons.
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It modulates the quantity of NE in the synaptic cleft.
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Name the transmembrane domains and what type of interaction/binding is provided in each.
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TMD(V)-H-bonding with the catecholamine
TMD(VI)-hydrophobic interaction with aromatic ring TMD(III)- inonic interaction with NE |
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Beta adrenoceptors are able to accommodate _______sidechains? (size)
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Bulky.
B1: Isoproterenol>Epi=NE B2: Isoproterenol>Epi>NE |
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Give brand names:Nadolol, Pindolol, Timolol, Sotalol.
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Corgard, Visken, Blocardren/Timoptic, Betapace.
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Give the Generic name: Adrenalin, Noradrenalin, Neo-Synephrine, Aramine
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Epinephrine, NE, Phenylephrine HCl,Metaraminol Bitartrate.
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Give brand name: Clonidine, Metaproterenol sulfate, Isoproterenol, terbutaline sulfate.
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Catapres, Alupent, Isuprel, Brethine.
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Give generic name: Proventil, Serevent, Yutopar, Dobutrex.
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Albuterol, Salmeterol, Ritodrine, Dobutamine HCl
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Give the Generic name: Adrenalin, Noradrenalin, Neo-Synephrine, Aramine
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Epinephrine, NE, Phenylephrine HCl,Metaraminol Bitartrate.
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Give brand name: Clonidine, Metaproterenol sulfate, Isoproterenol, terbutaline sulfate.
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Catapres, Alupent, Isuprel, Brethine.
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Give generic name: Proventil, Serevent, Yutopar, Dobutrex.
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Albuterol, Salmeterol, Ritodrine, Dobutamine HCl
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Name the catecholamines that are endogenous to the body.
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NE, Dopa, and Epi
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All receptors are composed of a ____________ that is transmembrane and coupled with G-proteins.
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A 7-unit helical strucutre
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T or F: All Beta recptors are coupled to Gs protein which stimulates AC.
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True
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T or F: Alpha 2 recpetora are coupled to Gi protein rectors which inhibits AC.
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True
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T or F: Alpha 1 receptors are coupled to Gq protein which inhibits PLC.
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Flase. Alpha 1 receptors are coupled to Gq proteins which stimulates PLC
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Where are the beta 1 receptor subtypes located?
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heart and kidney
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What receptor subtype is responsible for constriction in the eye, contraction of the uterus, and decreased GI motility?
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alpha 1
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What are the responsibilites of beta 2 receptors in the liver, intestine, and uterus?
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liver- increase gluconeogenesis/glycogenolysis
intestine- decrease GI motility Uterus- relaxation |
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What receptor subtype is under investigation for association with obesity?
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beta 3
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WHat drug inhibits the storage of NE?
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Reserpine(Serpasil)
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Metyrosine is the analog of what amino acid?
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Tyrosine
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What drug reduces the biosynthesis of Epi/NE?
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Metyrosine(Demser)
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_____ acts as a competitive inhibitor of tyrosine hydroxylase.
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Demser(Metyrosine)
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Name two drugs that inhibit release of NE and the functional grp they have in common.
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Guaethidine and Guanadrel. They both contain guanine.
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Arenergic agonists aka
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sympathomimetics
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For high agonist effect the OH grps should be in what positions?
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Meta and para
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T of F: The OH grp beta to the amine with S-absolute config is active.
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False. R-absolute config.
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T of F the bulkier the subtitution on N the more Beta selective.
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True
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Substitution on what carbon reduces affinity of both alpha and beta receptors?
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Alpha carbon substitution.
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For COMT to metabolize something it must have what structure?
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Catechol structure
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A compound should have what stereochemistry to have high agonist activity?
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1R(beta carbon), 2S (alpha carbon)
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What is the difference between Imidazole and imidazoladine?
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Imidizole has unsaturated Carbons(double bonds) while imidazoladine has totally saturated Carbons(no double bonds)
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Imidazoline and derivatives are selctive for what receptors?
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alpha receptors
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Can catecholamines be given orally?
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No b/c highly hydrophilic, light sensitive, and easily oxidized.
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Dopa can be given in low doses to increase Bld flow to the kidneys w/o doing what to the heart?
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W/o increasing haert rate.
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In moderate doses Dopa can increase cardiac output w/o producing peripheral ______?
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vasoconstriction
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What are the uses of Epi?
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1. tmt of hypotensive crisis
2. stimulate heart in cardiac arrest 3.nasal decongestant and bronchodilator 4.aphylactic shock 5.tmt of open angle glaucoma |
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Draw the structure of guanidine.
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look on page 11 in book.
(CN3H5) |
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What receptor is located in the eye, liver, intestine, uterus, and peripheral vasculature?
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alpha 1
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T or F: 75% of NE is recovered by Uptake-1.
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False 95% is recovered
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What type of sympathetic drugs lower blood pressure?
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B blockers, alpha 1 antagonists( alpha 2 receptors lower high BP but there is no specific drug for it)
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Give brand name:
Ritodrine |
Yutopar
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Proventil
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Albuterol
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Salmeterol
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Serevent
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Neo-Synephrine
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Phenylephedrine
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Clonidin
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Catapres
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Terbutaline
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Brethine
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Afrinol
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Pseudoephedrine
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Define aura which is associated with migranes.
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Positive aura -> blinding lights
negativeaura-> blind spots |