Glossary of Med Chem Exam Adrenergic

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

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