Glossary of Med Chem Exam Adrenergic
Other Decks By This User
- 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)
- 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
- 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
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
You must Login or Register to add cards