CAS BI 315 Lecture Notes - Lecture 7: Vasoconstriction, Neurotransmitter, Adderall
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receptor | Agonist | antagonist | |
a1 | Norephinephrine | Phenylephrine | |
a2 | Phenoxybenzamine | Prazosin | |
B1 | Clonidine | Yohimbine | |
Norephinephrine | Propranolol | ||
Epinephrine | Metoprolol | ||
Isoproterenol | |||
Dobutamine | |||
B2 | Epinephrine | Proranolol | |
Norepinephrine | Butoxamine | ||
Isoproterenol | |||
Albuterol | |||
Nicotinic | Ach | Curare | |
Nicotine | |||
Hexamethonium | |||
Muscarinic | Ach | Atropine |
Assume all the chemicals in the table are available to you.
You are given a piece of smooth muscle tissue, you stimulate it with Norepinephrine and find the muscle responds with contractions. Your hypothesis is that the muscle contraction is caused by the activation of α1 adrenergic receptors. Now you need to design an experiment protocol to test your hypothesis.
Background knowledge: The figure below is an experiment setup, the red tissue in the organ bath is the smooth muscle tissues. In this kind of experiment smooth muscle tissue is minimally stretched vertically by two hooks or clips in the organ bath filled with physiological saline solution (PSS). Agonist is added to the PSS to challenge the muscle tissue, muscle contraction is sensed by a force transducer at the top and force is recorded by a computer. Adding antagonist before adding agonist blocks agonist action. PSS may or may not be changed, it depends on your purposes, e.g. if you want to block a type receptors, then you do not want change PSS after you add antagonist to the PSS. Your correct step is that you add antagonist to PSS, wait some time, and add agonist, you keep both antagonist and agonist in the PSS so that you can judge if the receptor blockage by antagonist abolish the agonist action.
The key to this assignment is that you eliminate possible cross-activities of agonists. Cross-activity means an agonist activate more than one types of receptors, you need block each type of the receptor in order to see what type of the receptor is activate to cause contraction. This muscle tissue can have both α and β receptor types and their subtypes, you need to demonstrate convincingly that you only stimulate α1 receptors.
Write an experimental protocol to demonstrate your work, for each step in the protocol you write the chemical(s) you add, why you add, what result you are expecting to see e.g. contract, relax, no response. If the step is to wash the tissue with fresh PSS, then you do not need to indicate the responses.
Here is an example of the answer.
step | chemical added | response |
1. | epinephrine, activate alpha and beta receptors, | blood vessel ring contract slightly. |
2. | wash with PSS | |
3. | alpha receptor antagonist and norepinerphine, block NE activating alpha receptor. | blood vessel ring should not contract. |
4. | wash with PSS | |
5. | ⦠| ⦠|
6. | ⦠| ⦠|
Discuss your protocol to show the relation between activation of α1 receptors and the vascular smooth muscle contraction.Design the experiemnt and its conclusion/ results.
Need help with biology questions:
1. To increase the excretion of an acidic drug, what would you do to the urine?
A. | Make it more basic | |
B. | None of the above | |
C. | Make it neutral | |
D. | Make it more acidic |
2. G-Protein coupled receptors directly act on which of the following secondary messenger molecules:
A. | cAMP | |
B. | ATP | |
C. | ADP | |
D. | GTP | |
E. | None of the above or more than one of the above |
3. Drug A and Drug B both produce the same level of biological/physiological response. Drug A produces this effect with 100 mg/kg dose. Drug B produces this effect with 50 mg/kg dose. Which of the following is true?:
A. | Drug B is more efficacious than Drug A. Both drugs are equally potent. | |
B. | Drug A is more efficacious than Drug B. Both drugs are equally potent. | |
C. | Drug A and B are equally efficacious. Drug A is more potent than Drug B. | |
D. | Drug A and B are equally efficacious. Drug B is more potent than Drug A. |
4. The stomach has a ______ pH, whereas the small intestines have a _______ pH. The colon has an approximately ___________ pH.
A. | High; low; neutral | |
B. | Low; high; neutral | |
C. | Low; neutral; neutral | |
D. | None of the above |
5. Which receptor is most likely to reduce norepinephrine levels when activated?
A. | alpha 2 adrenergic | |
B. | alpha 1 adrenergic | |
C. | dopamine D1 receptors |
6. Which of the following statements are FALSE?
A. | If the Vd of a drug is between 60 and 80 L the drug has likely distributed to the total body water of a 200 kg man. | |
B. | In the enterohepatic system the activity of bacteria to remove conjugates from a drug in the gut will decrease the clearance of the drug. | |
C. | Lipid drugs are more likely to be reabsorbed by the kidney from the urine. | |
D. | A weak basic drug (pKa = 6) will be mostly ionized in urine of a pH= 3 and only the non- ionized drug will be eliminated. | |
E. | The major conjugate in Phase 2 metabolism is glucuronide. |
7. Isoproterenol (β-agonist) is a vasodilator that increases HR. What happens to systolic and diastolic pressures upon IV administration of isoproterenol?
A. | â systolic; â diastolic | |
B. | â systolic; â diastolic | |
C. | â systolic; â diastolic | |
D. | â systolic; â diastolic | |
E. | None of the above |
8. If you want to increase the blood concentration of a drug A, you can perform which of the following procedures:
A. | Inhibit Drug A metabolism with Drug B | |
B. | Enhance Drug A reabsorption from renal proximal tubule by changing ionization of Drug A with Drug B | |
C. | Allow competition of Drug B with Drug A for active renal secretion processes | |
D. | Increase the binding of Drug A to serum albumin | |
E. | All of the above |
9. Which of the following describes Phase I metabolism?
A. | Inactive products are always produced in this phase. | |
B. | Large molecules such as glucuronic acid are conjugated to drugs in this phase. | |
C. | This phase may produce active metabolites from prodrugs. | |
D. | This phase only occurs in the liver. |
10. Which of the following is NOT an enzyme involved in the biosynthesis of biogenic amines?
A. | Phenylethanolamine N-methyl Transferase | |
B. | Dopamine β-hydroxylase | |
C. | Tyrosine dehydroxylase | |
D. | DOPA decarboxylase | |
E. | All of the above |
11. Why would an antibiotic at the same concentration be more active against bacteria in water than in serum or plasma? (Activity is measured in a test tube)
A. | activity of the antibiotic is increased in water. | |
B. | due to drug-protein interaction in serum | |
C. | the antibiotic is more stable in water | |
D. | all of the above | |
E. | none of the above |
12. Ion channels are targets for drugs. Which drug class targets Na+ channels?
A. | Benzodiazepines | |
B. | Beta blockers | |
C. | Local anesthetics | |
D. | Antihypertensive drugs (cardiac and smooth muscle) | |
E. | Glibenclimide (diabetic drug) |
13. _________________ not metabolized by catechol-O-methyltransferase (COMT).
A. | Dopamine | |
B. | Epinephrine | |
C. | Phenylephrine | |
D. | Norepinephrine | |
E. | All of the above are metabolized by COMT. |