[5] Adrenergic Receptors

Question 1

Rate Limiting Step of Norepinephrine

Answer 1

Tyrosine Hydroxylase

Tyrosine -> DOPA

Question 2

Receptors prolific in smooth muscles and blood vessels

Answer 2

Alpha-1

Question 3

Postsynaptic effector mostly found in the heart

Answer 3

Beta-1

Question 4

Postsynaptic effector cells especially in smooth muscles

Answer 4

Beta-2

Question 5

Postsynaptic effector cells especially in lipocytes

Answer 5

Beta-3

Question 6

Which has a methyl group? Epinephrine or Norepinephrine?

Answer 6

Epinephrine

because

NO-repinephrine

Question 7

Subtypes of Beta-1 Receptors

Answer 7

Heart

Juxtaglomerular cell

Question 8

Subtypes of Beta-2Receptors

Answer 8

Respiratory, uterine, and vascular smooth muscle
Skeletal Muscle
Human Liver

Question 9

Function: Activation of Beta-2 in Respiratory Tissue

Answer 9

Smooth muscle relaxation

Question 10

Function: Activation of Beta-2 in Skeletal Muscle

Answer 10

Potassium Uptake

Question 11

Function: Activation of Beta-2 in the Liver

Answer 11

Activates glycogenolysis

Question 12

Function: Activation of Beta-3 Receptors

Answer 12

Increased lipolysis

Question 13

Receptor Specificity is ____ but not _____?

Answer 13

Relative, but not absolute

Question 14

Parent Compound of Adrenergic Agents

Answer 14

Phenylethylamine

Question 15

Effect: Increased size of alkyl substituents on Amino Group

Answer 15

Increased beta-receptor activity

Decreased alpha-receptor activity

Question 16

A lower Kd value would mean?

Answer 16

Higher potency

Question 17

Effect: Decreased substitution of benzene ring

Answer 17

Increased bioavailability and prolongs duration of action

Since they are not catecholamines, they are spared from COMT Inactivation in the Gut and Liver

Question 18

Effect: Substitution on the Alpha Carbon

Answer 18

Prolonged action of drugs especially in noncatecholamines

Question 19

Effect: Substitution on the Beta-Carbon

Answer 19

Important for storage

Question 20

Relative Selectivity of Adrenoceptor Agonists

Alpha Agonists
Phenylephrine, Midodrine

Answer 20

Alpha 1 > Alpha 2&raquo_space;»> Beta

Me-dodrine, me is 1

Question 21

Relative Selectivity of Adrenoceptor Agonists

Alpha Agonists
Clonidine, Methylnorepinephrine

Answer 21

Alpha 2 > Alpha 1&raquo_space;»> Beta

Clone ni Din, so they are 2

Question 22

Beta-1 Receptor Agonist Effect as a:

Chronotrope
Intrope

Answer 22

C: +
I: +

Question 23

What receptor agonists do you use for Congestive Heart Failure and Cardiogenic Shock

Answer 23

Beta-1 Receptor

Question 24

Classification of Dobutamine

Answer 24

Complex

( + ) Isomer: Alpha 1 Antagonist ; Beta-1 Agonist

( - ) Potent Alpha 1 Agonist

Question 25

Function: Alpha-1 Receptor Agonists

Answer 25

Constriction smooth muscles causing increased peripheral resistance and venous return

Question 26

Are there Alpha-1 receptors in the heart?

Answer 26

Yes

Question 27

How come if you give a lot of epinephrine it actually causes decreased heart rate instead of increased?

Answer 27

Reflex Baroreceptor Vagal Discharge

Question 28

Function: Alpha-2 Receptor Agonist

Answer 28

Reduce blood pressure

Question 29

Classification of Clonidine

Answer 29

Alpha-2

Question 30

Classification of Methyldopa

Answer 30

Alpha-2 | Me-thoo

Question 31

Classification of Phenylephrine

Answer 31

Alpha-1

Question 32

Function: Alpha and Beta receptor agonists in GI Tract

Answer 32

Relax gastrointestinal smooth muscle

Question 33

Function: Alpha-2 Selective Agonists in GI Tract

Answer 33

Enhanced salt and water reabsorption | Treatment of diarrhea, Clonidine

Question 34

Function: Beta-2 Receptor Agonist in Genitourinary Tract

Answer 34

Relax smooth muscle | Relaxation of bladder wall

Question 35

Function: Alpha-1 Agonist in Genitourinary Tract

Answer 35

Constriction of bladder base, urethral sphincter

Question 36

Which receptor causes increased lipolysis in fat cells?

Answer 36

Beta-3 | 3 layers of fat

Question 37

Which receptor causes increased insulin uptake?

Answer 37

Beta-2 | In-THWOO-Lin, pretend may lithp ka

Question 38

Effect: Amphetamine

Answer 38

Non-exocytotic release of Norepinephrine It is taken up by NET and blocks MAO

Question 39

Examples of Alpha-1 Receptor Antagonists

Answer 39

Prazosin Terzosin Doxazosin (They are SIN-ners, antagonists to Alpha-1)

Question 40

What is Tamsulosin used for?

Answer 40

Benign Prostatic Hypertrophy Binds better to A and D better than B so it is used for this instead of for hypertension

Question 41

Is Epinephrine selective or non-selective?

Answer 41

Non-Selective

Question 42

Prototypic non-selective beta blocker

Answer 42

Propranolol

Question 43

Prototypic selective beta blocker

Answer 43

Metoprolol

Question 44

What are the selective B-Agonists?

Answer 44

A BEAM of B1-Blocker ``` Acebutolol Betaxolol Esmolol Atenolol Metoprolol ```

Question 45

Examples of Partial Agonists

Answer 45

Pindolol Acebutulol (Eh, why not Atenolol? Dahil hindi raw partial si Ate.)