Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology > Neuropharm GPCR > Flashcards

Neuropharm GPCR Flashcards

1
Q

G protein coupled receptors

A

Alpha 1 receptor
Alpha 2 receptor
Beta 1 receptor
Beta 2 receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

The alpha 1 Adrenergic receptor is a G protein coupled receptor associated with the _ subunit

A

Gq

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

The Gq subunit associated with the alpha 1 receptor activates _____

A

Phospholipase c

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What does phospholipase C do

A

Hydrolyzes PIP2 to DAG and IP2 in a signal transduction pathway

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

DAG

A

Second messenger that activates PKC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

IP3

A

Plays role in phosphorylation of certain proteins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Catecholamines including ___ and ____ signal through the alpha 1 receptor in the central and peripheral nervous systems

A

Norepinephrine

Epinephrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Effects of activation of alpha 1 receptor

A

Increased vascular smooth muscle contraction
Pupillary dilator muscle contraction
Intestinal and bladder sphincter muscle contraction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

How remember a1

A

Alpha 1 receptor
Gq magazine model flexing arm holding a smoothie muscle
His purple purples are dilated and intestines and bladder flexing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

How does alpha 1 effect pupillary dilator muscles

A

Contracts them

Also called myadrisis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

The alpha 2 receptor is a GPCR associated with the _ subunit

A

Gi

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

The Gi subunit associated with the alpha 2 receptor does what

A

Inhibit production of Camp from ATP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Catecholamines like ___ and ___ signal through the alpha 2 receptor

A

Norepinephrine epinephrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Where are alpha 2 receptors

A

On vascular prejunctional terminals

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What does an activated alpha 2 receptor do

A

Inhibits the release of norepinephrine in a form of negative feedback

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Effects of a2

A

Suppression of sympathetic outflow
Inhibition of insulin release from the pancreas
Inhibition of lipolysis in adipose tissue
Increased platelet aggregation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

The beta 1 Adrenergic receptor is a GPCR associated with the ___ subunit

A

Gs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What does G2 subunit, associated with beta 1, do

A

Activates adenylate cyclase to activate the cAMP-dependent pathway

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Effects of B1 activation

A

Increased cardiac output via an increase in heart rate
Increased cardiac contractility
Increased renin release from juxtaglomerular cells in the kidney
Increased lipolysis in adipose tissue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Name some selective b1 receptor agonist

A

Dobutamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What use dobutamine for

A

Cardiogenic shock

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Name some beta blockers

A

Atenolol
Esmolol
Metoprolol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

The beta 2 Adrenergic receptor is a GPCR associated with the _ subunit

A

Gs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What does Gs associated with b2 do

A

Activates adenylate cyclase, which catalyze the formation of cAMP which activates protein kinase A.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Result of B2 activation

A

Increased heart rate and contractility
Increased lipolysis
Increased insulin release
Increased aqueous humor production and ciliary muscle relaxation causing increased intraocular pressure
Smooth muscle relaxation in uterus
Smooth muscle relaxation in bronchi causing bronchodilator
Vasodilation int he muscle and liver to air int he fight or flight response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Beta 2 agonists are contraindicated in ___

A

Glaucoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Action of b2 on uterus clinically

A

Used to reduce uterine irritability and prevent or stop preterm labor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

A1 receptors mediate ___, b2 receptors mediate ___ in the msucle and liver to air in fight or flight response

A

Vasoconstriction

Vasodilation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Release of insulin is strongly inhibited by ___, why

A

Norepinephrine

Leads to increased blood glucose levels during stress

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

But norepinephrine also activates b2 which stimulates insulin release. Why does norepinephrine inhibit insulin release

A

Dominance of the role of the alpha 2 receptor, which decreases insulin release from pancreas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

When does lipolysis occur

A

When certain hormones that induce lipolysis trigger receptors that activate adenylate cyclase to increase production of cAMP, which activates lipases found in adipose tissue

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

How does a2 activation decrease lipolysis

A

Inhibits production of cAMP, activation of these receptors plays a role in decreasing lipolysis from adipose tissue as a part of negative feedback of the sympathetic pathway.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Platelates are also called

A

Thrombocytes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

How does a2 increase platelet activation

A

Platelets aggregate together using fibrinogen and Von williebrand factor, and are stimulated by ADP, thromboxane and a2 activation

35
Q

Inotropic effect

A

Actions of b1 receptor include increased atrial and ventricular contractility

36
Q

What does inotropic effect lead to

A

Increased cardiac output in the sympathetic response

37
Q

Effect of b1 on kidney

A

Increases renin release from juxtaglomerular cells in the kidney

38
Q

What does renin do

A

Enzyme that breaks down angiotensinogen to angiotensin 1, which is further cleaved by ACE enzyme into angiotensin II

39
Q

What does angiotensin II do

A

Constrict blood vessels, increases ADH secretion and aldosterone and stimulates the thirst reflex in the hypothalamus, leading to an increase in blood pressure

40
Q

Effect of increased renin on bp

A

Increased bp in sympathetic response

41
Q

How does b1 effect lipolysis

A

Activation leads to to increased lipolysis to help mobilize energy stores during the sympathetic response

42
Q

What is lipolysis

A

Breakdown of lipids, which involves the hydrolysis of triglycerides into free fatty acids, which can undergo degradation by beta oxidation to produce energy for the body

43
Q

B2 activation activates what

A

Adenylate cyclase, which catalyze the formation of cAMP, which activates PKA

44
Q

How does b2 increase heart rate

A

SA node

Chronotropic effect

45
Q

Chronotropic effect

A

Increased SA node rate

Increases cardiac output int he sympathetic response, although the effect is minor when compared to the beta1 receptor

46
Q

Actions of b2

A

Increased atrial and ventricular contractility, known as inotropic effect

47
Q

Inotropic effect

A

B2 increases atrial and ventricular contractility

48
Q

What does inotropic effect of b2 lead to

A

Increased CO in the sympathetic response although the effects in minor when compared to the b1 receptor

49
Q

Activation b2 lipolysis

A

Increases lipolysis to help mobiliza energy stores during the sympathetic response

50
Q

B2 insulin

A

Decrease in secretion in sympathetic response

51
Q

B2 eye

A

Increase aqueous humor in the eye

52
Q

How treat glaucoma

A

B2 antagonists such as timolol

53
Q

What are the ciliary muscles

A

Ring of smooth muscle in eye that controls accomodation for viewing objects and regulates the flow of aqueous humor into schlemms canal

54
Q

B2 and ciliar muscle

A

Relaxation in sympathetic

Increase in ciliary body size

55
Q

Effect of b2 relaxation of ciliary muscle on zonule fibers

A

Increases tension in zonule fibers of the eye, causing the lens to stretch flat, appropriate for far distance vision

Impedes aqueous flow leading to an increase in intraocular pressure

56
Q

A1 receptors mediate ___, beta 2 receptors mediate ___ in the muscle and liver to aid in fight or flight

A

Vasoconstriction

Vasodilation

57
Q

How treat asthma with b2 agonist

A

Bronchodilation

58
Q

How can b2 agonist prevent or stop preterm labor

A

Smooth muscle relaxation int he uterus which reduce uterine irritability

59
Q

Example of a b2 agonist used to decrease uterine tone as a tocolytic

A

Ritodrine

60
Q

Non selective beta blockers

A

First generation b blockers have antagonistic effects at b1 and b2 preventing direct sympathomimetics such as norepinephrine and epinephrine from binding to these receptors

61
Q

Where are b1 receptors

A

Heart kidney

62
Q

Where are b2

A

Lung, peripheral blood vessels and skeletal muscle

63
Q

What suffix do beta blockers have

A

Olol

64
Q

How do non selective beta blockers work

A

Prevent the release of cAMP, a secondary messenger int he Gs protein signal transduction pathway. Without camp, protein kinase A remains inactivated and thus ca currents are reduced

65
Q

Name the non selective beta blockers

A

Propranolol
Pindolol
Nadolol

Timolol

66
Q

Proparnolol was first developed for what

A

Angina pactoris and then used as anti hypertensive

Not commonly used for these anymore

67
Q

Why is propranolol not usually used usually for angina pectorals or as an antihypertensivee anymore

A

Side effects such as bronchospasm and thus exacerbation of chronic obstructive lung disease (COPD) and asthma
Depression
Exacerbation of peripheral arterial disease, and masking signs and symptoms of hypoglycemia in diabetics

68
Q

What is propranolol used for now

A

Long term post MI
Atrial fibrillation, A-flutter
Treat thyroid storm - arrhythmias
Thryotoxicosis
Essential tremor
Prevention of bleeding esophageal varices
Akathisia and chronic migraine prophylaxis

69
Q

Traditional use of nonselective beta blocker, timolol

A

First line therapy for the reduction of intraocular pressure in open angle glaucoma and is part of the empiric therapy for acute angle closure glaucoma

70
Q

Timolol was initially shown to not be an effective systemic hypotensive agent, but when formulated into a ___ drug it was demonstrated to be extremely effective in reduction of IOP

A

Topical

71
Q

But what is the preserved treatment for open angle glaucoma

A

Topical prostaglandins

72
Q

Side effects timolol

A

Cardiac arrhythmia and severe bronchospasm

73
Q

What is nadolol used for

A

Prevention of bleeding esophageal varices
Migraine headaches
Adult ADHD
Essential tremor and Parkinson’s disease

74
Q

Side effects of nadolol

A

Bradycardia, fatigue and bronchospasms

75
Q

Partial b agonists

A

Block b receptors but also have intrinsic sympathomimetic activity (ISA) and partially activate the receptor. At high doses they exert effects like epinephrine (increased pulse rate, increased blood pressure, bronchodilation)

76
Q

Example of partial b agonist

A

Pindolol, Acebutolol, Labetalol

77
Q

What is pinodolol used for

A

Treatment of angina pectoris and hypertension

78
Q

Why is treatment with pindolol rarely used

A

Due to its intrinsic sympathomimetic activity (ISA)

79
Q

Nonselective beta with alpha blocking

A

These drugs nonselectively block both b and a receptors . Their a blocking effects give them a vasodilatory effect Which potentiates the b blocking effect to reduce blood pressure

80
Q

Examples of nonselective b with a blocking

A

Carvedilol

Labetalol

81
Q

Carvedilol to treat what

A

CHF as an adjunct to conventional treatments (ACE inhibitors and diuretics)
Treat pregnancy induced hypertension and can be used 2nd line in hypertensive emergencies

82
Q

Labetolol

A

Treatment of pregnancy induced hypertension and can be used 2nd line in hypertensive emergencies

83
Q

Selective b blockers

A

Metoprolol, Betaxolol, Acebutolol, Atenolol

Pharmacology (52 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions