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Neuropharm GPCR Flashcards

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1
Q

G protein coupled receptors

A

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

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2
Q

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

A

Gq

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3
Q

The Gq subunit associated with the alpha 1 receptor activates _____

A

Phospholipase c

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4
Q

What does phospholipase C do

A

Hydrolyzes PIP2 to DAG and IP2 in a signal transduction pathway

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5
Q

DAG

A

Second messenger that activates PKC

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6
Q

IP3

A

Plays role in phosphorylation of certain proteins

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7
Q

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

A

Norepinephrine

Epinephrine

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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

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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

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10
Q

How does alpha 1 effect pupillary dilator muscles

A

Contracts them

Also called myadrisis

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11
Q

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

A

Gi

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12
Q

The Gi subunit associated with the alpha 2 receptor does what

A

Inhibit production of Camp from ATP

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13
Q

Catecholamines like ___ and ___ signal through the alpha 2 receptor

A

Norepinephrine epinephrine

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14
Q

Where are alpha 2 receptors

A

On vascular prejunctional terminals

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15
Q

What does an activated alpha 2 receptor do

A

Inhibits the release of norepinephrine in a form of negative feedback

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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

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17
Q

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

A

Gs

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18
Q

What does G2 subunit, associated with beta 1, do

A

Activates adenylate cyclase to activate the cAMP-dependent pathway

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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

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20
Q

Name some selective b1 receptor agonist

A

Dobutamine

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21
Q

What use dobutamine for

A

Cardiogenic shock

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22
Q

Name some beta blockers

A

Atenolol
Esmolol
Metoprolol

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23
Q

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

A

Gs

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24
Q

What does Gs associated with b2 do

A

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

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25
Result of B2 activation
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
26
Beta 2 agonists are contraindicated in ___
Glaucoma
27
Action of b2 on uterus clinically
Used to reduce uterine irritability and prevent or stop preterm labor
28
A1 receptors mediate ___, b2 receptors mediate ___ in the msucle and liver to air in fight or flight response
Vasoconstriction | Vasodilation
29
Release of insulin is strongly inhibited by ___, why
Norepinephrine | Leads to increased blood glucose levels during stress
30
But norepinephrine also activates b2 which stimulates insulin release. Why does norepinephrine inhibit insulin release
Dominance of the role of the alpha 2 receptor, which decreases insulin release from pancreas
31
When does lipolysis occur
When certain hormones that induce lipolysis trigger receptors that activate adenylate cyclase to increase production of cAMP, which activates lipases found in adipose tissue
32
How does a2 activation decrease lipolysis
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.
33
Platelates are also called
Thrombocytes
34
How does a2 increase platelet activation
Platelets aggregate together using fibrinogen and Von williebrand factor, and are stimulated by ADP, thromboxane and a2 activation
35
Inotropic effect
Actions of b1 receptor include increased atrial and ventricular contractility
36
What does inotropic effect lead to
Increased cardiac output in the sympathetic response
37
Effect of b1 on kidney
Increases renin release from juxtaglomerular cells in the kidney
38
What does renin do
Enzyme that breaks down angiotensinogen to angiotensin 1, which is further cleaved by ACE enzyme into angiotensin II
39
What does angiotensin II do
Constrict blood vessels, increases ADH secretion and aldosterone and stimulates the thirst reflex in the hypothalamus, leading to an increase in blood pressure
40
Effect of increased renin on bp
Increased bp in sympathetic response
41
How does b1 effect lipolysis
Activation leads to to increased lipolysis to help mobilize energy stores during the sympathetic response
42
What is lipolysis
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
B2 activation activates what
Adenylate cyclase, which catalyze the formation of cAMP, which activates PKA
44
How does b2 increase heart rate
SA node | Chronotropic effect
45
Chronotropic effect
Increased SA node rate | Increases cardiac output int he sympathetic response, although the effect is minor when compared to the beta1 receptor
46
Actions of b2
Increased atrial and ventricular contractility, known as inotropic effect
47
Inotropic effect
B2 increases atrial and ventricular contractility
48
What does inotropic effect of b2 lead to
Increased CO in the sympathetic response although the effects in minor when compared to the b1 receptor
49
Activation b2 lipolysis
Increases lipolysis to help mobiliza energy stores during the sympathetic response
50
B2 insulin
Decrease in secretion in sympathetic response
51
B2 eye
Increase aqueous humor in the eye
52
How treat glaucoma
B2 antagonists such as timolol
53
What are the ciliary muscles
Ring of smooth muscle in eye that controls accomodation for viewing objects and regulates the flow of aqueous humor into schlemms canal
54
B2 and ciliar muscle
Relaxation in sympathetic | Increase in ciliary body size
55
Effect of b2 relaxation of ciliary muscle on zonule fibers
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
A1 receptors mediate ___, beta 2 receptors mediate ___ in the muscle and liver to aid in fight or flight
Vasoconstriction | Vasodilation
57
How treat asthma with b2 agonist
Bronchodilation
58
How can b2 agonist prevent or stop preterm labor
Smooth muscle relaxation int he uterus which reduce uterine irritability
59
Example of a b2 agonist used to decrease uterine tone as a tocolytic
Ritodrine
60
Non selective beta blockers
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
Where are b1 receptors
Heart kidney
62
Where are b2
Lung, peripheral blood vessels and skeletal muscle
63
What suffix do beta blockers have
Olol
64
How do non selective beta blockers work
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
Name the non selective beta blockers
Propranolol Pindolol Nadolol Timolol
66
Proparnolol was first developed for what
Angina pactoris and then used as anti hypertensive | Not commonly used for these anymore
67
Why is propranolol not usually used usually for angina pectorals or as an antihypertensivee anymore
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
What is propranolol used for now
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
Traditional use of nonselective beta blocker, timolol
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
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
Topical
71
But what is the preserved treatment for open angle glaucoma
Topical prostaglandins
72
Side effects timolol
Cardiac arrhythmia and severe bronchospasm
73
What is nadolol used for
Prevention of bleeding esophageal varices Migraine headaches Adult ADHD Essential tremor and Parkinson’s disease
74
Side effects of nadolol
Bradycardia, fatigue and bronchospasms
75
Partial b agonists
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
Example of partial b agonist
Pindolol, Acebutolol, Labetalol
77
What is pinodolol used for
Treatment of angina pectoris and hypertension
78
Why is treatment with pindolol rarely used
Due to its intrinsic sympathomimetic activity (ISA)
79
Nonselective beta with alpha blocking
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
Examples of nonselective b with a blocking
Carvedilol | Labetalol
81
Carvedilol to treat what
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
Labetolol
Treatment of pregnancy induced hypertension and can be used 2nd line in hypertensive emergencies
83
Selective b blockers
Metoprolol, Betaxolol, Acebutolol, Atenolol

Pharmacology (52 decks)

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