Pharmacology of the ANS Flashcards
1
Q
What are the main neurotransmitters of the sympathetic nervous system?
A
NE and Epi
2
Q
What are the main neurotransmitters of the parasympathetic nervous system?
A
ACh
3
Q
What type of receptors are found in the sympathetic nervous system?
A
Alpha, Beta, (D)-dopamine, nAChR,mAChR
4
Q
What type of receptors are found in the sympathetic nervous system?
A
nAChR, mAChR
5
Q
What ntx is used in ALL PREGANGLIONIC AUTONOMIC FIBERS?
A
ACh
6
Q
What ntx is used in ALL POSTGANGLIONIC PARASYMPATHETIC FIBERS and only on sweat glands on sympathetic postganglionic fibers?
A
ACh
7
Q
Where is epinephrine synthesized?
A
Adrenal medulla
Few cells in the brainstem
8
Q
What is dopamine a precursor for?
A
Epi and NE
9
Q
On which type of tissues/systems does dopamine act?
A
CNS and vascular smooth muscle
10
Q
Where are cholinergic neurotransmitters produced? Where are they stored?
A
Cytoplasm
Acetylcholine varicositites
11
Q
What triggers the release of ACh from presynaptic vesicles?
A
Influx of Ca2+ at the axon terminals
12
Q
What breaks down ACh?
A
Acetylcholinesterase
13
Q
Where are nAChR receptors located?
A
CNS
Autonomic Ganglia (Nn)
Adrenal medulla (sympathetic)
14
Q
What are the functions of nAChRs?
A
Excitatory
Trigger the release of catecholamines
15
Q
What are nAChr agonists?
A
Acetylcholine
Nicotine
16
Q
Where are mAChR receptors located?
A
CNS
Autonomic ganglia
Effector organs (cardiac and smooth muscle, gland cells, nerve terminals)
Sweat glands (sympathetic)
17
Q
What is the function of mAChr?
A
Excitatory and inhibitory in parasympathetics
Sweat secretion in sympathetics
18
Q
What are some mAChR agonists?
A
Acetylcholine
Muscarine
19
Q
- Where are M1 receptors located
- What are the structural features of M1 receptors
- What is the mechanism of M1 receptor
A
- CNS, Ganglia
- GPCR, Gq
- Activation of PLC, IP3 and DAG cascade
20
Q
- Where are M2 receptors located?
- What are their structural features?
- What is the mechanism?
A
- Heart, nerves, smooth muscle
- GPCR, Gi/o
- Inhibit adenylyl cyclase (AC); Decrease cAMP production, activation of K+ channels
21
Q
- Where are M3 receptors located?
- What are their structural features?
- What is the mechanism?
A
- Glands, smooth muscle, endothelium
- GPCR, Gq/11
- Activation of PLC; IP3 and DAG cascade
22
Q
- Where are M4 receptors located?
- What are their structural features?
- What is their mechanism?
A
- CNS
- GPCR/Gi/o
- Inhibition of AC; decrease in cAMP production, activation of K+ channels
23
Q
- Where are M5 receptors located?
- What are the structural features of these receptors?
- What is their mechanism?
A
24
Q
- Where are Nm receptors located?
- What are their structural features?
- What is their mechanism?
A
- Skeletal muscle, NMJ
- Ligand gates ion channel
- Na+, K+ depolarizing ion channel
25
* Where are Nn receptors located?
* What are their structural features?
* What is their mechanism of action?
* Postganglionic cell body dendrites, CNS
* Ligand gated ion channels
* Na+,K+ depolarizing channel
26
* What are the steps of adrenergic neurotransmission?
* Synthesis
* Storage
* Release
* Reuptake
27
* Where does synthesis of NE and Epi occur? What steps are involved?
* Cytoplasm
1. **Tyrosine** transported into cell via **Na+ dependent tyrosine transporter**
2. **Tyrosine** is converted to **dopamine**
3. **Dopamine** transported into vesicles via **VMAT 2**
4. **Dopamine is converted to NE inside the vescicles** (generally speaking, this usually occurs in the adrenal medulla)****
28
* What are the steps in release of NE?
1. Ca2+ influx d/t depolarization at axon terminus
2. Vesicle fusion with presynaptic membrane
3. Release of NTX
4. NTX interacts with alpha or beta adrenergic receptors on postsynaptic cell
29
* What happens to the remaining NE in the synapse?
*
* Reuptake **via NET (NE Transporter)**
* **OR**
* **Metabolism via MAO or COMT**
30
* What drug blocks NE reuptake?
* Cocaine
31
What transporter is responsible for the reuptake of dopamine?
DAT (Oh shit its dat boi)
32
What drug blocks **VMAT 2?** What is a consequence of this?
* **Reserpine**
* Dopamine cannot be sent to the vesicles to be converted to Epi, NE, serotonin
33
* What type of receptors do catecholamines activate? Biochemically speaking-what type of receptors are these?
* Alpha and beta adrenergic (also DA)
* GPCR
34
* What are the primary adrenergic receptors on the heart?
Beta 1
35
* What is the agonist for an alpha 1 adrenergic receptor?
* What is it's main G protein?
* What tissue does it effect?
* What effects does it cause?
* Epinephrine
* Gq (increase PLC,IP3, DAG)
* Vascular, GU smooth muscle, heart, intestinal smooth muscle
* Constriction
* Increased contractile force in the heart
36
* What is the agonist for an apha 2 adrenergic receptor?
* What G protein does it use?
* What tissues does it effect?
* What are the physiological effects?
* Epinephrine more so than NE
* **Gi/G0 (Decrease adenylyl cyclase activity and lowers cAMP)**
* Platelets, nerve terminals, vascular smooth muscle, Beta cells of pancrease
* Clotting, Constriction, Decreased insulin secretion
37
* What are the agonists for beta 1 adrenergic receptors?
* What is its G protein?
* What tissues does it affect?
* What are the physiological responses?
* EPI AND NE
* **Gs; increased adenylyl cyslase, cAMP, \*L type Ca2+ channel opening\***
* Juxtaglomerular cells and heart
* Increased renin secretion, **increased force and rate of contraction, increased AV nodal conduction velocity**
38
* What are the agonists for a beta 2 adrenergic receptor?
* What is its G protein?
* What tissues does it affect?
* What are the physiological responses?
* Epi **\>\>** NE
* **Gs; increase in adenylyl cyclase**
* Smooth muscle, skeletal muscle
* **Dilation,** glycogenolysis, uptake of K+
39
* **What is the rule of thumb for alpha 1 receptors?**
**Stimulate contraction of all smooth muscle**
**Vasoconstriction in vascular smooth muscle**
40
* **What is the rule of thumb for beta 2 receptors?**
* **Vasodilation**
* **(I remeber when my beta died (beta receptor die-a-lates; LAME AS HELL BUT IF IT HELPS YOU REMEMBER?)**
41
* **What is the rule of thumb for muscarinic receptors?**
* **Contract smooth muscle (with a different intracellular signaling pathway than alpha 1 receptors)**
42
* What is the response of sympathetic nervous system on the SA node?
* What receptor is responsible for this physiologic response?
* Increases heart rate
* Beta 1
43
* What is the result of sympathetic activity on the atria?
* What adrenergic receptor is responsible for this effect?
* Increased contractility and conduction velocity
* B1
44
* What is the result of sympathetic stimulation of the AV node/ His Purkinje System?
* What receptor is responsible?
* Increase in automaticity and conduction velocity
* B1
45
What is the result of sympathetic activation of the ventricles?
What adrenergic receptor is responsible?
Increased contractility, conduction velocity, automaticity and rate of idioventricular pacemakers
B1
46
* What is the result of sympathetic activation of arteries and arterioles?
* What receptors are responsible?
* Constriction
* Alpha 1
47
* What is the result of sympathetic activation of tracheal and bronchial smooth muscle? What about bronchial glands?
* What receptors are responsible for these effects?
* Relaxation, decreased secretion (alpha 1), increased secretion (beta 2)
* Beta 2, alpha 1, alpha 2
48
* What effect does parasympathetic activation have on the heart?
* What receptors are responsible for this effect?
* Decrease in HR
* M2 receptors
49
* What affect does parasympathetic stimulation have on the atria?
* What receptors are involved?
* Decrease in contractility and shortened AP duration
* M2
50
What effect does parasympathetic stimulation have on the AV node and His/Purkinje System?
What receptors are involved?
* Decrease in conduction velocity, AV block, little effect
* M2
51
* What effect does parasympathetic stimulation have on the ventricles?
* What receptors are involved?
* Slight decrease in contractility
* M2
52
* Where in the body is there **no parasympathetic innervation?**
* **Arteries and arterioles**
53
* What effect does parasympathetic stimulation have on the endothelium of blood vessels?
* What receptors are involved?
* **Activation of NO synthase**
* **M3**
54
* What effect does parasympathetic stimulation have on tracheal/bronchial smooth muscle and bronchial glands?
* What receptors are involved?
* Contraction, stimulation
* M2,M3
55
* What is another name for EDRF?
NO
56
* What type of ANS innervation innervates the adrenal medulla?
* What triggers the release of Epi and NE from adrenal medulla?
* What is the ratio of NE/Epi released?
* Sympathetic
* Release of ACh from preganglionic fibers
* ACh binds NAChRs and produces a localized depolarization
* Release is 80% epi, 20% NE
57
* What happens as a respone of stretch in baroreceptors?
* What drug elicits this stretching?
* Parasympathetic activation
* Phelylephrine
