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MTP > Exam 3: Receptor Systems and ANS > Flashcards

Exam 3: Receptor Systems and ANS Flashcards

1
Q

What are the steps of signal transduction?

A
  1. Reception (Signal molecule and receptor binding)
  2. Transduction (Signal-transduction pathway)
  3. Response (Activation of cellular responses, secretion, smooth muscle metabolic hr, bp)
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2
Q

What are the properties of cell membrane receptors?

A
  1. Hydrophilic ligands can’t enter cell
  2. Binds to extracellular recpetors
  3. Fast responding
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3
Q

What are the properties of cytosolic or nuclear receptor binding?

A
  1. Lipophilic ligands diffuse through membrane into the cell to bind to receptors
  2. Activates or suppresses gene expression
  3. Slower responses depending on receptors
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4
Q

What is a G-coupled receptor?

A

A single proteins with seven transmembrane domains

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5
Q

What are the characteristics of G protein signaling?

A
  1. Trimeric protein that bind to quinine nucleotides
  2. Couple integral membrane receptors to target intracellular second messenger enzyme systems
  3. Molecular switch between inactive and active
  4. a subunit contains GTPases activity by hydrolyzes of GTP to GDP
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6
Q

Describe the resting state of G-protein signaling

A

G-a is associated with G-by and GDP

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6
Q

Describe the resting state of G-protein signaling

A

G-a is associated with G-by and GDP

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7
Q

Describe the activation of G-protein signaling

A
  1. GTP displaces GDP of a-subunit that dissociates from by subunits
  2. a stimulates adenylate cyclase that catalyzes cAMP from ATP
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8
Q

Describe the reassociation of G-protein signaling

A
  1. Intrinsic GTPase of a subunit hydrolyzes GTP to GDP
  2. a subunit returns to by subunits and induces resting state
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9
Q

Describe the signal transduction pathway induced by Gs?

A
  1. Drug binds to receptors activating G-proteins or protein kinases
  2. Gs is the transducer for adenylate cyclase
  3. Second messengers is cAMP from ATP and adenylate cyclase
  4. Second messengers increased Protein Kinase A (PKA)
  5. Ion channels open and increase intracellular Ca2+ activating other enzymes in the system (amplification of cellular responses)
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10
Q

How can increased intracellular cAMP increase gene transcription?

A
  1. Activated PKA enters the nucleus and phosphorylates CREB (cAMP response element binding)
  2. CREB recruits the coactivator CBP (CREB binding protein)
  3. CBP binds to CREB-binding element on DNA stimulating or inhibiting gene transcription
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10
Q

How can increased intracellular cAMP increase gene transcription?

A
  1. Activated PKA enters the nucleus and phosphorylates CREB (cAMP response element binding)
  2. CREB recruits the coactivator CBP (CREB binding protein)
  3. CBP binds to CREB-binding element on DNA stimulating or inhibiting gene transcription
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10
Q

How can increased intracellular cAMP increase gene transcription?

A
  1. Activated PKA enters the nucleus and phosphorylates CREB (cAMP response element binding)
  2. CREB recruits the coactivator CBP (CREB binding protein)
  3. CBP binds to CREB-binding element on DNA stimulating or inhibiting gene transcription
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11
Q

Describe the signal transduction pathway induced by Gi?

A
  1. First messenger binds to receptor
  2. Gi binds to adenylate cyclase inhibiting response
  3. Decreased cAMP production
  4. Decreased PKA
  5. Opening of K+ channels
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12
Q

Where are Gi regulations mainly found?

A

Muscarinic M2 receptors on heart

Adrenergic alpha-2 receptors are Gi

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13
Q

What is the G-protein link to Gq?

A
  1. Phospolipase C is activated by Gq hydrolyzed from PIP2
  2. PLC forms 2 second messengers
  3. DAG activates PKC
  4. PKC directly phosphorylates intracellular proteins and modulates gene expression through MAP kinase and NF-kb
  5. IP3 is activated to release Ca2+ from intracellular stores by binding to an IP3-gated Ca2+ channel in the ER
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14
Q

How can calcium be used as a second messenger system?

A
  1. Calcium binds to calcium binding protein such as calmodulin
  2. Ca2+/calmodulin complexes activate CaM-dependent kinases (CaM kinase II)
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15
Q

Why do we study autonomic pharmacology?

A

Determining the mechanism of drug action and anatomical information to predict the effects of drugs

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16
Q

What diseases are autonomic drugs used to treat?

A
  1. Angina
  2. Heart failure
  3. High BP
  4. Ocular pharmacotherapy
  5. ALzheimers
  6. GUT and prostatic hypertrophy
  7. Astma and COPD
  8. Septic and anaphylactic shock
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17
Q

What controls most autonomic function?

A

Pons and medulla

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18
Q

What is the purpose of the afferent (sensory) nervous system?

A

To maintain steady-state in an ever-changing environment

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19
Q

What are the 2 divisions of the ANS?

A

Para and sympathetic NS

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20
Q

What neurotransmitter activates the PNS?

A

ACh released by preganglionic (nicotinic) and postganglionic neurons (muscarinic)

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21
Q

What neurotransmitter activates the Sympathetic NS?

A
  1. ACh released by nicotinic receptors of preganglionic neurons
  2. Norepinephrine released by most postganglioninc neurons onto adrengegic receptors on end organs
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22
Q

Compare the lengths of pre and postganglionic neurons of the PNS and SNS?

A

PNS: long pre localized in ganglia, short post on innervated tissue
SNS: short pre localized in ganglion, long post

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23
Q

Describe the release of ACh in the adrenal medulla

A
  1. ACh is released onto nicotinic receptors by pressgang
  2. Nicotinic receptor is on adrenal medulla (modified catecholaminergic postganglionic secretory cell)
  3. Humoral release
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24
Q

What make sweat gland different from other SNS systems?

A

Release of ACh from both pre and postganglionic neurons

25
Q

What are the cholinergic receptors?

A
  1. Nicotinic
  2. Muscarinic
26
Q

What are the NE receptors?

A

Adrenergic

27
Q

Where are ACh synapses found?

A
  1. All motor (skeletal) nerves
  2. All preganglionic autonomic nerves and adrenal medulla (nicotinic)
  3. All postganglionic parasympathetic nerves (muscarinic)
  4. Few postganglionc cholinergic sympathetic nerves (sweat glands, muscarinic)
28
Q

Where are NE synapses found?

A
  1. Almost all postganglionic sympathetic fibers (adrenergic)
  2. Hormones release from adrenal medulla (NE and E bind to adrenergic)
29
Q

What is the difference between cholinergic and noradrenergic in regards to rest and digest?

A

C: discharge promotes digestion and absorption of food
N: Discharge maintains arterial and venous tone

30
Q

What is the NE and E response to fight or flight?

A
  1. Accelerates heat rate
  2. Increases BP
  3. Elevates plasma glucose
  4. Constricts blood vessels to skin and intestine
  5. Shuts of gastric secretion
  6. Lowers CNS threshold
  7. Relaxes pupils
31
Q

What are the autonomic controls of the SA node?

A

Syp: increases heart rate at receptors a1, b1, b2
Par: Decreases heart rate at M2

32
Q

What are the autonomic controls of the AV node?

A

S: Increases automaticity, conduction velocity at a1, b1, b2
P: Decreases automaticity, AV block at M2

33
Q

What are the autonomic controls of the atrium?

A

S: Increases force and conduction velocity at a1, b1, b2
P: Decrease force and conduction velocity at M2

34
Q

What is the autonomic controls of the ventricles?

A

S: Increases automaticity and contractile force at a1, b1, b2
P: Decrease automaticity and contractile force at M2

35
Q

What are the autonomic controls of the arterioles?

A

S: Constriction at a1
P: Dilation (not innervated) at M3

36
Q

What are the autonomic controls of skeletal muscles?

A

S: Dilation (Constriction) at b2 (a1)
P: Dilation (not innervated)

37
Q

What are the autonomic controls of coronary?

A

S: Dilation (Constriction) at b2 (a1)
P: Dilation (not innervated)

38
Q

What are the autonomic controls of veins?

A

S: Constriction at a1

39
Q

What innervates the vasculature?

A

Sympathetic nerve fibers, there is no parasympathetic innervation of the vasculature

40
Q

What are the autonomic controls of bronchial smooth muscle?

A

S: Relaxation, dilation (not innervated) at B2
P: Constriction at M3

41
Q

What are the autonomic controls of bronchial glands?

A

S: Increased secretion (decreased secretion) at B2 (a1)
P: Increased secretion at M3

42
Q

What are the autonomic controls of GIT smooth muscle?

A

S: Relaxation, decreased motility at a1, b2, presyn a2
P: Contraction, increased motility at M3

43
Q

What are the autonomic controls of sphincters?

A

S: Contraction at a1
P: Relaxation at M3

44
Q

What are the autonomic controls at glands and gastric acid?

A

S: Minimal effects
P: Secretion at M1

45
Q

What nervous system division also control the GIT other than the autonomic?

A

Enteric NS

46
Q

What are the autonomic controls of detrusor (bladder) muscle?

A

S: Relaxation at B2
P: Constriction at M3

47
Q

What are the autonomic controls of trigone muscle (sphincter)?

A

S: Contraction at a1
P: Relaxation (minimal) M3

48
Q

What are the autonomic controls of penis?

A

S: Ejacualation at a1
A: Erection at M

49
Q

What are the autonomic controls of renin secretion?

A

S: Increase renin at B1
P: none

50
Q

What are autonomic controls of the uterus when pregnant?

A

S: Contraction at a1
P: Variable at M3

51
Q

What are autonomic controls of the uterus when not pregnant?

A

S: Relaxation at b2
P: Variable

52
Q

What are autonomic controls of radial muscle of iris?

A

S: Contraction (mydriasis/dilation) at a1
P: None

53
Q

What are autonomic controls of the sphincter muscle in the iris?

A

S: None
P: Contraction (miosis) at M3

54
Q

What are the autonomic controls of ciliary muscle?

A

S: Relaxation (slight) at B2
P: Contraction (Near vision, accommodation) at M3

55
Q

What are autonomic controls of lacrimation?

A

P: Increases at M3

56
Q

What are the autonomic controls of ciliary epithelium?

A

S: Increases aqueous humor secretion at B2

57
Q

What are the autonomic controls of thermoregulatory sweat glands?

A

Sympathetic cholinergic increases sweating at M3

58
Q

What are the autonomic controls of apocrine glands?

A

S: Increases sweating in palms at a1

59
Q

What are the autonomic controls of pilomotor?

A

S: Piloerection at a1

60
Q

Wha are the autonomic controls of salivation?

A

S: Secretion of K+ and H20 at a1, secretion of amylase at b
P: Secretion of K+ and H20 at M3

61
Q

What are the autonomic controls of liver?

A

S: Glycogenolysis and gluconeogenesis at a1 and b2
P: Glycogen synthesis at M

62
Q

What are the autonomic controls of fat cells?

A

S: Lipolysis at B3

63
Q

What are the autonomic controls of insulin secretion?

A

S: Decreases at a2
P: Increases at M

MTP (15 decks)

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