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Flashcards in Pharmacology Capstone Deck (90):
0

sympathetic nervous system is aka

thoracolumbar

1

parasympathetic nervous system is aka

craniosacral

2

Parasympathetic NT and R

NT=Ach
R=NAchR, MAchR

3

Sympathetic NT and R

NT= NE>epi>Da; Ach
R= alpha, Beta, D, nAchR, mAchR

4

Cholinergic - think?

acetyl choline
muscarinic and nicotinic receptors

5

adrenergic think?

norepinephrine
epinephrine
dopamine

alpha, beta, D receptors
from tyrosine

6

major NT of the parasymp system

Ach

7

found at ALL PREganglionic autonomic fibers

Ach

8

found at ALL POST ganglionic parasympathetic fibers

Ach

9

found at a few POSTgaglionic sympathetic fibers (WHERE?)

Ach
sweat glands

10

major NT of the sympathetic nervous system

NE

11

found at a vast majority of postganglionic sympathetic fibers

NE

12

synthesis occurs in adrenal medulla and a few neuronal pathways in brainstem

EPI

13

Synthesized in the cytoplasm of neurons

Dopamine

14

Dopamine has actions where?

in the CNS and renal vascular smooth muscle

15

Neurons that release Ach are called

cholinergic neurons

16

Order of steps in cholinergic neurotransmission

Synthesis
storage
release
binding
termination

17

Synthesis of Ach

CHOLINE TRANSPORTER transports choline into neurons
dependant on cotransport with NA

CHOLINE ACETYLTRANSFERASE (ChAT) conbines acetyl coenxyme A with choline to make Ach

18

Storage of Ach

ATPase dependent Ach vesicular transporter transports Ach into neuronal vesicles.

19

Release of Ach

AP reaches axon terminal, causes opening of VgCa2+channels
Ca2+enters the neuron
Ca2+ influx promotes fusion of vesicular membrane with cell membrane
Ach is released

the SNARE protein complex is responsible for fusion of the vesicle membrane and synaptic membrane through VAMP and SNAP proteins

20

Binding of Ach to cholinergic receptors

Ach diffuses across the synaptic cleft
binds nachrs which facilitates Na entry into post-gang fiber or release of epi/NE from adrenal medulla
post-synaptic machrs are also activated by ach causing smooth muscle contraction, decrease in HR, glandular secretin etc

Ach can bind to and activate both nachr (+) and machr (-) to modify its own release.

21

activation of prejunctional nAchRs _________ Ach release

stimulates/potentiates

22

activation of prejunctional machrs ________further release

inhibits

23

Termination of Ach signaling

Acetylcholinesterase cleaves Ach into acetate and choline
acetate diffuses out of the synapse
choline is recycled into the nerve

24

What two types of receptors does Ach bind to?

nAchR
mAchR

25

Where are NnAchrs found

all ganglia (sym and parasymp) and adrenal medulla (symp)

26

where are mAChrs found

smooth and cardiac muscle
gland cells
nerve terminals

27

nAchR is what type of a channel

ionotropic (ligand gated ion channel)

28

nAchR allows what to pass through the channel

Na

29

mAchR is what type of receptor

metabotrpoic, GPCR

30

how many subtypes of muscarinic receptors are there

5

31

what are the predominant smooth muscle muscarinic receptors

M2 and M3

32

what is the predominant muscarinic receptor in cardiac muscle

M2

33

adrenergic transmission, think

catecholamines
(NE, E, Da)

34

principle NT of most of sympathetic post ganglionic fibers and ov certain tracts in CNS

NE

35

major hormone/NT released by adrenal medulla

epi

36

predominant NT of mammalian extrapyramidal system and several mesocortical and mesolimbic neuronal pathways

Dopamine

37

Steps of catecholamine signalling

synthesis
storage
release
binding
termination

38

Synthesis of catecholamines

tyrosine transported into nerve terminal by a Na dependent transporter
trosine--> DOPA->Dopamine->NE->Epi

final step occurs only in the adrenal medulla and in a few epi containing neuonal pathways in the brainstem

39

Storage of catecholamines

vesicular monoamine transporter (VMAT-2) transports Da into the vesicle
promiscuous, can also transport NE, epi, and seratonin across the vesicle membrane

40

reserpine

inhibits VMAT-2, leads to depletion of catecholamines from sympathetic nerve endings.

41

Release of catecholamines

similar to release of Ach after depolarization and influx of Ca2+.
in adrenal medulla, triggering event is release of Ach and its interaction with nAchRs on chromaffin cells to produce localized deppol

42

Binding of catecholamines to adrenergic receptors

diffuse across synaptic cleft and bind to adrenergic alpha and beta receptors

effector organ responses include: contraction, glycogenolysis, gluconeogenesis, relaxation and increased force and rate of cardiac muscle contraction

43

Termination of catecholamine signaling (3 ways)

reuptake into nerve terminals
dilution by diffusion
metabolic transformation

44

major mechanism that terminates the actions of catecholamines

reuptake

45

reuptake of catecholamines

by two neuronal membrane transporters NET and DAT (NE transporter and DA transporter)

46

Dilution by diffusion of catecholamines

diffuseion out of the junctional cleft and uptake ate extraneuronal sites by transporters ENT/ OCT1 and OCT2)

47

Metabolic transformation of catecholamines occurs through what enzymes?

MAO
COMT

48

examples of common sympathetic cotransmitters

ATP,
NPY

49

feedback on prejunctional receptors to inhibit release of each other

NE, NPY, ATP
sympathetics

50

examples of receptors on sympathetic nerve varicosities that also inhibit the release of sympathetic NTs include

M2 and M4, serotonin, PGE2, histamine, enkephalin, DA, and alpha 2

51

examples of receptors on sympathetic nerve varicosities that enhance sympathetic NT release

Beta 2, ang II, nAchR

52

How many subtypes of alpha adrenergic receptors are there?

2 - alpha1 and alpha2

53

THE END RESULT OF ALPHA-1 RECEPTOR ACTIVATION IS

muscle contraction

54

smooth muscle contraction results in ______
cardiac muscle contraction leads to ________
(alpha-1)

vasoconstriction
increase in contractile force on the heart

55

exception to alpha-1 rule

gut
activation of alpha 1 receptors and subsequent increas in Ca2+ causes hyperpolarization and muscle relaxation by activation of Ca2+ dependent K+channels

56

ACTIVATION OF ALPHA-2 RESULTS IN

vascular smooth muscle contraction, decreased insulin secretion adna a decreased release of NE (presynaptic alpha-2 receptors)

57

how many subtypes of Beta adrenergic receptors are there

three
B1, B2, B3

58

All B receptors are _____coupled receptors

Gs coupled

59

B1 receptors are found mainly

myocardium

60

ACTIVATION OF BETA-1 RECEPTORS RESULTS IN

increased force and rate of heart contraction and AV nodal conduction velocity

61

B2 receptors are mainly found

smooth muscle and most other sites

62

BETA 2 RECEPTOR ACTIVATION CAUSES

RELAXATION of
vascular, broncial, GU and GI smooth muscle

63

Beta 3 receptors are found

adipose tissue

64

ACTIVATION OF BETA 3 RECEPTORS RESULTS IN

lipolysis

65

triad of symptoms for pheochromocytoma

headache, perspiration, palpitations

66

alpha 1 receptors are found primarily

on sm m surrounding the vasculature

67

alpha 2 receptor primary location is

presynaptic in brain, leading to a decrease in sympathetic outflow

68

alpha 1 receptors are _____coupled

Gq

69

alpha 2 receptors are _____ coupled

Gi, Go

70

Primary tissue locations of adrenergic receptor subtypes
a1
a2
b1
b2
b3

a1 - postjunctional smooth muscle (contraction
a2 - presynaptic neurons, postynaptic tissues and blood platelets
- (ocular, adipose, intestinal, hepatic, renal, endocrine)
b1 - heart (stimulation)
b2 - bronchial, uterine, and vascular smooth muscle (relaxation)
b3 - adipose tissue (lipolysis)

71

centrally acting a2 think....

decrease in sympathetic outflow
decrease in sympathetic tone

72

muscarinic think....

increase body fluids

73

how do B2 and mAchR act on sm m surrounding organs

B2=relax
mAchR= contract

74

What type of receptor is the Dopamine receptor

GPCR

75

how many types of DA receptors are there

five

76

DA activates the D1 receptors in _______ whcich increases_____ and causes _____

renal sm. m
CAMP
dilation

77

stimulation of the D1 receptor will result in

vasodilation, natriuresis and diuresis (via renal vascular smooth muscle)

78

At higher concentrations DA can activate _____ and ____ receptors to cause ______ and _______

alpha 1
beta 1
general vascular vasoconstriction
increase in HR

79

decreased sweating cause

increased temperature

80

Smooth muscle of blood vessels is innervated by

sympathetic neurons
NOT parasympathetic neruons

81

how does vascular relaxation happen

need an intact epithelium
stumuli - Ach, physical stimuli, and vasoactive products of inflammation and platelet aggregation (bradykinin, histamine, serotonin, purines, thrombin)
endothelial cells release nitric oxide, which acts on sm m cells
causes vasodilation

Ach activates a mAchr in this scenario

82

three exceptions of mAchRs causing contraction

intestines
urinary bladder
vasculature

83

Baroreceptor reflex

need to add slides for this section but i dont GAFRN

84

Rule of thumb - Alpha 1

stimulate contraction of all smooth muscle
(vascular sm m= vasoconstriction; glandular sm m= secretion)

85

Rule of thumb - Beta2

relax smooth muscle
(vascular sm m - vasodilation)

86

Rule of thumb - muscarinic receptors

contract smooth muscle

87

Increase BP causes ______ baroreceptor firing leading to ______

increased
decrease in sympathetic output
increase in parasympathetic output

88

decreased BP leads to_______baroreceptor firing, resulting in _______

decreased
increase sympathetic discharge
decrease parasympathetic discharge

89

ordinary pressor doses of NE in a normal subject produce

increase in peripheral vascular resistance, increase in MAP and

slowing of the heart rate (compensatory response from reflexes)