ANS Receptors and Drug Targets Flashcards

1
Q

M1 receptor mechanism

A

Gq protein - STIMULATORY

activate PLC –> convert PIP2 –> IP3 + DAG –> increase Ca2+

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2
Q

M1 receptor locations

A

brain, salivary glands

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3
Q

M1 receptor effects

A

increase secretions

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4
Q

M2 receptor mechanism

A

Gi protein - INHIBITORY

inhibit AC –> decrease cAMP

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5
Q

M2 receptor locations

A

heart
lugns
smooth muscle
presynaptic neurons

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6
Q

M2 receptor effects

A

decrease HR/contractility
bronchoconstriction
smooth muscle contraction
autoinhibition of synapses

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7
Q

M3 receptor mechanism

A

Gq protein - STIMULATORY

activate PLC –> convert PIP2 –> IP3 + DAG –> increase Ca2+

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8
Q

M3 receptor locations

A

pupils
detrusor muscle
lungs

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9
Q

M3 receptor effects

A

miosis
detrusor contraction –> urine release
bronchoconstriction

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10
Q

a1 receptor mechanism

A

Gq protein - STIMULATORY

activate PLC –> convert PIP2 –> IP3 + DAG –> increase Ca2+

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11
Q

a1 receptor locations

A

blood vessels
pupils
smooth muscle
internal urethral sphincter
CNS

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12
Q

a1 receptor effects

A

vasoconstriction
hypertension
mydriasis
smooth muscle contraction
internal urethral sphincter contration –> urinary retention
increased alertness/excitement

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13
Q

a2 receptor mechanism

A

Gi protein - INHIBITORY

inhibit AC –> decrease cAMP

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14
Q

a2 receptor locations

A

presynaptic neurons
CNS (locus coeruleus)
heart
blood vessels
endocrine

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15
Q

a2 receptor effects

A

autoinhibition of synapses

a2 agonists:
sedation, amnesia, analgesia, muscle relaxation
decrease HR
high dose: vasoconstriction/hypertension
low dose: vasodilation/hypotension
inhibit ADH –> increased urination
inhibit insulin –> hyperglycemia

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16
Q

B receptor mechanism

A

Gs protein - STIMULATORY

stimulate AC –> increase cAMP

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17
Q

B1 receptor locations

A

heart

18
Q

B1 receptor effects

A

increase HR and contractility

19
Q

B2 receptor location

A

blood vessels
lungs
smooth muscle

20
Q

B2 receptor effects

A

vasodilation/hypotension
bronchodilation
smooth muscle relaxation

21
Q

B3 receptor location

A

detrusor muscle

22
Q

B3 receptor effects

A

detrusor muscle relaxation –> urinary retention

23
Q

D1 receptor mechanism

A

Gs protein - STIMULATORY

stimulate AC –> increase cAMP

24
Q

D1 receptor location

A

blood vessels

25
Q

D1 receptor effects

A

vasodilation
increases blood flow

26
Q

D2 receptor mechanism

A

Gi protein - INHIBITORY

inhibit AC –> decrease cAMP

27
Q

D2 receptor location

A

CNS
CRTZ

28
Q

D2 receptor effects

A

emesis
induce anxiety and fear

29
Q

u/k opioid mechanism

A

Gi protein - INHIBITORY

inhibit AC –> decrease cAMP

30
Q

u/k opioid location

A

periphery/spinal cord interneurons
CNS
respiratory centers
GI

31
Q

u/k opioid effects

A

analgesia
sedation (dogs)
euphoria (cats, low dose)
excitement (cats/horses, high dose)
hypoventilation
decreased peristalsis

32
Q

benzodiazepine mechanism

A

binds y subunit of GABAa receptor

opens Cl- pore to hyperpolarize cell

33
Q

benzodiazepine locations

A

CNS
hippocampus
skeletal muscle

34
Q

benzodiazepine effects

A

sedation (sheep, goats, cattle, pigs)
excitement (dogs, cats, horses)
anticonvulsant
amnesia
muscle relaxation

35
Q

anesthetic GABAa mechanism

A

binds to a or b subunit

36
Q

anesthetic GABAa locations

A

CNS
hippocampus
skeletal muscle
respiratory

37
Q

anesthetic GABAa effects

A

anesthesia
hypoventilation
sedation (sheep, goats, cattle, pigs)
excitement (dogs, cats, horses)
anticonvulsant
amnesia
muscle relaxation

38
Q

NMDA receptor mechanism

A

binds to glutamate receptor to open cation pore to depolarize cell

39
Q

NMDA receptor locations

A

CNS
hippocampus
periphery & spinal cord
skeletal muscle

40
Q

NMDA receptor effects

A

mediates pathways between brainstem and cortex
memory formation
modulates pain pathways
inhibits UMNs of skeletal muscle