cellular receptors and drug action Flashcards

1
Q

if a receptor is inside the cell, what kind of endogenous ligand is it going to have

A

it means that the endogenous liagnd is fat soluble, this is because the fat soluble can pass the inside of the cell

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2
Q

intracellular receptor

A

inside the cell, the endogenous ligand is very small and fat soluble

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3
Q

intracellular receptors directly effect what

A

our DNA

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4
Q

spanning enzymes

A

insulin - the receptor is located inside the membrane

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5
Q

receptor located on a ion channel

A

binds to receptor, ion channel opens, causing an influx of molecules

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6
Q

g-protien coupled receptors

A

they stimulate effectors to produce intracellular changes

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7
Q

what g-protiens subgroups exist

A

gs, gi, gq

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8
Q

what receptors interact with g protiens

A

light, odorants, hormones, neurotransmitters, and prostaglandins

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9
Q

what effectors are associated with the cAMP signal transduction pathway

A

adenylyl cyclase

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10
Q

what are gs and gi always affecting

A

adenylyl cyclase

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11
Q

what happens when adenylyl cyclase is activated

A

it turns ATP into AMP then CAMP

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12
Q

phospholipase C

A

only associated with gq

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13
Q

phospholipase C is associated with what signal transduction pathway

A

phsophatidylinositol

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14
Q

PIP yields how many messangers?

A

2 - IP3 and DAG

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15
Q

what is IP3 and DAG - what changes do they lead to

A

these are secondary messangers in the cell that lead to physiological changes

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16
Q

what 2nd messengers come from the cAMP signal transduction pathway

A

cAMP

17
Q

what is the endogenous ligand for the muscarinic receptor

A

potassium

18
Q

how does heart rate slow down through the signal transduction pathway

A

acetylcholine binds to muscarinic receptor, g protien is stimulated, potassium channel opens slowing heart rate

19
Q

gs protien and activation of protien kinases

A

gs stimulates adenylyl cyclase, coverts to atp,Camp activates protien kinases

20
Q

how do protien kinases activate enzymes

A

by adding a phosphate group

21
Q

what effector is associated with gs

A

adenylyl cyclase

22
Q

what does gi protien do

A

inhibits adenylyl cyclase, leads to a decrease in cAMP

23
Q

albuterol and gs protien

A

adenylyl cyclase - increase in cAMP - activation of enzymes, Ca+2, inactivate MLCK, decreased levels of these cause the bronchial relaxation

24
Q

what decreases levels of ca and MLCK

A

increase in cAMP

25
Q

what process is this? adenylyl cyclase - increase in cAMP - activation of enzymes, Ca+2, inactivate MLCK, decreased levels of these cause the bronchial relaxation

A

albuterol (bronchiodialator)

26
Q

adenylyl cyclase increases what levels

A

cyclic AMP

27
Q

name for ventalin

A

salbutamol/albutterol

28
Q

misprosol is linked with what receptor

A

gi

29
Q

gi and misoprostal peptic ulcers

A

Gi binds, inhibit acetylyl cyclase, cAMP production decreases, protien kinases are not activated, enzyme pumps that help produce sotmach acid are blocked, stomach acid decreased

30
Q

what drug also causes uterine contraction

A

misprostoal

31
Q

GQ linked to phospholipase C

A

PLC links to PIP, PIP yields two messangers (IP3 and DAG) IP3 binds to the SR, binding of CA, DAG binds to calcium channels on cell membrane, calcium into cell

32
Q

what process is this? PLC links to PIP, PIP yields two messangers (IP3 and DAG) IP3 binds to the SR, binding of CA, DAG binds to calcium channels on cell membrane, calcium into cell

A

gq and phospholipase c

33
Q

DAG binds to what?

A

binds to calcium channels on the cell membrane facilitating the movement of extracellular calcium into the cell

34
Q

what does IP3 bind to?

A

binds to the SR, stimulating the release of Ca+2 into the cytoplasm

35
Q

ergonovine and Gq protien

A

binds to gq protiens, stimualtes IP3 DAG, release of Ca, induces contraction of the uterus and blood vessels

36
Q

what can ergonovine and gq protiens help with

A

can help to terminate postpartum hemorrhage