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Pharm Block 9 > Receptors > Flashcards

Receptors Flashcards

1
Q

Purpose is to approve or reject applications from drug companies to market new drugs; old drugs which fail to meet, purity, safety or efficacy standards may be removed from the market

A

FDA

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2
Q

Purpose is to establish a balance between legitimate medical needs while minimizing the availability of the drug for abuse

A

DEA

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3
Q

Regulates the manufacture, distribution, dispensing, use and possession of all CNS drugs with abuse potential with the exceptions of alcohol and tobacco

A

1970-comprehensive drug abuse, prevention and control act

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4
Q

What schedule class has the highest potential abuse?

A

C-1

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5
Q

What drugs are included in C-1 drugs

A

Heroin, LSD, marijuana, mescaline, PCP….illegals

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6
Q

What drugs are common in C2

A

Morphine and methylphenidate

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7
Q

What class does Tylenol #3 belong to

A

C-III

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8
Q

What class are benzodiazepines part of

A

C-IV

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9
Q

Which class has the least abuse potential

A

C-V

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10
Q

What class are gabapentin and some codeine-containing cough syrups part of

A

C-V

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11
Q

What is a true receptor

A

Elicits a biological response when bound by an agonist

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12
Q

Receptor ligand binding theory

A

Drug molecule and biological target must come together (don’t act at a distance, must result in selective binding

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13
Q

What are most receptors

A

Proteins

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14
Q

When a drug binds and there is no detectable changes in function of the biological system

A

Insert binding sites

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15
Q

Ionization and binding

A

It can affect binding

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16
Q

Physical characteristics of drugs

A

Solid
Liquid
Gas

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17
Q

Drug size

A

Related to specificity for a receptor and movement within the body

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18
Q

What is the order of bonds from strongest to weakest?

A 
Covalent 
Ionic 
Hydrogen 
Dipole-dipole 
Hydrophobic
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19
Q

What is the order of bonds from selective to not so selective

A 
Hydrophobic
Dipole-dipole
Hydrogen 
Ionic 
Covalent
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20
Q

Which drugs are usually more selective?

A

Drugs which bind via weak bonding to their receptors. They have less places to bind to

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21
Q

__________ is crucial for proper binding (lock and key)

A

Drug shape

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22
Q

What aspect of drug shape is most important

A

Chirality

-mirror images, but nonsuperimposable

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23
Q

What are two examples of ion channel receptors

A
  • ligand gated ion channels

- voltage gated ion channels

24
Q

Examples of ligand gated ion channels

A

Nicotinic Ach receptors
Glutamate receptors
GABA receptors

25
Q

Where are nicotinic Ach receptors found

A
  • ligand-gated ion channel

- found on muscle cell end plate NM junction, at all autonomic ganglia, in the CNS

26
Q

How do nicotinic Ach receptors open the channel

A

Binding of 2 molecules of Ach opens channel, both alpha subunits must be occupied

27
Q

Prolonged Ach contact with nicotinic receptor

A

Desensitization

28
Q

How many subunits on nicotinic Ach receptor

A

5, alpha subunit must bind 2 Ach

29
Q

Main excitatory NT in the CNS

A

Glutamate

30
Q

What kind of receptors are glutamate receptors

A

Either ligand-gated ion channels (ionotropic) or G-protein coupled (metabotropic)

31
Q

Glutamate agonists

A

AMP, kainite, and N-methyl-D-aspartate (NMDA)

32
Q

What kind of glutamate receptors are plugged with Mg2+ until depolarization?

A

NMDA

33
Q

What is the primary inhibitory NT of the CNS?

A

GABA

34
Q

What kind of receptors are GABA receptors

A

Inhibitory, hyperpolarization.

Ion channels

35
Q

What are clinical examples of GABA receptors

A

Drugs that treat anxiety and sleep

36
Q

What are voltage gated ion channels not activated by

A

NT

37
Q

Where are voltage gated ion channels present

A

In excitable tissues (cardiac)

38
Q

What do voltage gated Na, Ca, or K channels open in response to

A

Action potentials or something that changes the voltage/membrane potential

39
Q

Receptor binding activated adenylyl cyclase which converts ATP to cAMP: cAMP activated protein kinase A

A

Gs protein

40
Q

Receptor binding inhibits adenylyl cyclase whihc prevents the conversion of ATP to cAMP and therefore the activation of protein kinase A

A

GI proteins

41
Q

Receptor binding activates phospholipase C; phospholipase C releases inositol triphosphate (IP3) and DAG from membrane phosphatidylinositol; IP3 activates Ca2+ and calmodulin-dependent proteins kinases; DAG activates proteins kinase C

A

Gq protein

42
Q

What does IP3 activate

A

Ca2+ and calmodulin dependent protein kinases

43
Q

What does DAG activate

A

Protein kinase C

44
Q

Activates Ca2+ channels, activates adenylyl cyclase

A

Gs

45
Q

Activates K+ channels, inhibits adenylyl cyclase

A

Gi

46
Q

Activates phospholipase C

A

Gq

47
Q

Examples of Gs receptors

A 
B adrenergic (B1, B2, B3)
Dopamine D1 receptors
48
Q

Examples of Gi receptors

A
  • muscarinic M2
  • dopamine D2 receptors
  • alpha2 adrenergic
49
Q

Examples of Gq receptors

A

A1 adrenergic
Muscarinic M3
Muscarinic M1

50
Q

What are receptor tyrosine kinases activated by

A

Growth FACTORs and insulin

51
Q

What are cytokines receptors activated by

A

Growth HORMONE, erythropoietin, interferons

52
Q

How do receptor tyrosine kinases work

A

Have an extracellular ligand binding domain, a single transmembrane domain and in intracellular domain which contains the intrinsic kinase activity for signaling. After ligand binding, receptors dimerize. Phosphorylates itself from ATP, not activated

53
Q

How do cytokines receptors work

A

Similar mechanism to receptor tyrosine kinases, but kinase activity is not intrinsic but rather mediated by the JAK family of proteins. JAK activates STATs by phosphorylation

54
Q

Types of intracellular receptors

A

Steroid hormones and nitric oxide

55
Q

What do steroid hormones do

A

Stimulate transcription of genes by binding to a cytoplasmic receptor

56
Q

Steroid receptor ligand complex inside the cell

A

Transported to the nucleus where transcription is activated

57
Q

Where does nitric oxide come from

A

Endothelial cells, diffuse into smooth muscle

Pharm Block 9 (7 decks)

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