02 - Drug receptor interactions (pharmacodynamics) Flashcards

1
Q

Agonists…

A

activate receptors!

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2
Q

Antagonists…

A

block the action of an agonist

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3
Q

Benzodiazepines bind to the ( allosteric / orthosteric ) site of ( GABA A / GABA B / alpha-andrenergic) receptors

A

Allosteric site of GABA A

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4
Q

Benzodiazepines enhance the endogenous…

A

Effect of GABA (leading to greater hyperpolarisation, as more Cl- passes through the ion channel)

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5
Q

NSAIDs work by…

A

Enzyme inhibition

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6
Q

NSAIDs inhibit…

A

Cyclooxegenase

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7
Q

Drugs that mimic the endogenous process at a receptor are acting as…

A

Agonists

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8
Q

Drugs that inhibit the endogenous process at a receptor are acting as..

A

Antagonists

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9
Q

Histamine receptors have at least…

A

14 subtypes

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10
Q

Receptor subtypes may have both different specificities for agonists and differences in the…

A

Signal transduction pathway

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11
Q

The 4 major types of receptor are…

A
  1. Ligand-gated ion channel receptors
  2. G-Protein coupled receptors
  3. Enzyme (kinase) linked receptors
  4. Intracellular receptors
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12
Q

Which type of receptor acts the fastest?

A

Ligand-gated ion channel receptors (ionotropic)

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13
Q

All ionotropic channels have ( intracellular / extracellular ) ligand binding sites

A

Extracellular

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14
Q

G-Protein coupled receptors are slower than ligand-gated ion channel receptors, but have a…

A

Greater variety of responses

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15
Q

G-Protein coupled receptors are the most common…

A

Receptor type and drug target

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16
Q

G-Protein coupled receptors can either be (2)…

A

Direct (linked with an enzyme) or Indirect (triggers an ion channel)

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17
Q

adrenoreceptors are…

A

G-protein coupled receptors

18
Q

Salbutamol is a drug which mimics the endogenous effects of which neurotransmitter on which receptors?

A

Epinephrine, (beta-2) andrenoreceptors

19
Q

A trimeric G-protein is comprised of 3 subunits…

A
  • alpha
  • beta
  • gamma
20
Q

Which G-protein subunit has the most significant catalytic activity?

A

Alpha (which binds GTP)

21
Q

Name the 3 main subtypes of alpha-subunit….

A
  1. Gs (activates adenyl cyclase, Ca2+ channels)
  2. Gi (inhibits adenyl cyclase, activates K+ channels)
  3. Gq (activates phospholipase C)
22
Q

alpha 1 adrenoreceptor activates a G-protein with which alpha subunit type?

A

Gq -> activates phospholipase C

23
Q

alpha 2 adrenoreceptor activates a G-protein with which alpha subunit type?

A

Gi -> inhibits adenyl cyclase and activates K+ channels

24
Q

beta 1 and 2 adrenoreceptors activate a G-protein with which alpha subunit type?

A

Gs -> stimulates adenyl cyclase and activates Ca2+ channels

25
Q

The stimulation of adenyl cyclase via activation of the beta 1 adrenoreceptor results in…

A

Accelerated heart rate

26
Q

The stimulation of adenyl cyclase via activation of the beta 2 adrenoreceptor results in…

A

Broncodilation

27
Q

Salbutamol is a beta 2 adrenoreceptor ( agonist / antagonist)

A

Agonist

leads to broncodilation, used to treat asthma symptoms

28
Q

Atenalol is a beta 1 adrenoreceptor ( agonist / antagonist)

A

Antagonist

lowers heart rate

29
Q

Kinase linked receptors feature a large extra cellular binding site linked to the intracellular domain by a…

A

Single membrane-spanning helix

30
Q

Nuclear receptor binding sites are…

A

Intracellular

So the ligand must cross the cell membrane

31
Q

Nuclear receptors are divided into (2)…

A

Class I and Class II

32
Q

Class I nuclear receptors are found in the…

A

Cytoplasm

33
Q

Class I nuclear receptors form…

A

Homodimers

34
Q

Class I nuclear receptors bind…

A

Endocrine (Steroid, hormone) ligands

35
Q

Class II nuclear receptors are found in the…

A

Nucleus

36
Q

Class II nuclear receptors form…

A

Heterodimers

37
Q

Class II nuclear receptors bind…

A

Lipid (fatty acid) ligands

38
Q

Most receptor operated channels have…

a) a single binding site
b) two binding sites
c) multiple binding sites
d) no binding sites

A

c) multiple binding sites

39
Q

Binding at one site can affect…

A

Binding at other sites

40
Q

The orthosteric site is the…

A

Main binding site

41
Q

Binding at the allosteric site can…

A

Modulate affinity at the orthosteric site (+/-) and bind antagonists

42
Q

Receptors may also have areas known as…

A

Effector regions

Which also effect the receptor