Drugs and receptors Flashcards

1
Q

what is a receptor

A

part of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to ligand observable effects

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2
Q

what classes of chemicals can receptors communicate with

A

Neurotransmitters
Autacoids
Hormones

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3
Q

What type of receptors are there

A

Ligand gated ion channels

G protein-coupled receptors

Kinase linked receptors

Cytosolic/nuclear receptors

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4
Q

What are G protein-coupled receptor? (GPCR)

A

Family of proteins involved in transmitting signals from GPCR’s

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5
Q

what binds to and hydrolised GTP and GDP (guanine triphosphate + Guanine diphosphate

A

G proteins (gioamome. nucleotide-binding-proteins)

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6
Q

what is a kinase

A

Enzymes that catalyse the transfer of phosphate groups

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7
Q

What is a nuclear receptor and how do they worl

A

Steroid hormone receptors

Worryk by modifying gene transcription

has zinc fingers that bind to DNA

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8
Q

what type of cancer is tamoxifen used

A

Estrogen receptor+ cancers

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9
Q

give an example where an inbalance in chemicals can lead to a pathology

A

Allergy –> inc histamine

Parkinsons –> reduced histamine

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10
Q

Give and example where an imbalance in receptor can lead to a pathology

A

Myasthenia gravis – loss of ACh receptors

Mastocytosis –> increased c-kit receptor

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11
Q

What is an agonist

A

a compound that binds to a receptor and activated it

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12
Q

what is an antagonist

A
  • A compound that reduces the effect of an agonist
  • Affinity but not efficacy
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13
Q

give the equation for intrinsic activity

A

intrinsic activity = Emax of partial agonist / Emax of full agonist

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14
Q

What does intrinsic activity mean

A

the ability of a drug-receptor complex to produce a maximum function response

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15
Q

what is selective agonism

A

potency of a range of agonists

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16
Q

What is selective antagonism

A

competitive antagonists

17
Q

is nicotine nad agonist or antagonist

A

agonist

18
Q

What are all the histamine receptors characterized as

A

H1 = allergy
H2 - Gastric acid secretion
H3 = Monstly CNS disorders (narcolepsy, ADHD, alzheimers)
H4 = immine system and inflammatory conditions (asthma, arthritis)

19
Q

wgat is effacacy

A

Described how well a ligand activates the receptor

20
Q

T/F agonists have no affinity but have effacacy

A

F
Agonists Have affinity and efficacy

21
Q

T/F antagonists have affinity but no efficacy

A

T

22
Q

what is an irreversible antagonist

A

irreversibly dound to a receptor

23
Q

Define inverse agonism

A

drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of an agonist

24
Q

Describe tolerance

A

-Reduction in agonist effect over time
-continuously, repeatedly, high cons

25
Q

Descripe desensitization

A

Uncouples, internalized, degraded

26
Q

what are the passive ion transporters

A

Symporters and channels

27
Q

What are the active ion treansporter

A

ATP-ases

28
Q

Competitive agonists are
a) Surmountable and irreversible
b)surmountable and reversible
c)insurmountable and irreversible
d)insurmountable and reversible

A

b

29
Q

Non competetive agonists are
a) Surmountable and irreversible
b)surmountable and reversible
c)insurmountable and irreversible
d)insurmountable and reversible

A

C

30
Q

what is the difference between a Full, partial and Inverse AGONIST

A

Full agonist: high efficacy, produces** full respons**e while occupying a relatively low amount of receptors. **Affinity but efficacy
**
-Partial agonist: lower efficacy than a full agonist. It produces sub-maximal activation even when occupying the total receptor population; therefore cannot produce the maximal response, irrespective of the concentration applied. Won’t reach eMax

-Inverse agonist: effect opposite to that of an agonist, yet **binds to the same receptor binding site as an agonist **

31
Q
A