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Pharmacology > Drugs and Receptors > Flashcards

Drugs and Receptors Flashcards

1
Q

Durggability

A

Whether a protein has the capacity to be a target/ have high affinity to a drug

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2
Q

Give examples of proteins that are drug targets?

A

Receptors
Enzymes
Transporters
Ion channels

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3
Q

What is a receptor?

A

Component of cell that interacts with a specific ligand, intitiates change of biochemical events

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4
Q

Examples of autacoids (2self”-“relief”)

A

Cytokines, histamine

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5
Q

Types of receptors

A

Ligand-gated ion channels
G protein coupled receptors
Kinase-linked receptors
Cytosolic/nuclear receptors

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6
Q

Example of ligand-gated ion channels

A

Nicotinic ACh receptor

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7
Q

Ion channels are pore-forming m_____ proteins, causing electric charge distribution

A

membrane

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8
Q

Example of G protein coupled receptor

A

Beta-adrenoreceptors

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9
Q

G proteins (AKA guanine nucleotide-binding proteins) activity is regulated by factors that control their ability to bind to and h______ guanosine triphosphate (GTP) to guanosine diphosphate (GDP)

A

hydrolyse

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10
Q

Example of Kinase-linked receptors

A

Receptors for growth factors

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11
Q

Kinases are enzymes that catalyse transfer of phosphate groups between proteins, process called p_______

A

phosphorylation

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12
Q

Example of cytosolic/nuclear receptors

A

Steroid receptors

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13
Q

Nuclear receptors work by modifying gene t_______

A

transcription

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14
Q

Tamoxifen (breast cancer drug) acts as a selective o_____ receptor modulator or as a partial agonist of the o_____ receptors

A

oestrogen

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15
Q

Give an example of too much of a molecule causing a disease

A

Histamine and allergic reaction

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16
Q

Give an example of too little of a molecule causing a disease

A

Reduced dopamine, Parkinson’s

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17
Q

Either an imbalance of chemicals or r____ can cause disease

A

receptors

18
Q

Agonist

A

A compound that binds to a receptors and activates it

19
Q

Antagonist

A

A compound that reduces the effect of an agonist

20
Q

Receptor ligands

A

A molecule that binds to another usually larger molecule

21
Q

What model describes how drugs activate receptors via a conformational change of receptor from “off” to “on”?

A

The two state model

22
Q

Potency - what is EC50?

A

The concentration that gives half the maximal response

23
Q

Efficacy (Emax)

A

The maximum response achievable

24
Q

Intrinsic activity (IA) or efficacy refers to the ability of a drug-receptor complex to produce a maximum f____ response

A

functional

25
Q

Cholinergic receptors respond to n__________

A

neurotransmitters

26
Q

What the 2 categories of cholinergic receptors?

A

Nicotinic (n) and muscarinic (m)

27
Q

What is the antagonist for the agonist muscarine which acts on the receptor mAChR?

A

atropine

28
Q

What is the antagonist for the agonist nicotine which acts on the receptor nAChR?

A

curare

29
Q

Affinity

A

How well a ligand binds to the receptor, property shown both agonists and antagonists

30
Q

Efficacy

A

Describes how well a ligand activates the receptor

31
Q

Antagonists have zero e_____

A

efficacy (doesn’t activate the receptor)

32
Q

Receptor reserve is the phenomenon in which an agonist produces the m_____ response by activating only a fraction of the available receptor population present in the system

A

maximal

33
Q

What are 2 tissue-related factors that govern drug action?

A

Number of receptors, signal amplification

34
Q

What are 2 receptor-related factors that govern drug action?

A

Affinity and efficacy

35
Q

What is inverse agonism?

A

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

36
Q

True or false: no compound is every truly specific?

A

True

37
Q

What word is used instead of specific

A

Selective

38
Q

Is salbutamol a selective or non-selective B-adrenoreceptor agonist?

A

Selective

39
Q

Isoprenaline, a drug used for bradycardia and heart block is a selective/ non-selective B-adrenoreceptor agonist?

A

Non-selective

40
Q
A

Pharmacology (9 decks)

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