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Medicinal Chemistry > Drug Receptor Interaction > Flashcards

Drug Receptor Interaction Flashcards

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1
Q

Define drug

A
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2
Q

Define receptor

A
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3
Q

Define ligand

A

Molecule that binds to a receptor

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4
Q

What are the types of ligands?

A

Endogenous → neurotransmitter, hormone
Exogenous → pharmaceutical drugs, toxins

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5
Q

Cell membrane is made up of what?

A

Phospholipid bilayer

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6
Q

The hydrophobic tails interact how?

A
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7
Q

The polar head groups interact how?

A
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8
Q

What floats in the membrane ?

A

Proteins

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9
Q

Proteins can act as what

A

Ion channels
Carriers

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10
Q

List the drug targets

A
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11
Q

Drug targets are what

A

Large molecule - macromolecules

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12
Q

How do drugs interact with their targets?

A

By binding to binding sites

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13
Q

Binding sites are typically what?

A

Hydrophobic pockets on the surface of macromolecules

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14
Q

Binding interactions typically involve what?

A

Intermolecular bonds

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15
Q

Most drugs are in equilibrium between what?

A

Being bound and unbound to their target

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16
Q

Define binding regions

A

Specific regions within the binding site that are involved in binding interactions

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17
Q

Define binding groups

A

Functional groups on the drug involved in binding interactions with the binding regions

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18
Q

List the intermolecular bonds

A

Electrostatic/ ionic bond
Hydrogen bond
Dipole - dipole interaction
Van der Waals forces

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19
Q

Ionic bond takes place between what ?

A

Between groups of opposite charge either on the drug site or receptor site

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20
Q

Strength of the ionic bond is what ?

A

Inversely proportional to the distance between the two charged groups

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21
Q

In which intermolecular bonding the strength of interaction drops off less rapidly with distance that with other forms of intermolecular bonding

A

Electrostatic/ ionic bond

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22
Q

Hydrogen bond takes place between what?

A

Between an electron deficient hydrogen and an electron rich hetero atom

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23
Q

hydrogen bond donor is

A

Electron deficient hydrogen

24
Q

Hydrogen bond accepter is

A

Electron rich heteroatom

25
Q

Give examples of strong hydrogen bond acceptors

A
26
Q

Give examples of moderate hydrogen bond acceptors

A

Carboxylic acid
Amide oxygen
Ketone
Ester
Ether
Alcohol

27
Q

Compare doxycycline and tetracycline

A
28
Q

Dipole-dipole interaction occurs how ?

A
29
Q

What happens with the strength of the interaction with distance?

A
30
Q

Van der waals forces occur how ?

A
31
Q

What is the phenomenon of chelation significantly involved in?

A

Biological system and to some extent in explaining drug action

32
Q

Numerous enzyme system contain what?

A

Metal ions chelated to them

33
Q

What is EDTA

A
34
Q

What is used in the treatment of lead and vanadium poisoning ?

A

EDTA

35
Q

In blood samples EDTA is used for what ?

A

To prevent clotting by chelating with Ca++ ions

36
Q

Define affinity

A

Measures the attractiveness of a drug to a receptor

37
Q

Define efficacy

A

The ability of a drug to produce a biological response as a result of its interaction with the receptor

38
Q

What are the two types of drugs

A

Agonist
Antagonist

39
Q

Define agonist

A
40
Q

Define antagonist

A
41
Q

How does a drug bind to a receptor

A
42
Q

Binding results in what?

A

In an induced fit of that receptor

43
Q

Describe the induced - fit mechanism

A
44
Q

What are the two types of chemical messengers

A

Neurotransmitters
Hormones

45
Q

Define neurotransmitters

A
46
Q

Define hormones

A
47
Q

Induced fit of the protein results in what?

A

Domino effect

48
Q

Domino effect is known as what

A

Signal transduction, leading to a chemical signal being received inside the cell

49
Q

Binding interactions must be what ?

A
50
Q

What are the types of signal transduction/ types of receptors

A
51
Q

Explain the action of ligand gated ion channels

A
52
Q

Explain the action of kinase linked receptors

A
53
Q

Explain the activation of G-protein

A
54
Q

What are the factors that need to be considered in drug design

A
55
Q

How to design an agonist ?

A

Medicinal Chemistry (11 decks)

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