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MTP > Exam 2: Receptors and Drug-Receptor Interactions > Flashcards

Exam 2: Receptors and Drug-Receptor Interactions Flashcards

1
Q

Is a receptor stereometric?

A

No, receptor does not have an enantiomer of itself therefore it’s static

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2
Q

What is stereoiosomerism?

A

A carbon atom with 4 different substituents that doesn’t posses a plane or point of symmetry

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3
Q

What make a molecule symetrical?

A

Carbon contains 2 or more of the same substituents of a plane or point of symmetry

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4
Q

How are the substituents of a carbon sorted?

A

From highest to lowest molecular weights

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5
Q

What are enantiomers?

A

Nonsuperimposible molecules that are mirror images

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6
Q

Identify the relationship of these 2 molecules

A

Enantiomers

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7
Q

Identify the relationship of these 2 molecules

A

Enantiomers

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8
Q

Identify the relationship of these 2 molecules

A

Enantiomers

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9
Q

What are diastereomers?

A

Nonsuperimposible molecules that have the same molecular formula however are not mirror images

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10
Q

Identify the relationship of these 2 molecules

A

Diastereomers

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11
Q

Identify the relationship of these 2 molecules

A

Diastereomers

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12
Q

What are E-Z isomers?

A

Pertains to alkene carbons

E: high and low priority groups on both sides

Z: same priority group on either sides

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13
Q

Identify the relationship of these 2 molecules

A

E-Z isomers

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14
Q

Define occupancy theory

A

The prediction of a response that is related to the number of receptors are bound by an agonist

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15
Q

According to the occupancy theory, how do we create a greater response?

A

Having more drugs bound to the receptor to where receptors become saturated

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16
Q

What is the rate theory?

A

The number of drug-receptor interactions per unit time determines the intensity of the response

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17
Q

According to rate theory, how do we create a greater response?

A

Drugs that associate with then rapidly dissociate from the receptor, allowing another drug molecule to interact with the receptor

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18
Q

What is the induced-fit theory?

A

The drug approached the receptor a conformational change occurs in the receptor to allow for effective binding

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19
Q

Describe the shape of a receptor in regards to induced-fit?

A

Receptor does not normally exist in the proper conformation for drug binding, when a drug dissociates the the receptor revert to its original form

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20
Q

What is macromolecular perturbation theory?

A

Suggests that 2 types of conformational changes exist and the rate of their existence determine the observed biological response

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21
Q

What are the conformational changes that occur for macromolecular perturbation theory?

A
  1. Agonist produces a specific form for biological response
  2. Antagonist produce non-specific forms that fails to produce a response
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22
Q

What is activation-aggregation theory?

A

Receptors are always at equilibrium between active and inactive forms

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23
Q

How does agonists and antagonist shift equilibrium?

A

Agonists: Shift it towards active state

Antagonists: shift it towards inactive states

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24
Q

How does a drug-receptor complex form?

A

The solvent molecule on the receptor is displaced by drug to produce a solvated complex

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25
What make a solvated complex effective?
Interactions between drug and receptor must be stronger than interactions with the solvent
26
Why are drug-receptor complex formation entropically unfavored?
1. Causes a loss in conformational degrees of freedom form ligands and proteins 2. Causes a loss of 3 rotational and 3 translations degrees of freedom
27
How do drug-receptor complexes compensate for being entropically unfavored?
Highly favorable enthalpic interactions between drug and receptor
28
What bond is considered a strong bond?
Covalent due to its irreversibility
29
What makes a drug inactivate?
When the concentration in the extracellular fluid decreases, drug-receptor binding are irreversible due to weak non-covalent interactions
30
Why is it important for drugs to be irreversible?
Desired drugs are predictable and pharmacological action can be terminated after a limited time
31
In what cases are drugs irreversible?
1. Chemo to kill tumor cells 2. Antibiotics to kill bacteria
32
What is a covalent bond?
A chemical bond formed by sharing a pair of electrons (suicide inhibitors)
33
What are ionic interactions?
Drug and receptor groups will be mutually attracted provided they have opposite charge
34
What makes an ionic interaction beneficial?
Effective at further distances compared of IM forces
35
What makes a dipole weaker than an ion?
Dipole charge is less than an ion
36
What is a hydrogen bond?
Formed between the H+ and an electronegative atom (SNO)
37
What is the difference between inter and intramolecular bonds?
Inter: interactions between 2 molecules Intra: interactions in a single molecule
38
What is a charge-transfer complexes?
When a molecule that is a good electron donor comes into contact with a molecule that is a good electron acceptor, the donor may transfer some of its charge to the acceptor creating a molecular dipole-dipole interactions
39
What type of molecules can achieve charge-transfer complexes?
Donor groups containing pi electrons
40
What are hydrophobic interactions?
When water molecules orient themselves around the molecule and are in a higher energy state in the presence of a nonpolar region of molecule
41
What is the behavior of 2 nonpolar molecules in contact?
Nonpolor dissolve together (not attracted) by their decrease in free energy due to the increased entropy of water molecules
42
What are van der waals?
Non polar molecules that have a temporary nonsymmetrical distribution of electron density (temporary dipole)
43
What make a van der waal weak?
Only significant when there is a close surface contact of atoms
44
Identify the potential interactions of the drug
A: Hydrophobic B: H-bond C: Ion or ion-dipole D: Hydrophobic E: Hydrophobic F: Dipole-dipole or H-bond G: Hydrophobic H: Charge-transfer or H-bond
45
What is spatial arrangement?
The location of functional groups about their molecular scaffold and their proximity to thei interaction site within the receptor
46
What is a pharmacophore?
The minimum structural requirements of a molecule that will be recognized by a receptor and possess a specific activity
47
What make antihistamine molecules similar?
They have specific binding sites on the H1 receptor that have an appropriate topography for interactions with certain groups
48
What make an antihistamine different from a histamine molecule?
It is an H1 antagonist containing a tertiary amino group what will is protonated at physiological pH creating an ionic bond between drug and receptor
49
Describe how two enantiomers become diasteriomers when bound to a receptor?
Receptors are static and molecule will have different binding properties
50
What configuration do all human amino acids come in?
L
51
In what ways do enantiomeric drugs have varying degrees of activity?
1. One enantiomer may possess activity while the other might be completely inactive 2. Both enantiomer may have equal effect 3. Most often, both enantiomer will demonstrate some activity with one enantiomer demonstrating activity to a much higher degree
52
What is an eutomer?
The more potent isomer
53
What is a distomer?
The less potent isomer
54
What is a eudismic ratio?
The ratio of more potent (higher affintiy) enantiomer to the less potent enantiomer
55
What type of enantiomer has the highest degree of receptor complementary?
Highly potent antagonist
56
When are high eudismic ratio observed?
In stereoisomers typically found in antagonists because receptors can not hold distomers
57
When are low eudismic rations observed?
When eutomer has a lower affinity for the receptor or when the stereogenic centers lies outside the region of critical receptor binding
58
What are isomeric ballast?
Distomer that are considered as an impurity in a mixture that can contribute to adverse reactions
59
What are the dangers of racemic mixtures?
One enantiomer may antagonize the other and no effect will be observed
60
What is a hybrid drug?
A type of compound with 2 separate mechanisms of action and therapeutic activities
61
What are psedo-hybrid drugs?
When multiple isomeric forms are involved in the biological activity
62
What are the stereoisomeric forms?
RR, SS, RS, SR
63
What are RR isomers of antihypertensives used for?
Beta-blocking activity
64
What are SR isomers of antihypertensives used for?
Alpha-blocking activity
65
What are SS and RS of antihypertensive used for?
Completely inactive, the isomeric ballast
66
Why are isomeric ballast not typically removed for economic reasons?
1. Separation of enantiomers is very difficult and time consuming 2. Separation of all isomers lowers the overall yield of the active component
67
What is a racemic switch?
A single-entity drug of one enantiomer
68
What are the advantages of single isomers?
1. Lower effects and toxicity 2. Half of racemate dose to achieve maximum therapeutic effect 3. Can increased the dose of purified racemate if max effect was not observed
69
What are the disadvantages of single isomers?
1. Dosing a single enantiomer can cause unobserved side effect that other enantiomer was masking 2. Can cause a lower effect than expected from the racemate
70
What does this picture indicate?
Enantiomeric binding selectivity
71
What makes drug more potent?
The more bonds its able to make with the receptor
72
What does this picture tell you about the drug?
The E form is more potent than the Z form because its ability to bind to the receptor. E is the eutomers.
73
What are rotamers?
A set of isomeric conformers of a drug molecule
74
What are bioactive conformation?
A receptor may bind only one of the conformers
75
What makes a conformational isomer?
1. Free rotation about single bonds providing conformational flexibility 2. Variety of conformations in space without breakage of bonds
76
What is the favorable conformational isomer (bioactive conformation)?
The molecule that exists in its lowest energy state
77
What can prevent molecules from assuming their lowest energy state?
Intramolecule h bond

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