Long Slide Part 2

Question 1

Binding of drugs in —— binding domain induces —— changes, alter distribution of charges and transmitted to —— domain to be transmitted to —— domain

Answer 1

Ligand
Confirmational
Coupling
Effector

Question 2

Binding can be specific and irreversible. T/F

Answer 2

False it’s reversible

Question 3

Binding or interaction of drug-receptor is by what means?

Answer 3

Chemical bonds

Question 4

Ligands bind to?

Answer 4

Receptors

Question 5

Individual receptors have the same amino acid sequencing. T/F

Answer 5

False. They are different

Question 6

Examples of Acetylcholine

Answer 6

Muscarinic and Nicotinic

Question 7

Examples of Muscarininc receptor subtypes

Answer 7

M1, M2, M3, M4, M5

Question 8

Examples of Nictotinic receptor subtypes

Answer 8

Nm and Nn

Question 9

What is the oldest and classical criteria of classification of receptors based on potencies of selective agonist and agonists. Give examples

Answer 9

Muscarinic
Nicotinic
Alpha and Beta adrenergic

Question 10

Measurement of specific binding of high affinity radio labeled ligand to cellular fragments usually membranes in vitro and it’s selective displacement by various selective agonist/antagonists is used to delineate receptor subtype. This Criteria of classification is under?

Give me examples

Answer 10

Ligand binding

Multiple 5-HT receptors were distinguished by this approach

Question 11

In what receptor criteria is a receptor subtypes distinguished by the mechanism through which their activation is linked to the response?

Give examples

Answer 11

Transducer pathway

M cholinergic receptors act through G-proteins
N cholinergic receptor gates influx of sodium ions

Question 12

The cardiac receptor is beta adrenergic receptor as beta 2. T/F

Answer 12

False it’s Beta 1

Question 13

The bronchial adrenergic receptor is Beta 2. T/F

Answer 13

True

Question 14

Receptors without known ligands are called?

Answer 14

Orphan receptors

Question 15

The receptor protein is cloned and it’s amino acid sequence as well as three dimensional structure is worked out. What type of Receptor Criteria is this?

Answer 15

Molecular cloning

Question 16

What Receptor Criteria approach led to flood of receptor subtypes and several isoforms?

Answer 16

Molecular cloning

Question 17

Receptors are regulatory binding sites capable of ———

Answer 17

Generating a response

Question 18

What kind of receptors bind drugs to them with no pharmacological response?

Answer 18

Silent receptors

Question 19

What type of receptors are called drug acceptors or sites of loss?

Answer 19

Plasma proteins

Question 20

Silent receptors are also called?

Answer 20

Drug acceptors or Sites of loss

Question 21

What Receptor Criteria can you find receptors without known ligands?

Answer 21

Molecular cloning

Question 22

What kind of receptor can produce maximal response when even less than 1% of the receptor is occupied?

Answer 22

Spare receptors

Question 23

Depletion of noradrenaline/treatment with adrenergic antagonists results in?

Answer 23

Super-sensitivity of tissues to noradrenaline and your increase in receptor number

Question 24

Administration of beta blocker causes a decrease in adrenergic receptors. T/F?

Answer 24

False. It causes an increase

Question 25

What is up regulation?

Answer 25

Increase in number of receptors and subsequent increase in receptor sensitivity

Question 26

What is reduction in number of receptors available for activation known as?

Answer 26

Down regualtion

Question 27

Continued exposure to drugs/agonist can result in?

Answer 27

Desensitization, tolerance, refractoriness

Question 28

Down regulation of receptors leads to?

Answer 28

Decreased No of receptors Reduced affinity to drug

Question 29

Repeated administration of Adrenergic agonist in asthma leads to down regulation of beta receptors. T/F

Answer 29

True

Question 30

I’m Myasthenia Gracias autoantibodies inactivate what?

Answer 30

Nicotinic acetylcholine receptors

Question 31

Autoantibodies can also mimic the effects of antagonists. T/F

Answer 31

False. Agonist

Question 32

What an example of a case where autoantibodies mimic the effects of agonist?

Answer 32

Thyroid hyper-secretion caused by activation of thyrotropin receptors

Question 33

Mention the receptor related diseases

Answer 33

Testicular feminisation Insulin resistant diabetes Familial hypercholesterolaemia

Question 34

Most transmembrane signaling is accomplished by a large number of different molecular mechanisms. T/F

Answer 34

False! It’s small

Question 35

What are the four major categories of transducer mechanism?

Answer 35

GPCR Receptors with intrinsic ion channel Enzyme linked receptors Transcription factors(receptors for gene expression)

Question 36

What receptors mediate the majority of cellular responses to external stimuli?

Answer 36

GPCR

Question 37

Ligand binding and channel opening occur on a millisecond timescale so they are confirmed to excitable tissues. What are those excitable tissues?

Answer 37

CNS NMJ Autonomic ganglia

Question 38

Receptors mediate diverse functions such as?

Answer 38

NT Cardiac conduction Muscle contraction

Question 39

Stimulation of Nicotinic receptor by Ach results in ———

Answer 39

Na influx Generation of AP Activation of skeletal muscle contraction

Question 40

What enhances the stimulation of GABA, resulting in increased Chloride influx and hyper-polarization of the respective cell?

Answer 40

Benzodiazepines