Module 1 Receptors And Genetics

Question 1

Ligand

Answer 1

Molecule or ion that has specific functions causing a biological response

Allows change inside the cell or transmit a signal

Question 2

Receptors Types

Answer 2

Intracellular receptors
1) Steriods

Cell Surface receptors

1) ligand gated ion channels - fast
2) g protein coupled - slow
3) receptors tyrosine kinases

Question 3

Ligand Gated Ion Channels

Answer 3

Lock and key
Neurotransmitters
Ion binding enzyme or voltage channels to exchange, release, or store to produce a response

Question 4

G-Protein Coupled Receptors

Answer 4

1. transmit signals
   GTP active or GDP inactive
2. any disruption of GPCR = DISEASE
3. Has 3 subunits: alpha, beta, gamma

Question 5

Receptor Tyrosine Kinase RTK

Answer 5

1. Enzyme linked to transfer amino acids
2. Responsible for growth factor, platelet derived growth factor (wound healing, nerve growth)
3. Overgrowth of factors = CANCER

Question 6

Agonist

Answer 6

Activates

Natural or synthetic
Full and partial

Question 7

Inverse Agonist

Answer 7

Opposite expected effect

Question 8

Anatagonist

Answer 8

Inactivates / BLOCKs action of other meds

Usually reversible

Question 9

Pharmokinetics

Answer 9

Absorption, Distribution, Metabolism, Elimination

Movement

Question 10

Pharmacodynamics

Answer 10

What the drug does to the body

Question 11

Up regulation

Answer 11

Missing ligand the cell will make more receptors

Question 12

Down regulation

Answer 12

Increase stimulation by a ligand the cell will decrease number of receptors for the specific ligand

Question 13

Acetylcholice

Fast neurotransmittors is what structure receotor type?

Answer 13

Ligand gated ion chanel

Question 14

Slow transmission norepinephrine is what receptor structure type?

Answer 14

G Protein Coupled Receptors

Question 15

Insulin growth factor is what structure type of receptor

Answer 15

Enzyme-linked receptor

Question 16

Steriod hormones and thyroid hormone is what structure receptor type?

Answer 16

Nuclear receptors

Question 17

Alpha receptors subtypes a1 a2

Answer 17

a1: vascular smooth muscle, GU smooth muscle, liver and post synaptic in CNS
a2: pancreatic islet B cells, platelets, nerve terminals, CNS. vascular smooth muscle, pre and post synaptic

Question 18

cAMP

Cyclic adenosine mknophosphate

Answer 18

Second messenger that mediates biological responses

Question 19

Presynaptic Alpha 2 are g-protein linked receptors

Answer 19

Inhibits release of norepinephrine

Negative feedback system for norepinephrine release

Question 20

a1 vascular agonist

Answer 20

Dopamine, phenylephrine, methoxamine

Question 21

Alpha 1 : Gq

Answer 21

Vasocontriction: Smooth muscle contraction
GU: Urinary retention
LIVER: Glycogenolysis= ⬆️glucose⬇️ renin
Postsynaptic CNS: excitation, pupil dilation

Alpha 1 Agonist: Phenylephrine*

Question 22

Alpha 2 (GI) : Adrenergic Receptor

Answer 22

⬇️cAMP: hyperpolarization ⬇️ intracellular Ca2+
Presynaptic: ⬇️ NE release, ⬇️ HR,
Postsynaptic: Vasocontriction and platelet clusters
Pancreas B cells: ⬇️insulin ⬆️ glucose

Alpha 2 Agonist: Clonidine

Question 23

Beta 1 : Adrenergic Receptor

Answer 23

⬆️cAMP = ⬆️Ca2

HEART: ⬆️ HR ⬆️ Contractility
KIDNEY: ⬆️ Renin ⬆️ BP

Beta 1 AGONIST: DOBUTAMINE

Question 24

Beta 2: Andrenergic Receptor (Gs)

Answer 24

⬆️cAMP ⬆️Ca2+
LUNGS: Bronchodilaton
VASCULAR: Vasodilation
GI/GU: ⬇️ GI motility and inhibtion of labor

Beta 2 Agonist : Albuterol, Salmetrol

Question 25

Dopamine: Adrenergic Receptor

D1, D5

Answer 25

⬆️cAMP ⬆️Ca2

BRAIN: different areas
PERPHERAL TISSUES: VASODILATION
KIDNEYS: DILATION

Question 26

D2, D3, D4 Adrenergic Receptor

Answer 26

⬇️cAMP

Opposite of D1 And D5

Question 27

Cholingeric Receptors

Answer 27

1) Nicotinic: ligand-gated ion channel

2) Muscarinic: g protein coupled

Question 28

Nicotonic Receptor: Cholinergic 2 receptor subtypes…

Ligand-ion gated channel: FAST

Answer 28

1) Nm: Neuromuscular Junction
- Depolarization muscle contraction
- Postsynaptic skeletal neuro-muscular junction
- Nicotonic agonist: SUCCINYLCHOLINE
2) Nn: Ganglia
- Depolarization transmission of cholinergic signals
- Autonomic ganglia (post-ganglionic)
- Adrenal medulla

Question 29

GABA RECEPTORS: (inhibitors) CNS depression

GABA A (fast)

GABA B (slow)

Answer 29

GABA A: Ligand-gated ion channel

Brain: barbiturates and benzodiazepines

Allow Chloride ions to go into neurons: (-)intracellular (+) extracellular: causes hyperpolarized less likely to have an action potential

Question 30

GABA RECEPTORS (inhibtors) CNS depression

GABA A (fast)

GABA B (slow)

Answer 30

GABA B: G-Protein Couple

Peripheral Tissue: baclofen an antispasmodic agent

Activate potassium channels: hyperpolarization to decrease action potential

Question 31

Serotonin

ligand-gated ion channel (fast)

Directly coupled to fast Na+ and K+ ion channels

Answer 31

CNS, periphery, GI tract

Zofran (Ondansetron) = antagonist

Question 32

Name the 3 opioid receptors

G-protein-coupled receptors

Answer 32

Mu (MOR)
Kappa (KOR)
Delta (DOR)

Question 33

Mu (MOR) side effects and drug example

Opioid Receptor

Answer 33

Activation causes respiratory depression, decreased GI motility

Agonist: MOrphine
Antagonist: Narcan

Question 34

Kappa (KOR) side effects and drug example

Opioid Receptor

Answer 34

Decreased GI motility

Dysphoria

Question 35

Delta (DOR)

Opioid Receptor

Answer 35

Supraspinal and spinal analgesia

Activation causes modulation of hormone and neurotransmitter release

Question 36

Cytochrome P450 (CYP) 3A4

GENETICS: Where is it found in the body?

Answer 36

LIVER AND INTESTINES

Question 37

Cytochrome P450 (CYP) 3A4 Why is it relevant to anesthesia?

Answer 37

It is responsible for the metabolism of the half-life in anesthesia drugs

Question 38

Four environmental factors that affect metabolic pathways

Answer 38

smoking
alcohol
dietary supplements
diet

Question 39

Stereochemistry

Answer 39

study how molecules are the structured and their manipulation