Test 2

Front 1

Pharmacological Antagonism

Back 1

process of inhibiting or preventing an agonist-induced receptor response

Front 2

Competitive antagonism (def)

Back 2

-both agonist and antagonist bind to the same recognition site at the same time and their presence causes competition for such sites
-antagonist can be overcome with increasing concentration of agonist

Front 3

Effect Curve (competitive antagonism)

Back 3

-curve shifts to the right
- degree of shift depends on antagonist []

Front 4

Noncompetitive antagonism (def)

Back 4

- prevent agonist action in a way that can not change with increased agonist []

Front 5

Effect curve (noncompetitive antagonism)

Back 5

-curve doesn't reach maximum of the agonist only curve
-curve w/agonist only and noncompetive curve still have the same ED50

Front 6

Physiological antagonism

Back 6

2 drugs bind to diff. receptors and counterbalance each other by producing opposite effects

Front 7

Biochemical antagonism

Back 7

one drug indirectly decreases the amt of second drug that would otherwise be available to the site of rxn

Front 8

Chemical antagonism

Back 8

rxn b/w another molecule to form an inactive product

Front 9

Inverse agonist

Back 9

the drug has a higher affinity will produce an opposite of the agonist (often confused with competitive antagonist)

Front 10

Full agonist

Back 10

has a higher affinity for the acitve state of conformation that drives the receptor to be activated

Front 11

Partial agonist

Back 11

has a moderate affinity for the active conformation and produces an effect that will be less even at saturating concentrations

Front 12

Competitive agonist (in terms of affinity)

Back 12

bind with equal affinity for the active and inactive state and will not alter equilibrium

Front 13

Quantal dose-effect

Back 13

all or none affect; either the drug causes the receptor to reach the maximum capability or it doesn't

Front 14

TD50
LD50
ED50

Back 14

=median toxic dose
=median lethal dose
=median effective dose

Front 15

CSF <1

Back 15

drug is not safe (flatter curve on the graph=greater likelihood of undesirable effects w/in therapeutic range

Front 16

CSF >1

Back 16

dose is effective in 99% of the population and lethal in 1% of the population

Front 17

Pre-Pro-hormones

Back 17

-encoded by genes
-transcribed into mRNA
-translated into pre-pro-hormones
-processed to give the secreted and active form

Front 18

Pathway of pre-pro-hormone

Back 18

1. N-terminal signal peptide targets hormone precursor to the RER
2.uptake into RER occurs during translation
3.precursors progress through Golgi network and are delivered to membrance in secretory vesicles
4.processing to mature forms begins during these transitions

Front 19

Steps in RER and Golgi

Back 19

1. conversion of pre-pro-hormone to pro-hormones
2.proteolytic conversion of pro-hormones to mature hormones

Front 20

Purpose of pre-pro-hormone

Back 20

1. ensures transport through secretory pathway
2.delays activation

Front 21

Places of proteolytic processing (sites and locations)

Back 21

at dibasic amino acid sites
1.begins in trans golgi network
2.continues in secretory vesicle
3. final steps can occur in the extracellular fluid after secretion

Front 22

Enkephalin precursor

Back 22

-single gene that encodes multiple copies of single hormone
-encodes 6 Met-ENK molecules and 1 Leu-ENK molecule

Front 23

Enkephalin (fxn.)

Back 23

alleviate pain and promote euphoric effects

Front 24

Opiomelanocortin precursor

Back 24

-single gene that encodes several different hormones
-mature hormones have diverse biological activity

Front 25

Pre-pro-insulin

Back 25

-single gene encodes an inactive precursor of a single hormone
-conversion to pro-insulin occurs in the ER
-transition to mature insulin happens in the secretory vesicles by removal of C-peptide

Front 26

Pleomorphic phenotypes

Back 26

-result from mutations in a single gene coding for more than one protein
-result from mutations in prohormone processing enzymes (that act on more than one hormone)

Front 27

Pharmacology

Back 27

science of how drugs act on the body and how the body acts on drugs

Front 28

Agonist

Back 28

bind to the physiological receptors and mimic stimulatory effects

Front 29

Antagonists

Back 29

-bind to receptors and prevent binding (and activation) by agonists
-exhibit no direct activity
-block the activity of endogenous signaling molecule

Front 30

Full agonist

Back 30

produces maximal tissue response

Front 31

Partial agonist

Back 31

produce less than maximum repsonse

Front 32

Hydrophilic hormones

Back 32

stimulate networks of intracellular signal transduction pathways

Front 33

Hydrophilic hormones (regulate)

Back 33

-protein phosphorylation
-GTP hydrolysis
-protein localization

Front 34

Sensor/Producer cells

Back 34

-sense specific stimuli from the external environment
-produce hormones in responser to these stimuli

Front 35

Target Cells

Back 35

-have receptors for hormones
-hormone binds and causes the target cell to respond by changing their cellular fxns

Front 36

Hormones

Back 36

-intercellular info carriers b/w sensor and target cells
-coordinate acitivites of different cells in a multicellular organism

Front 37

Receptors (hormone lecture)

Back 37

-proteins that bind hormones with high specificity and affinity

Front 38

Responses

Back 38

-changes in any cellular processes including gene expression, enzyme activities, proliferative capacity, secretory proteins, and morphology

Front 39

Classical hormones

Back 39

-radius of action
~endocrine:produced by endocrine glands and transported by circulatory sys to target cells
~paracrine: produced by cells that are in close proximity to the target cells
~autocrine:produced by cells that are also the targets

Front 40

Chemical hormones

Back 40

-water solubility
~hydrophilic:bind to receptors on the outer surface of the cell
~lipophilic:bind to intracellular receptors

Front 41

Lipophilic hormones

Back 41

-control gene expression
-diffuse through plasma membrane
-bind to intracellular receptors that are xscriptional factors

Front 42

Hydrophilic hormones

Back 42

-control activities of cellular proteins including:
-enzymes
-xscription factors
-cytoskeletal proteins
-bind to the extracellular domain of cell surface receptors that span the membrane
-binding "activates" cytoplasmic domain

Front 43

Receptors (hydrophilic vs. lipophilic)

Back 43

-Hydrophilic are transmembrance proteins

Front 44

G-protein receptors

Back 44

-heterotirmeric protein, regulates an effector enzyme that produce a second messenger
-mediates cellular responses from polypeptide hormones and neurotransmitters

Front 45

4 classes of receptors that bind hydrophilic hormones

Back 45

-G-protein receptors
-enzyme receptors
-ion channel receptors
-cytokine receptors

Front 46

Enzyme receptors

Back 46

-most common are tyrosine kinase receptors
-bind polypeptide hormones
-extracellular domains