Drug-Receptor Interactions

Question 1

Receptor

Answer 1

Proteins that participate in intracellular communication via chemical signals

Question 2

Ligands

Answer 2

molecules that bind to receptors

Question 3

Ligands include:

Answer 3

drugs and endogenous signaling molecules (hormones and neurotransmitters)

Question 4

A particular cell function may be increased or decreased by

Answer 4

activation of the cell’s receptor by a ligand

Question 5

A ligand may interact with

Answer 5

multiple receptor subtypes

Question 6

This binding “unlocks” the cell’s response

Answer 6

ligand binding to it’s receptor

Question 7

Agonist

Answer 7

A drug that causes the receptor to respond the same way as the naturally occurring substance. “pick the lock”.

Question 8

Antagonist

Answer 8

Drug binds to receptor but doesn’t produce response. Prevents binding of endogenous hormone or neurotransmitter.

Question 9

Ligand-Gated Ion Channels

Answer 9

Located on cell surface. Transmembrane. Nicotinic Ach, Glutamate, Glycine, and GABA.

Question 10

Protein receptors

Answer 10

Tyrosine kinase linked. cell surface. transmembrane. GF, insulin, peptide hormones.

Question 11

G-Protein-Coupled receptors

Answer 11

cell surface. transmembrane. muscarinic receptor, alpha and beta adrenergic receptor, eicosamoids.

Question 12

Ligand-Activated Transcription factors

Answer 12

cytoplasm. steroid hormones, thyroid hormones, vit D.

Question 13

Transmembrane ion channels

Answer 13

ligand or voltage gated. Nicotinic Ach receptor (Na+ flux), GABA receptor (Cl- flux), glycine receptors, glutamate receptors

Question 14

Alpha1-adrenergic receptor

Answer 14

activation of phospholipase

Question 15

Alpha2-adrenergic receptor

Answer 15

inhibition of adenylyl cyclase

Question 16

B-adrenergic receptor

Answer 16

stimulation of adenylyl cyclase

Question 17

Muscarinic receptor

Answer 17

activation of phospholipase

Question 18

Transmembrane receptors with enzymatic cytosolic domains

Answer 18

tyrosine kinase (insulin and GF), tyrosine phosphatases (found in immune cells), guanylyl cyclases (natriuretic peptide)

Question 19

Intracellular transcription factor receptor

Answer 19

steroids, androgens, estrogen, thyroid, hormone, VitD, retinoid

Question 20

Extracellular transcription factor receptor

Answer 20

ACE, acetylcholinesterase

Question 21

Adhesion receptor

Answer 21

integrins

Question 22

Ligand-binding domain can be found

Answer 22

extracellularly, within the channel, or intracellularly.

Question 23

Two important drug classes act by altering the conductance of ion channels

Answer 23

local anesthetics and benzodiazepines