50. Receptors and Signalling

Question 1

what type of receptor is bound and activated by the neurotransmitters/hormones - adrenaline and noradrenaline

Answer 1

G protein coupled adrenoreceptors

Question 2

alpha 1 is Ga….
activation of phosp….. …
Increase of I…. and D…
contraction of ?

Answer 2

Gaq
Phospholipid C
IP3 and DAG
vascular smooth muscle

Question 3

alpha 2 Ga…
inhibition of ……
decrease of c…..
increase of ….. channels
decrease of …… channels
relaxation of the….
Inhibition of n……

Answer 3

Gai
adenylyl cyclase
cAMP
K+ channels
GI tract
noradrenaline

Question 4

Beta 1 is Ga…
stimulation of aden…..
increase of c….
Increased

Answer 4

Gas
adenylyl cyclase
cAMP
Heart rate and cardiac muscle contraction

Question 5

Beta 2 is Ga…
stimulation of aden…..
increase of c….
Dilation of the

Answer 5

Gas
adenylyl cyclase
cAMP
Bronchi
(also incr. HR but to a lesser extent than B1)

Question 6

Beta 3 is Ga…
stimulation of aden…..
increase of c….
causes……

Answer 6

Gas
adenylyl cyclase
cAMP
Thermogenesis in skeletal muscle

Question 7

what binds/activates B2 adrenoreceptors to cause bronchodilation for asthmatic patients

Answer 7

salbutamol

Question 8

what binds/activates B1 and B2 adrenoreceptors to cause bronchodilation and has a massive side effect of Tachycardia

Answer 8

Isoprenaline

Question 9

name some of Beta1 agonists

Answer 9

Noradrenaline
Adrenaline
Pindolol (partial )

Question 10

name some of Beta2 agonists

Answer 10

Adrenaline
Noradrenaline
Salbutamol
Salmeterol
Pindolol (partial)

Question 11

name 6 beta blockers (antagonists)

Answer 11

Bisoprolol
atenolol
propranol
metoprolol
carvedilol
sotalol

Question 12

Receptors may be divided into 4 main ‘super-families’ or classes based upon their common structure and function?
name them.

Answer 12

Ligand gated ion channels
G protein coupled receptors
Kinase linked receptors
nuclear receptors

Question 13

Give an example of a Ligand gated ion channel

Answer 13

Nicotinic acetylcholine receptor

Question 14

Nicotinic acetylcholine receptor are permeable to what?

Answer 14

Na+, K+ and Ca2+

Question 15

what do Nicotinic acetylcholine receptors do

Answer 15

Modulate fast synaptic excitation in the nervous system - excitatory post-synaptic potentials (EPSPs) and motor endplate potentials (EPPs). Also expressed on the post-ganglionic neuronal cell bodies in the autonomic nervous system

Question 16

Drugs that act at as agonists at nicotinic acetylcholine receptors (nAChRs) are…?

Answer 16

acetylcholine
Nicotine
Varenicline (partial)

Question 17

which drug is a phosphodiesterase inhibitor -> inndicated fro COPD

Answer 17

Theophylline

Question 18

kinase linked receptors are

Answer 18

insulin receptors

Question 19

kinase linked receptors are also called

Answer 19

enzyme coupled receptors

Question 20

kinase linked receptors, when activated cause

Answer 20

parallel signaling cascades

Question 21

Nuclear receptors are generally bound by….

Answer 21

steroid hormones

Question 22

Nuclear receptors are ……….so are not …………. to the cell membrane

Answer 22

Intracellular…. Bound.

Question 23

Nuclear receptors contain

Answer 23

DNA binding domains allowing for the control for gene transcription

Question 24

what is the nuclear receptor structure

Answer 24

N-AF1-DBD-Hinge-LBD-AF2-C

AF-activation function site
DBD- DNA binding domain
LBD-Ligand binding domain

Question 25

steroid hormones are ……… and pass through the plasma membrane to bind to nuclear receptors

Answer 25

Lipophillic

Question 26

Drug Targets can be divided into 4 main categories:

Answer 26

1. Receptors
   
   2. Enzymes
   3. Ion Channels
      
      4. Carrier Proteins

Question 27

what is ibuprofen

Answer 27

a non steroidal anti inflammatory drug (NSAID) that acts at cyclooxygenase enzymes

Question 28

how does ibuprofen work

Answer 28

It works by blocking enzymes in your body known as cyclooxygenase enzymes (COX-1 and COX-2).
These enzymes usually help produce substances called prostaglandins.
Prostaglandins are involved in causing pain, swelling, and inflammation by making blood vessels widen (vasodilation).

Question 29

what side effects for taking ibuprofen

Answer 29

Irritation of the GI tract, possible impairment of renal function via inhibition of prostaglandin-evoked vasodilation.

Question 30

what kind of drug is amlodipine

Answer 30

calcium channel blocker (antihypertensive)

Question 31

when is amlodipine used

Answer 31

when a patient has angina and/or hypertension

Question 32

how does amlodipine work

Answer 32

Calcium channel blocker so is an antagonist at Cav1.3 however slow association and long duration of action

Question 33

what are SSRIs and what are they commonly used to treat

Answer 33

SSRIs stand for Selective Serotonin Reuptake Inhibitors. They are a class of drugs commonly used to treat depression and anxiety disorders.

Question 34

what is SERT

Answer 34

Serotonin Transporter. It’s a protein that plays a crucial role in the brain’s serotonin system.

Question 35

what is the function of SERT

Answer 35

is responsible for transporting serotonin, a neurotransmitter, from the space between nerve cells (the synaptic cleft) back into the nerve cell that released it (the presynaptic neuron).
This process is known as serotonin reuptake.

Question 36

so what is the role in SSRIs in reducing depression

Answer 36

SSRIs (Selective Serotonin Reuptake Inhibitors) work by blocking SERT. This inhibition increases the amount of serotonin available in the synaptic cleft, which can help improve mood and reduce anxiety

Question 37

name some drugs that act as SSRIs (antagonists at SERT)

Answer 37

Citalopram
Escitalopram
Fluoxetine
Fluvoxamine
Paroxetine
Sertraline

Question 38

Sodium Valproate is used to treat who?

Answer 38

Epileptic people

Question 39

Sodium Valproate has many what….

Answer 39

mechanisms of action