Neurotransmission & ANS Pharmacology III: Other Mediators: Amines, Peptides, Eicosanoids, & NO

Question 1

What precursor is Serotonin synthesised from?

Answer 1

L-Tryptophan

Question 2

What receptors does Serotonin act via?

Answer 2

5-HT receptors

Question 3

TRUE OR FALSE:
5-HT receptors are structurally similar to adrenoceptors?

Answer 3

True.
Therefore, cross-effects of drugs

Question 4

Which drug acts on the 5-HT1D receptor?

Answer 4

• Sumpatripan
• Used to treat migraines
• Agonist

Question 5

Which drug acts on the 5-HT2A receptor?

Answer 5

• Psychedelic drugs e.g. LSD
• Agonist

Question 6

Which drug acts on the 5-HT3 receptor?

Answer 6

• Ondansetron
• Used to control nausea / vomiting
• Antagonist

Question 7

What precursor is Histamine synthesised from?

Answer 7

L-histidine

Question 8

Where is Histamine stored?

Answer 8

Granules within mast cells and basophils

Question 9

Which Histamine receptor type is found on bronchial smooth muscle, ileum, and endothelial cells?

Answer 9

H1

Question 10

Which Histamine receptor type is found on gastric parietal cells, uterine smooth muscle, vascular smooth muscle, and heart?

Answer 10

H2

Question 11

Which Histamine receptor type is found in the CNS?

Answer 11

H3

Question 12

What are the FIVE Opioid Peptide Receptors?

Answer 12

1. μ (mu)
2. δ (delta)
3. κ (kappa)
4. ORL1(nociceptive)
5. ζ (zeta)

Question 13

Are Opioid Receptors ion channels or GPCRs?

Answer 13

Gi / G0 coupled

Question 14

What are TWO examples of Tachykinins?

Answer 14

1. Substance P
2. Neurokinins A & B

Question 15

Which receptors do Tachykinins act via?

Answer 15

G-protein coupled NK1, NK2 & NK3 receptors

Question 16

What is an example of a Bradykinin?

Answer 16

9-mer neuropeptide

Question 17

Which receptors do Bradykinins act via?

Answer 17

B1 & B2 receptors

Question 18

What happens when Bradykinins act on a receptor?

Answer 18

GPCRs activate phospholipase A2 that leads to prostaglandin synthesis

Question 19

TRUE OR FALSE:
Eicosanoids are pre-synthesised and stored?

Answer 19

False.
They are made ‘on demand’

Question 20

What type of structure do Prostaglandins have?

Answer 20

5-member ring structure

Question 21

What receptors do Prostaglandins act via?

Answer 21

G-protein coupled prostanoid receptors

Question 22

What type of structure do Thromboxanes have?

Answer 22

6-member ring structure

Question 23

What receptors do Thromboxanes act via?

Answer 23

Prostanoid receptors

Question 24

What is the structure of Leukotrienes?

Answer 24

Straight chain, 3 conjugated double bonds

Question 25

What receptors do Leukotrienes act via?

Answer 25

G-protein coupled leukotriene (LT) receptors

Question 26

What are Endocannabinoids derivatives of?

Answer 26

Arachidonic acid

Question 27

Where are Endocannabinoid CB1 receptors located?

Answer 27

Brain

Question 28

Where are Endocannabinoid CB2 receptors located?

Answer 28

Immune system

Question 29

What types of receptors are Endocannabinoid CB1 & CB2 receptors?

Answer 29

GPCRs
* coupled via G1 (decreases cAMP) and G0 (opens K+ channels)

Question 30

Which enzyme does Nitric Oxide activate?

Answer 30

Guanylyl Cyclase to cGMP

Question 31

Apart from NO, what TWO other gases have signalling roles?

Answer 31

CO & H2S

Question 32

What are THREE characteristics of gases with signalling roles?

Answer 32

1. Synthesised by enzymes, then diffuse 3D
2. Target protein haeme groups or redox-active amino acids
3. Short-lived, so are generated as needed