Important Drugs and Their Function

Question 1

Cav2.x

Answer 1

blocked by agatoxin, conotoxins, SNX-482. Found in nerve body

Question 2

Cav3.x

Answer 2

blocked by kurtoxin (scorpion venom) andd found in the synapse

Question 3

Cav1.x

Answer 3

modulated by dihydropyridines (DHP)

Question 4

hERG K+ channels expressed in HEK293 (Kv11.1)

Answer 4

blocked by cisapride, induced cardiac pathology to induce or treat arrhythmia

Question 5

The problem with extended depolarization

Answer 5

longer we depolarize, the more K+ channels open and there is more backflow

Question 6

KvLQT channels (Kv7.x)

Answer 6

heart attack

Question 7

K+ channel blockers in nature

Answer 7

BDS-I, BDS-II, Charybdotoxin, Agitoxins, Dendrotoxins, Apamine

Question 8

SUR2B

Answer 8

target to modify insulin secretion by increasing amount secreted

Question 9

Cholinergic

Answer 9

• acetylcholine
• cation channel
• EPSP
• 4 transmembrane
• 5 to make a channel

Question 10

Biogenic Amines

Answer 10

• serotonin
• cation channel
• EPSP
• 5HT3R
• 4 transmembrane
• 2 cytosolic loops

Question 11

Purines

Answer 11

• ATP
• Cation channel
• EPSP
• 2 transmembrane
• 3 to make a channel

Question 12

Amino Acids

Answer 12

• glutamate
• cation ion channel
• EPSP
• 3 transmembrane
• 4 to make a channel
• Glycine and GABA
• Cl- channels
• IPSP
• 4 transmembrane
• 5 to make a channel

Question 13

M2 portion of transmembrane segment

Answer 13

important for ion selectivity

Question 14

Nicotinic Acetylcholine Receptor Agonists

Answer 14

Nicotine, carbamylcholine, succinylcholine, levamisole, pyrantel

Question 15

Nicotinic Acetylcholine Receptor Antagonists

Answer 15

trimethaphan (ganglionic block), alpha-bungarotoxin, curare

Question 16

alpha bunarotoxin

Answer 16

cobra venom, competitive antagonist, high R affinity

Question 17

Serotonin HT3 receptor agonists

Answer 17

2-methyl serotonin

Question 18

Serotonin HT3 receptor antagonists

Answer 18

Dolasetron (helps with vomiting and nausea), Ondasetron, Granisetron, Palonosetrom, Alosetron (withdrawn from the market for side effects)

Question 19

5-HT3R antagonist

Answer 19

non-selective channels, supposed to help with nausea and vomiting in cancer patients

Question 20

Purinergic Receptors (P2X) agonists

Answer 20

ATP, alphabeta methylene ATP

Question 21

Where are P2X receptors found?

Answer 21

in the CNS, PNS, neuroglia

for mechanosensation, neuromodulation, neuropathic pain

Question 22

Glutamate receptor subtypes (NMDA and non-NMDA)

Answer 22

kainate, AMPA and NMDA

Question 23

NMDA - glutamate receptor

Answer 23

• glycine required to bind at separate binding site to partially depolarize.
• voltage as cofactors
• antagonists: ketamine and PCP

Question 24

non-NMDA - glutamate receptor

Answer 24

• Kainate and AMPA

- found in dorsal root ganglion and CNS

Question 25

Glycine receptor agonist

Answer 25

Glycine, beta-alanine, taurine

Question 26

Glycine receptor antagonist

Answer 26

Strychnine - rodent poison

Question 27

GlyR structure info

Answer 27

• mutations lead to hyperkplexia

- cytosolic region reacts with Gephrin

Question 28

GABA receptor agonist

Answer 28

GABA, Baclofen, muscimol, benzodiazepines, ethanol, barbiturates, avermectins, volatile anesthetics, some steroids –> used to treat seizures

Question 29

GABA receptor antagonist

Answer 29

bicuculline, gabazine, some steroids, picrotoxin –> these are all seizure inducing and not used clinically only for research

Question 30

GABA receptor inverse agonist

Answer 30

DMCM, Ro15-4513 (used for alcohol poisoning)

Question 31

Gephyrin

Answer 31

is a scaffolding component, is linked to receptors, tubules, actin, collybistin and neuroligin 2

Question 32

Acetylcholine fate

Answer 32

broken down by cholinesterase

Question 33

Serotonin fate

Answer 33

Reuptaken by SERTs or broken down by monoamine oxidase

Question 34

Glycine/GABA/Glutamate fate

Answer 34

Reuptaken perisynaptically by glial cells (GlyT1, GAT-3, EAAT1/2 GLT1) or presynaptically by GlyT2, GAT-1, EAAT3/4