Zusammenfassung der Ressource
Drugs acting
on ion channel
- Importance of ion channels
- Neuronal excitability -
action potential
neurotransmitters
- coupling contraction-
muscle (NMJ)
- control the volume - prevent
from swelling
- Mutation in channels can lead to
channelopathies - LQ syndrome
- animal venom - blocking neurotoxin
- dendrotoxin
- W-agatoxin IV and
W-agatoxin IIIA
- apamin
- Puffer fish has TTX in
the intestines
- Mechanisms of ion channel modulation - TTX
- sy,mbiotic organism
- Block Na Channel
- Na channel mechanism
- Guanidium moiety
- Puffer fish has Glutamate
on 387 - does not get
affected
- cardiac Na channel
- 385, (cys) 387(glutamine), 388 (Arg)
- Local Anesthetics
- Two groups - aromatic
ring +
ester(procaine)/amide
(lidocaine)
- Hydrophilic pathway
- LA block when Na channel is
open
- Hydrophobic pathway
- LA enters when
channel inactivated
- pore portals
- Unwanted effects
- CNS
- cardiovascular
- Binds to F1759 ub Nav1.5
- physical block
- electrostatic repulsion
- Other drugs acting on channel
- Anticonvulsants - carbazepine
- Class I antidyshythmic drugs
- Dihydropyrifine -
Ca antagonist
- Tolbutamine - BK channel
- isoflurane - two K pore domain