DREADDS Flashcards
1
Q
What does DREADDS stand for?
A
Designer receptor exclusiviely activated by designer drugs
2
Q
How many types of GPCR
A
1000 GPCR, 4% of protein encoded by genome
3
Q
Two components needed for DREADD
A
Inert ligand and modified GPCR compementary to that ligand
4
Q
Muscarinc GPCR categories
A
M1,M3,M5 = Gq—- incr PLC incr DAG and IP3
M2,M4 = Gi/o —- decr Adenylyl cyclase decr CAMP
5
Q
Site diected mutagenisis in muscarince GPCR
A
Tyrosine 33rd resdiue — cysteine 3rd TM
Alanine 46th residue — Glycine 5th TM
6
Q
CNO
A
clozapine-N-Oxide most common used ligand
its inert and high bioavailability, highly potent
7
Q
hM4Di
A
CNO binds and opens K+ channels, K+ flows out = hyperdepolarisation
8
Q
hM3Dq
A
CNO binds and causes neuronal firing
