Cholinergic Receptors

Question 1

Dale, 1936

Answer 1

Identified the presence of ACh at the neuromuscular junction

Question 2

Miyazawa, 2003

Answer 2

Showed that ACh binding to the a1 subunit of nAChRs causes a1 to rotate which destabilises the gate and allows it to open enabling ions to flow through (relatively unselective-Na, K, Ca)

Question 3

Wess, 1993

Answer 3

Showed the muscarininc receptor was a GPCR with 7 transmembrane domains based on an alpha helical wheel model

Question 4

Zoli, 2014

Answer 4

(Use for any description of nAChRs)

Decline in nAChRs has been linked to cognitive dysfunction and several psychiatric disorders

Question 5

Matera, 2014

Answer 5

(Use for any description of mAChRs)
Development of muscarininc antagonists has been successful e.g Ipratropium and Tropicamide and Atropine, but development of selective agonists proves difficult because of the high levels of multiple subtype expression on cells