TABLE 2

Effects on other neuronal nAChR

Single-concentration tests were conducted with the compounds applied alone to determine agonism or coapplied with ACh to determine antagonism. Compounds scored as positive for agonism produced responses that were above our limit of detection and >5% the amplitude of ACh controls. Compounds scored as positive (+ or ++) for antagonism reduced ACh responses so that the coapplication responses were <80% (+) or <40% (++) the amplitude of ACh controls. The compounds in the choline series were tested at 1 mM, and all other compounds were tested at 100 µM. Dashes indicate that no activity was detected.

Compoundα3β4α4β2
AgonismAntagonismIC50Antagonism
µM
tetMA++
EtriMA++
diEdiMA++
triEMA+++
TEA+++
Choline
(2OHE)-EdiMA+
(2OHE)-diEMA+++
BtriMA+
BEdiMA++124 ± 13
BdiEMA++92 ± 33
BtriEA++39 ± 17+
diMPyrr++
EMPyrr+
diEPyrr++59 ± 3+
diMPip+++
EMPip++90 ± 4
diEPip++51 ± 1+
diMHHA++111 ± 14
EMHHA++55 ± 4+
diEHHA+++21 ± 1.5+