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Vol. 284, Issue 2, 777-789, February 1998
2
4, 34 and
44 Stably Expressed in HEK293 Cells
SIBIA Neurosciences, Inc., La Jolla, California
Human embryonic kidney (HEK293) cells were transfected with cDNA
encoding the human 
4 neuronal nicotinic acetylcholine (ACh) receptor
subunit in pairwise combination with human 
2, 3 or 4 subunits.
Cell lines A2B4, A3B4.2 and A4B4 were identified that stably express
mRNA and protein corresponding to 2 and 4, to 3 and 4 and
to 4 and 4 subunits, respectively. Specific binding of
[3H]epibatidine was detected in A2B4, A3B4.2 and A4B4
cells with Kd (mean ± S.D. in pM) values
of 42 ± 10, 230 ± 12 and 187 ± 29 and with
Bmax (fmol/mg protein) values of 1104 ± 338, 2010 ± 184 and 3683 ± 1450, respectively. Whole-cell
patch-clamp recordings in each cell line demonstrated that (
)nicotine
(Nic), ACh, cytisine (Cyt) and 1,1-dimethyl-4-phenylpiperazinium iodide
(DMPP) elicit transient inward currents. The current-voltage
(I-V) relation of these currents showed strong
inward rectification. Pharmacological characterization of
agonist-induced elevations of intracellular free Ca++
concentration revealed a distinct rank order of agonist potency for
each subunit combination as follows: 24, (+)epibatidine (Epi) > Cyt > suberyldicholine (Sub) = Nic = DMPP; 34,
Epi > DMPP = Cyt = Nic = Sub; 44, Epi > Cyt = Sub > Nic > DMPP. The noncompetitive
antagonists mecamylamine and d-tubocurarine did not display subtype
selectivity. In contrast, the Kb value for the
competitive antagonist dihydro--erythroidine (DHE) was highest at
34 compared with 24 or 44 receptors. These data
illustrate that the A2B4, A3B4.2 and A4B4 stable cell lines are
powerful tools for examining the functional and pharmacological
properties of human 24, 34 and 44 neuronal nicotinic
receptors.
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