. 2021 Apr 8;26(8):2149. doi: 10.3390/molecules26082149

Table 1.

Inhibitory potency (IC50) of SSRIs for different nAChR subtypes.

nAChR Subtype	SSRI	Method	IC₅₀ (μM)	References
hα4β2	Fluoxetine	Voltage-clamp	1.83	[69]
	Fluoxetine	Ca²⁺ influx	4.4 ± 0.6	[70]
	Paroxetine	Ca²⁺ influx	8.6 ± 2.3	[70]
	Citalopram	Ca²⁺ influx	19.0 ± 4.2	[68]
rα2β4	Fluoxetine	Voltage-clamp	0.37 ^b	[71]
	Fluoxetine	Voltage-clamp	0.45 ± 0.03 ^c	[27]
	Nor-fluoxetine	Voltage-clamp	0.13 ^b	[71]
	Zimelidine	Voltage-clamp	0.67 ^b	[71]
hα3β4	Fluoxetine	Ca²⁺ influx	2.0 ± 0.4	[70]
	Paroxetine	Ca²⁺ influx	2.6 ± 0.3	[70]
	Citalopram	Ca²⁺ influx	5.1 ± 1.3	[68]
rα3β4	Fluoxetine	Voltage-clamp	0.64 ± 0.03 ^c	[27]
rα4β4	Fluoxetine	Voltage-clamp (+100–200 µM Zn²⁺)	0.3 ± 0.045 ^d 0.17 ± 0.018 ^d	[72]
rα3β4α5	Fluoxetine	⁸⁶Rb⁺ efflux	2.5	[73]
	Paroxetine	⁸⁶Rb⁺ efflux	4.9	[73]
	Sertraline	⁸⁶Rb⁺ efflux	3.1	[73]
hα7	Fluoxetine	Voltage-clamp	1.6	[74]
		Ca²⁺ influx	4.7 ± 0.83	[75]
		Ca²⁺ influx	4.9 ± 1.0	[70]
		Voltage-clamp	5.27	[69]
	Paroxetine	Ca²⁺ influx	8.6 ± 2.0	[70]
	Paroxetine	Ca²⁺ influx	9.1 ± 0.6	[75]
	Sertraline	Ca²⁺ influx	10.0 ± 0.81	[75]
	Citalopram	Ca ²⁺ influx	18.8 ± 1.1	[68]
Hippocampal rα7 *	Nor-fluoxetine	Voltage-clamp	0.82 ± 0.04 ^a	[76]
	Fluoxetine	Voltage-clamp	0.66 ± 0.06 ^a	[76]
	Escitalopram	Voltage-clamp	28.9 ± 5.1	[76]
hα3β2	Fluoxetine	Voltage-clamp	4.14	[69]
rα9α10	Citalopram	Voltage-clamp	7.5 ± 0.9	[68]
mα1β1γδ	Fluoxetine	⁸⁶Rb⁺ efflux	2.1	[73]
		Voltage-clamp (0 mV)	2.2	[26]
		Voltage-clamp (+100–200 µM Zn²⁺)	0.45± 0.04 ^d 0.19 ± 0.02 ^d	[72]
		Voltage-clamp	0.22 ^b	[71]
		Voltage-clamp	0.3 ^e	[27]
hα1β1γδ	Fluoxetine	Ca²⁺ influx: 5 min pre-incubation 240 min pre-incubation 1440 min pre-incubation	1.8 ± 0.6 0.22 ± 0.01 0.17 ± 0.08	[77]
hα1β1εδ	Fluoxetine	Ca²⁺ influx	0.85 ^b 0.55 ^b	[30]
mα1β1γδ	Nor-fluoxetine	Voltage-clamp	0.07 ^b	[71]
hα1β1γδ	Paroxetine	Ca²⁺ influx: 5 min pre-incubation	4.8 ± 0.6	[77]
mα1β1γδ	Paroxetine	⁸⁶Rb⁺ efflux	5.6	[73]
mα1β1γδ	Sertraline	⁸⁶Rb⁺ efflux	3.5	[73]
Habenular mα3β4 *	Citalopram	Patch-clamp	7.6 ± 1.0	[68]
Hippocampal nAChRs	Citalopram	Nicotine-evoked NA release	0.93	[78]
Hippocampal nAChRs	Fluoxetine	Nicotine-evoked NA release	0.57	[78]
nAChRs from superior cervical ganglion	Fluoxetine	Ca²⁺ influx	2.0	[69]

h, human. r, rat. m, mouse. * denotes the potential existence of other subunit(s). The ratio between the agonist-induced response in the presence of the antidepressant and the control agonist-induced response at the respective concentration of the antidepressant (^a 20, ^b 10, ^c 2, ^d 5, and ^e 1 µM, respectively).