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. Author manuscript; available in PMC: 2024 Jan 1.
Published in final edited form as: Adv Neurobiol. 2023;30:101–129. doi: 10.1007/978-3-031-21054-9_4

Table 4.7.

Systematic SAR exploration of citalopram and talopram analogs

Compound X Y Z R SERT S1
binding IC50
(μM)		 T1/2 for [3H]S-CIT
dissociation (min)		 SERT allosteric
potency IC50 (μM)
Escitalopram (16a) CN F H CH3 0.010 [0.0008; 0.013] 790 ± 160 5.8 [5.4; 6.3]
Talopram (16n) H H CH3 H 0.718 100 ± 3.8 ND
16o CN F H H 0.041 [0.032; 0.051] 380 ± 26 10.1 [10.0; 10.2]
16p CN F CH3 CH3 6.4 [4.7; 8.8] 1090 ± 130 3.6 [3.3; 3.8]
16q CN H CH3 CH3 10 [9.2; 12] 440 ± 30 12 [10; 13]

ND not determined