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. Author manuscript; available in PMC: 2021 May 15.
Published in final edited form as: Eur J Med Chem. 2020 Mar 23;194:112261. doi: 10.1016/j.ejmech.2020.112261

Table 1.

The pharmacological properties of the benzyl alcohol derivatives studied compared to propofol.

Structure Abbreviated name LoRR in Tadpoles EC50 ± SD, μM (# of animals) Enhancement of [3H]muscimol binding in α1β3γ2L GABAARs EC50 ± SD, μM (N) Protection against photoincorporation in the β subunit of α1β3γ2L GABAARs in the presence of GABA
[3H]azietomidate IC50, μM) (N, R2) [3H]pTFD-di-iPr-BnOH IC50, μM) (N, R2) [3H]R-mTFD-MPAB IC50, μM (N, R2)
graphic file with name nihms-1581390-t0002.jpg BnOH 2,000 ± 210a >50,000 ND ND ND
graphic file with name nihms-1581390-t0003.jpg pTFD-BnOH 28 ± 7b (30) 700 ± 81 (3) 305 ± 33 (5, 0.92) ND 465 ± 5 (5, 0.87)
graphic file with name nihms-1581390-t0004.jpg Di-iPr-BnOH 16 ± 1 (30) 40 ± 6 (2) 92 ± 6 (5, 0.97) ND 243 ± 23 (5, 0.91)
graphic file with name nihms-1581390-t0005.jpg pTFD-di-iPr-BnOH 2.5 ± 0.6 (73) 7.4 ± 0.7 (6) 460 ± 70 (4, 0.59) 18 ± 2 (4, 0.94) 26 ± 5 Bns = 42 ± 3% (4, 0.87)
graphic file with name nihms-1581390-t0006.jpg Propofol 0.63 ± 0.09c 5.4 ± 0.9 (2) 8 ± 1d 32 ± 6 (4, 0.87) 44 ± 4d
a

[38];

b

[21];

c

[37];

d

[15].

ND: not determined. N: Number of independent determinations of the EC50 or IC50.