Table 1.

−Log(EC₅₀) of the Propofol Analogues for Potentiation of GABA_A Responses, Direct Activation, and Anesthetic Action in Tadpoles

Compd	Potentiation	Direct activation	Tadpole LORR	ClogP
1, phenol	3.0*	1.0	2.8*	1.5
2, 2,6-dimethylphenol	3.9*	3.7*	4.2*	2.5
3, 2,6-dimethylthiophenol	1.0	1.0	1.0	2.9
4, 2,6-dibromophenol	1.0	1.0	1.0	3.0
5, 2-isopropylphenol	4.4*	3.8*	3.9*	2.9
6, 2,6-dimethoxyphenol	1.0	1.0	1.0	1.1
7, 2-isopropylthiophenol	1.0	1.0	1.0	3.3
8, 2,6-diethylphenol	4.9*	3.9*	4.7*	3.4
9, 2-cyclopentylphenol	1.0	1.0	1.0	3.5
10, 2-hydroxy-3-isopropylbenzoic acid	1.0	1.0	1.0	3.6
11, 2-tert-butyl-6-methylphenol	6.3*	4.7*	4.5*	3.8
12, 2,6-diethylphenyl bromide	4.7*	3.9*	3.8*	5.1
13, 2,6-diethylphenyl isocyanate	4.6*	3.6*	3.8*	2.0
14, 1,3-diisopropylbenzene	1.0	1.0	1.0	5.0
15, 2,6-diethylphenyl isothiocyanate	4.8*	3.5*	3.8*	5.4
16, 2,6-diisopropylphenol (propofol)	5.7*	5.0*	5.7*	4.3
17, 3,5-diisopropylcatechol	4.4*	3.7*	4.3*	3.7
18, 2,6-diisopropylphenyl isocyanate	1.0	1.0	1.0	2.8
19, 2,4-di-tert-butylphenol	1.0	1.0	1.0	5.1
20, 3,5-di-tert-butylphenol	4.0*	3.3*	4.0*	5.1
21, 2,6-di-tert-butylphenol	1.0	1.0	1.0	5.1
22, 2,6-diisopropylphenyl isothiocyanate	1.0	1.0	1.0	6.2
23, 4-iodo-2,6-diisopropylphenol	5.0*	4.5*	5.6*	5.7
24, 2,6-di-sec-butylphenol	5.6*	4.7*	6.4*	5.4
25, 2,4-di-sec-butylphenol	4.5*	3.6*	5.0*	5.4
26, 2,6-dicyclopentylphenol	1.0	1.0	1.0	5.6
27, 2,6-dicyclohexylphenol	1.0	1.0	1.0	6.7

^aThe last column is the ClogP of each compound. Activities are expressed as −log(EC₅₀), with EC₅₀ in molar units. Experimentally obtained values are indicated by *. The inactive compounds have been assigned a −log(EC₅₀) of 1.0.