Table 1.

Half-maximal Concentration (IC₅₀) for Antagonizing Direct Activation by 20 μM Etomidate (in the Presence of Flumazenil) and Calculated Log Octanol/Water Partition Coefficient Values

Class	Compound Name	IC50 (μM)	95% Confidence Interval (μM)	Calculated Log Octanol/Water Partition Coefficien†
5-Aryl-1,4-benzodiazepines	Diazepam	13*	10–16*	2.96
		15	11–20
	Nordiazepam	32	17–60	3.02
	Nitrazepam	130	61–260	2.32
	Lorazepam	≥ 1,000	—	2.37
	Fludiazepam	390	210–730	2.75
	1-Me	76	53–110	1.10
	7-Me	45	35–58	2.72
	1,4’-Me	22	18–27	2.75
	1,7-Me	24	18–32	2.75
Diazolo- and triazolo- benzodiazepines	Midazolam	560	220–1,400	3.42
	Alprazolam	63	46–85	2.55
	Estazolam	59	47–74	2.29
	Imidazenil	190	110–310	2.44
Benzodiazepine antagonists	Flumazenil	≥ 1,000	—	1.29
	Bromazenil	450	150–1,400	2.01
	Iomazenil	640	210–1,900	2.27
Unclassified	Bromazepam	460	170–1,200	1.70
	4’–2-ol	54	41–73	2.28
	Clobazam	180	100–320	2.44
	Sulazepam	64	38–110	3.11
	Medazepam	≥ 1,000	—	4.12
	Diazenil	18	11–29	3.56
	Hydro-diazenil	≥ 1,000	—	2.84

[Benzodiazepine]:[Flumazenil] = 1:2 unless otherwise indicated.

^*[Diazepam]:[Flumazenil] = 1:4.

^†Calculated by ChemBioDraw Ultra 12.0.3 (Cambridgesoft, USA).