Table 3. Chemical and Metabolic Stability of Aryl N-[ω-(6-Fluoroindol-1-yl)alkyl]carbamates and Aryl 4-[2-(6-Fluoroindol-1-yl)ethyl]piperidine-1-carboxylates.

		stability (%)a
comp.	R	porcine liver S9 fractions	porcine blood plasma	porcine albumin solution	PBS buffer (pH 7.4)
14	4-phenyl	76 ± 2	83 ± 9n = 8	93 ± 6n = 6	>95
26	4-fluorophenyl	69 ± 4	59 ± 13n = 6	91 ± 6n = 5	>95
27	3-fluorophenyl	62 ± 5	10 ± 3	76 ± 4	>95
28	2-fluorophenyl	76 ± 2	19 ± 6	69 ± 5	91 ± 3
29	4-cyanophenyl	n.t.	n.t.	n.t.	12 ±3
30	3-cyanophenyl	49 ± 4	< 5	<5	72 ± 3
31	2-cyanophenyl	n.t.	n.t.	n.t.	3 ± 2
33	4-carboxyphenyl	59 ± 6	37 ± 2	90 ± 9	>95
35	3-carboxyphenyl	74 ± 2	78 ± 1	93 ± 3	>95
37	2-carboxyphenyl	77 ± 3	28 ± 4	74 ± 2	73 ± 6
39	4-(carboxymethyl)phenyl	85 ± 3	88 ± 4	>95	>95
41	3-(carboxymethyl)phenyl	73 ± 2	83 ± 5	>95	>95
43	2-(carboxymethyl)phenyl	82 ± 5	89 ± 1	89 ± 3	>95
44	pyridin-3-yl	53 ± 7	<5	27 ± 3	60 ± 2
45	2-methylpyridin-3-yl	65 ± 9	23 ± 6	70 ± 8	75 ± 4
46	4-methylpyridin-3-yl	56 ± 8	8 ± 2	68 ± 6	74 ± 4
47	5-methylpyridin-3-yl	57 ± 5	<5	37 ± 4	72 ± 4
48	6-methylpyridin-3-yl	51 ± 9	<5	62 ± 4	82 ± 6
49	indol-4-yl	78 ± 4	80 ± 3	81 ± 6	>95
54	4-carboxy	66 ± 9	94 ± 3	93 ± 8	>95
56	3-carboxy	72 ± 7	>95	94 ± 3	>95
58	2-carboxy	72 ± 6	>95	89 ± 6	>95
URB597 (1)		80 ± 4	77 ± 6	95 ± 7	>95
ABX-1431 (2)		81 ± 3	95 ± 2	87 ± 6	90 ± 5
physostigmine		57 ± 4	>95	>95	>95

^aPercent of parent remaining after incubation in porcine liver homogenate, porcine plasma, or porcine albumin solution for 30 min or PBS buffer (pH 7.4) for 60 min; values are means ± standard deviations of independent determinations (n = 3, unless otherwise stated); n.t., not tested.