Table 1. Comparison of Dopamine, Serotonin, and Norepinephrine Transporter Uptake Inhibition and Release Data for a Series of N-Alkylpropiophenones Using Rat Synaptosomes^a.

							DATb		SERTb
PAL #	compd	Z	R1	R2	X	Y	inhibition IC50 (nM)	release EC50 (nM)	inhibition IC50 (nM)	release EC50 (nM)
433	3a	O	CH(CH2CH2)	H	Cl	H	533 ± 61			1328 ± 148
							265 ± 94c		3180 ± 170c
1122	(−)-3a	O	CH(CH2CH2)	H	Cl	H	294 ± 24			562 ± 152
1123	(+)-3a	O	CH(CH2CH2)	H	Cl	H	369 ± 40			733 ± 163
363	6	O	nC3H7	H	Cl	H	793 ± 66		>10k
361	7	O	C2H5	H	Cl	H	5920 ± 621		>10k
586	3b	O	CH(CH2CH2)	H	Br	H	386 ± 29			621 ± 141
588	3c	O	CH(CH2CH2)	H	CH3	H	1104 ± 69			1067 ± 203
591	3d	O	CH(CH2CH2)	H	OCH3	H	2372 ± 175			1014 ± 118
743	3e	O	CH(CH2CH2)	H	H	Cl	2011 ± 178			1632 ± 161
744	3f	O	CH(CH2CH2)	H	H	CH3	1103 ± 884			667 ± 92
787	3g	O	CH(CH2CH2)	H	Cl	Cl	425 ± 22			356 ± 96
820	3h	O	CH(CH2CH2)	H	Cl	CH3	592 ± 31			181 ± 31
304	8	H,H	H	H	Cl	H		11.8 ± 0.7		120 ± 6
434	9	O	CH3	H	Cl	H		46.8 ± 4.0		410 ± 38
426	10	H,H	CH3	CH3	H	H		225 ± 9		4698 ± 479
429	11	O	CH3	CH3	H	H		411 ± 98	>10K
550	12	H,H	H	C2H5	H	H	2596 ± 408		>10K

^aND = not determined; PAL = phenyl amine library.

^bData are represented as means ± SD and are the result of N = 3 performed in triplicate.

^cData from Carroll et al.¹